OrganismsDiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPhenomena and ProcessesAnthropology, Education, Sociology and Social PhenomenaHumanities
AminoquinolinesPrimaquineChloroquineHemolytic AgentsAntimalarialsMefloquineAmodiaquineGlucosephosphate Dehydrogenase DeficiencyPlasmodiumPlasmodium falciparumMalariaDrug ResistanceDrug Evaluation, PreclinicalWorld War IWorld War IIAmerican Civil WarWarHistory, 20th CenturyMalaria, FalciparumHalogenationFluorineSulfonamidesStereoisomerismRhodiumIridiumChloroquinolinolsPyrazinesPhosgeneMass Spectrometry
Aminoquinolines
Quinolines substituted in any position by one or more amino groups.
Primaquine
An aminoquinoline that is given by mouth to produce a radical cure and prevent relapse of vivax and ovale malarias following treatment with a blood schizontocide. It has also been used to prevent transmission of falciparum malaria by those returning to areas where there is a potential for re-introduction of malaria. Adverse effects include anemias and GI disturbances. (From Martindale, The Extra Pharmacopeia, 30th ed, p404)
Chloroquine
The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.
Hemolytic Agents
Substances that are toxic to blood in general, including the clotting mechanism; hematotoxins may refer to the hematopoietic system.
Antimalarials
Agents used in the treatment of malaria. They are usually classified on the basis of their action against plasmodia at different stages in their life cycle in the human. (From AMA, Drug Evaluations Annual, 1992, p1585)
Mefloquine
A phospholipid-interacting antimalarial drug (ANTIMALARIALS). It is very effective against PLASMODIUM FALCIPARUM with very few side effects.
Amodiaquine
A 4-aminoquinoline compound with anti-inflammatory properties.
Glucosephosphate Dehydrogenase Deficiency
A disease-producing enzyme deficiency subject to many variants, some of which cause a deficiency of GLUCOSE-6-PHOSPHATE DEHYDROGENASE activity in erythrocytes, leading to hemolytic anemia.
Plasmodium
A genus of protozoa that comprise the malaria parasites of mammals. Four species infect humans (although occasional infections with primate malarias may occur). These are PLASMODIUM FALCIPARUM; PLASMODIUM MALARIAE; PLASMODIUM OVALE, and PLASMODIUM VIVAX. Species causing infection in vertebrates other than man include: PLASMODIUM BERGHEI; PLASMODIUM CHABAUDI; P. vinckei, and PLASMODIUM YOELII in rodents; P. brasilianum, PLASMODIUM CYNOMOLGI; and PLASMODIUM KNOWLESI in monkeys; and PLASMODIUM GALLINACEUM in chickens.
Plasmodium falciparum
A species of protozoa that is the causal agent of falciparum malaria (MALARIA, FALCIPARUM). It is most prevalent in the tropics and subtropics.
Malaria
A protozoan disease caused in humans by four species of the PLASMODIUM genus: PLASMODIUM FALCIPARUM; PLASMODIUM VIVAX; PLASMODIUM OVALE; and PLASMODIUM MALARIAE; and transmitted by the bite of an infected female mosquito of the genus ANOPHELES. Malaria is endemic in parts of Asia, Africa, Central and South America, Oceania, and certain Caribbean islands. It is characterized by extreme exhaustion associated with paroxysms of high FEVER; SWEATING; shaking CHILLS; and ANEMIA. Malaria in ANIMALS is caused by other species of plasmodia.
Drug Resistance
Diminished or failed response of an organism, disease or tissue to the intended effectiveness of a chemical or drug. It should be differentiated from DRUG TOLERANCE which is the progressive diminution of the susceptibility of a human or animal to the effects of a drug, as a result of continued administration.
Drug Evaluation, Preclinical
Preclinical testing of drugs in experimental animals or in vitro for their biological and toxic effects and potential clinical applications.
World War I
Global conflict primarily fought on European continent, that occurred between 1914 and 1918.
World War II
Global conflict involving countries of Europe, Africa, Asia, and North America that occurred between 1939 and 1945.
American Civil War
1861-1865 conflict between the Union (Northern states) and the 11 Southern states that seceded and were organized as the Confederate States of America.
War
Hostile conflict between organized groups of people.
History, 20th Century
Time period from 1901 through 2000 of the common era.
Malaria, Falciparum
Malaria caused by PLASMODIUM FALCIPARUM. This is the severest form of malaria and is associated with the highest levels of parasites in the blood. This disease is characterized by irregularly recurring febrile paroxysms that in extreme cases occur with acute cerebral, renal, or gastrointestinal manifestations.
Halogenation
Covalent attachment of HALOGENS to other compounds.
Fluorine
A nonmetallic, diatomic gas that is a trace element and member of the halogen family. It is used in dentistry as flouride (FLUORIDES) to prevent dental caries.
Sulfonamides
A group of compounds that contain the structure SO2NH2.
Stereoisomerism
The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
Rhodium
Rhodium. A hard and rare metal of the platinum group, atomic number 45, atomic weight 102.905, symbol Rh. (Dorland, 28th ed)
Iridium
A metallic element with the atomic symbol Ir, atomic number 77, and atomic weight 192.22.
Chloroquinolinols
8-Hydroxyquinolinols chlorinated on the number 5 and/or 7 carbon atom(s). They are antibacterial, antiprotozoal, and antidiarrheal, especially in amebiasis, and have also been used as antiseborrheics. The compounds are mostly used topically, but have been used also as animal feed additives. They may cause optic and other neuropathies and are most frequently administered in combination with other agents.
Pyrazines
Phosgene
A highly toxic gas that has been used as a chemical warfare agent. It is an insidious poison as it is not irritating immediately, even when fatal concentrations are inhaled. (From The Merck Index, 11th ed, p7304)
Mass Spectrometry
An analytical method used in determining the identity of a chemical based on its mass using mass analyzers/mass spectrometers.

Central nervous system-mediated hyperglycemic effects of NIK-247, a cholinesterase inhibitor, and MKC-231, a choline uptake enhancer, in rats. (1/943)

We investigated the effects of intracerebroventricular administration of NIK-247 (9-amino-2,3,5,6,7,8-hexahydro-1H-cyclo-penta(b)-quinoline monohydrate hydrochloride; a cholinesterase inhibitor) or MKC-231 (2-(2-oxypyrrolidin-1-yl)-N-(2,3-dimethyl-5,6,7,8-tetrahydrofur o[2,3-b]quinolin-4-yl) acetoamide; a choline uptake enhancer) on plasma glucose level in comparison with that of neostigmine administration in rats. The extents of NIK-247- and MKC-231-induced hyperglycemia were considerably less than that by neostigmine, suggesting that the potencies of the drugs to produce the peripheral hyperglycemia may be pharmacologically negligible.  (+info)

The immune response modifier imiquimod requires STAT-1 for induction of interferon, interferon-stimulated genes, and interleukin-6. (2/943)

Imiquimod is an oral inducer of interferon (IFN) and several other proinflammatory cytokines and has been successfully used topically as an antiviral agent for the treatment of genital warts. We have investigated the molecular mechanisms by which imiquimod induces the expression of IFNs, IFN-stimulated genes (ISGs), and proinflammatory cytokines in vivo, using mice deficient in various components of the IFN signaling system. Mice deficient in the transcription factor interferon regulatory factor 1 (IRF-1) or in the serine/threonine protein kinase PKR responded normally to imiquimod, producing high levels of circulating IFN and induction of several ISGs. On the other hand, when mice deficient in STAT-1 were treated, a 32-fold reduction in the level of circulating IFN was observed, together with a lack of induction of 2-5 oligo adenylate synthetase (2-5 OAS) and IRF-1 genes. Interestingly, there was also a lack of induction of interleukin-6 (IL-6) gene expression, although tumor necrosis factor was induced and readily detected in serum. In mice deficient in the type I IFN receptor, imiquimod induced levels of IFN similar to those in control mice, but again, neither 2-5 OAS, IRF-1, nor IL-6 genes were induced in mutant mice. Our results suggest that STAT-1 plays a critical role in the mechanism of gene activation by imiquimod. Moreover, induction of IL-6 gene expression appears to be dependent on components of the IFN signaling cascade.  (+info)

Nitric oxide inhibits L-type Ca2+ current in glomus cells of the rabbit carotid body via a cGMP-independent mechanism. (3/943)

Previous studies have shown that nitric oxide (NO) inhibits carotid body sensory activity. To begin to understand the cellular mechanisms associated with the actions of NO in the carotid body, we monitored the effects of NO donors on the macroscopic Ca2+ current in glomus cells isolated from rabbit carotid bodies. Experiments were performed on freshly dissociated glomus cells from adult rabbit carotid bodies using the whole cell configuration of the patch-clamp technique. The NO donors sodium nitroprusside (SNP; 600 microM, n = 7) and spermine nitric oxide (SNO; 100 microM, n = 7) inhibited the Ca2+ current in glomus cells in a voltage-independent manner. These effects of NO donors were rapid in onset and peaked within 1 or 2 min. In contrast, the outward K+ current was unaffected by SNP (600 microM, n = 6), indicating that the inhibition by SNP was not a nonspecific membrane effect. 2-(4-carboxyphenyl)-4,4,5, 5-tetramethyl-imidazoline-1-oxyl-3-oxide (carboxy-PTIO; 500 microM), an NO scavenger, prevented inhibition of the Ca2+ current by SNP (n = 7), whereas neither superoxide dismutase (SOD; 2,000 U/ml, n = 4), a superoxide scavenger, nor sodium hydrosulfite (SHS; 1 mM, n = 7), a reducing agent, prevented inhibition of the Ca2+ current by SNP. However, SNP inhibition of the Ca2+ current was reversible in the presence of either SOD or SHS. These results suggest that NO itself inhibits Ca2+ current in a reversible manner and that subsequent formation of peroxynitrites results in irreversible inhibition. SNP inhibition of the Ca2+ current was not affected by 30 microM LY 83, 583 (n = 7) nor was it mimicked by 600 microM 8-bromoguanosine 3':5'-cyclic monophosphate (8-Br-cGMP; n = 6), suggesting that the effects of NO on the Ca2+ current are mediated, in part, via a cGMP-independent mechanism. N-ethylmaleimide (NEM; 2.5 mM, n = 6) prevented the inhibition of the Ca2+ current by SNP, indicating that SNP is acting via a modification of sulfhydryl groups on Ca2+ channel proteins. Norepinephrine (NE; 10 microM) further inhibited the Ca2+ current in the presence of NEM (n = 7), implying that NEM did not nonspecifically eliminate Ca2+ current modulation. Nisoldipine, an L-type Ca2+ channel blocker (2 microM, n = 6), prevented the inhibition of Ca2+ current by SNP, whereas omega-conotoxin GVIA, an N-type Ca2+ channel blocker (1 microM, n = 9), did not prevent the inhibition of Ca2+ current by SNP. These results demonstrate that NO inhibits L-type Ca2+ channels in adult rabbit glomus cells, in part, due to a modification of calcium channel proteins. The inhibition might provide one plausible mechanism for efferent inhibition of carotid body activity by NO.  (+info)

Possible novel mechanism for bitter taste mediated through cGMP. (4/943)

Taste is the least understood among sensory systems, and bitter taste mechanisms pose a special challenge because they are elicited by a large variety of compounds. We studied bitter taste signal transduction with the quench-flow method and monitored the rapid kinetics of the second messenger guanosine 3',5'-cyclic monophosphate (cGMP) production and degradation in mouse taste tissue. In response to the bitter stimulants, caffeine and theophylline but not strychnine or denatonium cGMP levels demonstrated a rapid and transient increase that peaked at 50 ms and gradually declined throughout the following 4.5 s. The theophylline- and caffeine-induced effect was rapid, transient, concentration dependent and gustatory tissue-specific. The effect could be partially suppressed in the presence of the soluble guanylyl cyclase (GC) inhibitor 10 microM ODQ and 30 microM methylene blue but not 50 microM LY 83583 and boosted by nitric oxide donors 25 microM NOR-3 or 100 microM sodium nitroprusside. The proposed mechanism for this novel cGMP-mediated bitter taste signal transduction is cGMP production partially by the soluble GC and caffeine-induced inhibition of one or several phosphodiesterases.  (+info)

Treatment of experimental leishmaniasis with the immunomodulators imiquimod and S-28463: efficacy and mode of action. (5/943)

There is a need for new, effective, and less toxic treatments for leishmaniasis, an infectious disease caused by Leishmania protozoa and is a major cause of suffering and morbidity in much of the developing world. Imiquimod, an immune-response modifier, has recently been approved by the Food and Drug Administration for the treatment of genital warts caused by human papillomaviruses. Imiquimod initiates a local immune reaction, including the stimulation of macrophages, resulting in resolution of human papillomavirus infection and regression of the viral lesion. Since imiquimod activates a number of immune cells, including macrophages, which are the only host cells of Leishmania species, an investigation was done to determine whether it induces leishmanicidal properties in infected macrophages in vitro and in vivo in a mouse model. Imiquimod and a related compound, S-28463, effectively stimulated leishmanicidal activity in macrophages; moreover, imiquimod stimulated signal transduction associated with inducing nitric oxide synthesis in macrophages.  (+info)

Protection against hydrogen peroxide cytotoxicity in rat-1 fibroblasts provided by the oncoprotein Bcl-2: maintenance of calcium homoeostasis is secondary to the effect of Bcl-2 on cellular glutathione. (6/943)

The oncoprotein Bcl-2 protects cells against apoptosis, but the exact molecular mechanism that underlies this function has not yet been identified. Studying H2O2-induced cell injury in Rat-1 fibroblast cells, we observed that Bcl-2 had a protective effect against the increase in cytosolic calcium concentration and subsequent cell death. Furthermore, overexpression of Bcl-2 resulted in an alteration of cellular glutathione status: the total amount of cellular glutathione was increased by about 60% and the redox potential of the cellular glutathione pool was maintained in a more reduced state during H2O2 exposure compared with non-Bcl-2-expressing controls. In our cytotoxicity model, disruption of cellular glutathione homoeostasis closely correlated with the pathological elevation of cytosolic calcium concentration. Stabilization of the glutathione pool by Bcl-2, N-acetylcysteine or glucose delayed the cytosolic calcium increase and subsequent cell death, whereas depletion of glutathione by dl-buthionine-(S, R)-sulphoximine, sensitized Bcl-2-transfected cells towards cytosolic calcium increase and cell death. We therefore suggest that the protection exerted by Bcl-2 against H2O2-induced cytosolic calcium elevation and subsequent cell death is secondary to its effect on the cellular glutathione metabolism.  (+info)

Nitric oxide stimulates cGMP production and mimics synaptic responses in metacerebral neurons of Aplysia. (7/943)

Nitric oxide (NO) acts as a neurotransmitter and neuromodulator in the nervous systems of many vertebrates and invertebrates. We investigated the mechanism of NO action at an identified synapse between a mechanoafferent neuron, C2, and the serotonergic metacerebral cell (MCC) in the cerebral ganglion of the mollusc Aplysia californica. Stimulation of C2 produces a decreasing conductance, very slow EPSP in the MCC. C2 is thought to use histamine and NO as cotransmitters at this synapse, because both agents mimic the membrane responses. Now we provide evidence that treatment with NO donors stimulates soluble guanylyl cyclase (sGC) in the MCC, and as a result cGMP increases. S-Nitrosocysteine (SNC, an NO donor) and 8-bromo-cGMP (8-Br-cGMP) both induced the membrane depolarization and increase in input resistance that are characteristic of the very slow EPSP. Two inhibitors of sGC, 6-anilino-5,8-quinolinequinone (LY83583) and 1H-[1,2,4]oxadiazolo[4, 3-a]quinoxaline-1-one (ODQ), suppressed both the very slow EPSP and the membrane responses to SNC but not the histamine membrane responses. NO-induced cGMP production was determined in the MCC using cGMP immunocytochemistry (cGMP-IR). In the presence of 3-isobutyl-1-methylxanthine (IBMX), 10 microM SNC was sufficient to induce cGMP-IR, and the staining intensity increased as the SNC dose was increased. This cGMP-IR was suppressed by ODQ in a dose-dependent manner and completely blocked by 10 microM ODQ. Histamine did not induce cGMP-IR. The results suggest that NO stimulates sGC-dependent cGMP synthesis in the MCC and that cGMP mediates the membrane responses. The cotransmitter histamine induces essentially the same membrane responses but seems to use a separate and distinct second messenger pathway.  (+info)

Histochemically reactive zinc in plaques of the Swedish mutant beta-amyloid precursor protein transgenic mice. (8/943)

Endogenous metals such as zinc may contribute to beta-amyloid (Abeta) aggregation and hence the plaque formation. In the present study, we examined brains of four Swedish mutant amyloid precursor protein (APP) transgenic mice at 12 months of age for histochemically reactive zinc in the plaques. Here, we report that all the Congo red (+) mature plaques contained chelatable zinc, as demonstrated by staining with the zinc-specific fluorescent dye 6-methoxy-8-quinolyl-para-toluenesulfonamide (TSQ). On the other hand, Congo red (-) preamyloid Abeta deposits were not stained with TSQ. Interestingly, although cerebellum contained similar degree of preamyloid Abeta deposits as cerebral cortex, it was completely devoid of Congo red- or TSQ-stained mature plaques. Although zinc from plaques was only slowly and partially removed by a specific zinc remover, dithizone, treatment of brain sections with heparinase-III, which degrades heparan sulfate proteoglycan (HSPG), another major constituent of plaques, greatly fastened the zinc removal with dithizone. The present study has demonstrated the presence of histochemically reactive zinc in plaques, but not preamyloid Abeta deposits, of the Swedish mutant APP transgenic mice. Because preamyloid Abeta deposits fail to develop into congophilic plaques in cerebellum where synaptic vesicle zinc is deficient, the synaptic zinc may be a necessary element in the plaque formation. In holding zinc inside plaques, HSPG may contribute in addition to Abeta.  (+info)

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Chloroquine (CQ), a 4-aminoquinoline, accumulates in acidic digestive vacuoles of the malaria parasite, preventing conversion of toxic haematin to beta-haematin. We examine how bis 4-aminoquinoline piperaquine (PQ) and its hydroxy-modification (OH-PQ) retain potency on chloroquine-resistant (CQ-R) Plasmodium falciparum. For CQ, PQ, OH-PQ and 4 and 5, representing halves of PQ, beta-haematin inhibitory activity (BHIA) was assayed, while potency was determined in CQ-sensitive (CQ-S) and CQ-R P. falciparum. From measured pK(a)s and the pH-modulated distribution of base between water and lipid (logD), the vacuolar accumulation ratio (VAR) of charged drug from plasma water (pH 7.4) into vacuolar water (pH 4.8) and lipid accumulation ratio (LAR) were calculated. All agents were active in BHIA. In CQ-S, PQ, OH-PQ and CQ were equally potent while 4 and 5 were 100 times less potent. CQ with two basic centres has a VAR of 143,482, while 4 and 5, with two basic centres of lower pK(a)s have VARs of 1287 and ...
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Malaria remains a major disease in the developing world and globally is the most important parasitic disease causing significant morbidity and mortality. Because of widespread resistance to conventional antimalarials, including chloroquine (CQ), new drugs are urgently needed. Here we report on the antimalarial efficacy, both in vitro and in vivo, of a series of aminoquinoline derivatives with adamantane or benzothiophene as a carrier. In vitro efficacy was evaluated by a lactate dehydrogenase (LDH) assay in cultures of a CQ-sensitive (3D7) and CQ-resistant (Dd2) strain of Plasmodium falcipanim. Of a series of 26 screened compounds, 12 that exerted a growth inhibition rate of ,= 5% were further examined in vitro to determine the 50% inhibitory concentration (IC50) values. Nine compounds shown in preliminary experiments to be non-toxic in vivo were evaluated in C57BL/6 mice infected with Plasmodium herghei ANKA strain using a modified Thompson test. All nine compounds examined in vivo pr...olonged ...
https://cer.ihtm.bg.ac.rs/handle/123456789/2172
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Natural products are a prolific source for the identification of new biologically active compounds. In the present work, we studied the in vitro and in vivo antimalarial efficacy and ADME-Tox profile of a molecular hybrid (AM1) between 4-aminoquinoline and a quinolizidine moiety derived from lupinine (Lupinus luteus). The aim was to find a compound endowed with the target product profile-1 (TCP-1: molecules that clear asexual blood-stage parasitaemia), proposed by the Medicine for Malaria Venture to accomplish the goal of malaria elimination/eradication. AM1 displayed a very attractive profile in terms of both in vitro and in vivo activity. By using standard in vitro antimalarial assays, AM1 showed low nanomolar inhibitory activity against chloroquine-sensitive and resistant P. falciparum strains (range IC50 16-53 nM), matched with a high potency against P. vivax field isolates (Mean IC50 29 nM). Low toxicity and additivity with artemisinin derivatives were also demonstrated in vitro. High in vivo oral
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This treatment is highly effective for the precancerous actinic keratoses, especially when used to treat in cases with numerous lesions. It is about 80% effective in the treatment of superficial skin cancers. It is 50-80% effective in the treatment of very superficial skin cancers.. It is more unpredictable than Efudix and reactions may be severe and can lead to ulceration and scarring. It may be associated with a flu like illness (especially when large areas area treated). It is for these reasons, that SPSSCC will typically recommend Efudix instead of Aldara.. ...
http://www.perthskincancer.com.au/aldara/
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http://www.ttimesworld.com
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Im 28 years old and just had a beautiful baby girl 6 months ago. My post delivery pap smear came back as abnormal. After having a colopscopy and biopsy done the results came back as low grade vaginal dysplasia. My OB told me to use a cream called Aldara for 10 weeks (twice a week) so I did! about a month later my dad passed away and I have been under continuous stress and one thing after another seems to be going wrong!! so when I went for my next colopscopy and biopsy just recently it showed that my vaginal dysplasia had gone from mild to moderate and now I have also developed dysplasia on my cervix!! I was religiously using Aldara like my OB had suggested but it seems to have made it worse!!! now he has told me to try another cream called efudex(sorry am not sure if thats how you spell it!) has anyone had any experience with this cream or with Aldara? am really confused, as I thoroughly researched Aldara before I used it and really thought it would help diminish the dysplasia altogether! ...
https://csn.cancer.org/comment/838242
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Zyclara: Imiquimod cream belongs to a group of medications called immune response modifiers. It works by stimulating the bodys defenses to fight certain types of skin conditions. Imiquimod cream is used to treat actinic keratosis (AK) on the face or balding scalp in adults. AK is a skin condition that could turn into skin cancer (symptoms include rough, red, scaly patches or lesions, or crusts) that is caused by chronic sun exposure.
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NFATc1 supports imiquimod-induced skin inflammation by suppressing IL-10 synthesis in B cellsNFATc1 supports imiquimod-induced skin inflammation by suppressing IL-10 synthesis in B cells
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I have had an area of concern (to me) on my nose for over 3 years. Have been to the dermatologist numerous times during this period and she said it was nothing. I finally insisted on a biopsy and it came back as superficial basal cell. They are recommending Mohs surgery but I am nervous about it as it is in a location (right side tip) that could possibly require extensive reconstruction surgery. I had a consult with the surgeon this weekend and he said the lesion appears small and probably wouldnt require reconstruction (forehead flap) but wouldnt know for sure until they did the surgery. I asked about using Aldara and both my dermatologist and Mohs surgeon agreed I could try that and then be reevaluated after that treatment.. Now Im reading all the scary reviews of bad side effects online for Aldara. Cant decide if I should just do the Mohs or try the Aldara.. I had Mohs 13 years ago (also on my nose but on the far side-2 passes). The closure was just 7 stitches and no scars left ...
https://community.macmillan.org.uk/cancer_types/skin-cancer/f/skin-cancer-forum/189863/mohs-or-aldara
Eruptive keratoacanthoma following topical imiquimod for in situ squamous cell carcinoma of the skin in a renal transplant...Eruptive keratoacanthoma following topical imiquimod for in situ squamous cell carcinoma of the skin in a renal transplant...
Pini, A M; Koch, S; Schärer, L; French, L E; Läuchli, S; Hofbauer, G F L (2008). Eruptive keratoacanthoma following topical imiquimod for in situ squamous cell carcinoma of the skin in a renal transplant recipient. Journal of the American Academy of Dermatology, 59(5):S116-S117. ...
http://www.zora.uzh.ch/id/eprint/14019/
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Psoriasis is a chronic inflammatory skin disease with a strong genetic background and is triggered by environmental factors. Available evidence supports CD6, a lymphocyte surface receptor mostly expressed by T cells, as a putative target in autoimmunity. Accordingly, a humanized anti-CD6 antibody has been assayed for the treatment of certain autoimmune disorders, including psoriasis. Here, we present novel evidence in mice and humans for a direct involvement of CD6 in psoriasis pathophysiology. First, an attenuated form of imiquimod-induced psoriasis-like skin inflammation was demonstrated in CD6-deficient mice, as deduced from lower epidermal thickness and local reduced production of pro-inflammatory cytokines, namely, interleukin-17A ...
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Melanoma is the most serious type of skin cancer as a malignant tumor of melanocytes. Metastatic melanoma can be fatal with the 5-year survival rate below 15% and median survival of about 6-8 months.1 Due to the development of metastatic disease which is highly resistant to conventional chemotherapeutics and radiation, the intensive research and effort into new drugs and treatments2 afforded merely the response rates of approximately 20% or less. We report here the synthesis of a novel series of aminoquinoline derivatives 1a-p based on the structural features of Sorafenib (Nexavar)3 (Figure 1) and their antiproliferative activities and selectivities against human melanoma cell line and fibroblast cell line ...
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C5-regioselective C-H fluorination of 8-aminoquinoline amides and sulfonamides with selectfluor under metal-free conditions -...C5-regioselective C-H fluorination of 8-aminoquinoline amides and sulfonamides with selectfluor under metal-free conditions -...
A novel and efficient regioselective C-H fluorination of 8-aminoquinoline amides and sulfonamides at C5 position was achieved. Using selectfluor as
http://pubs.rsc.org/en/content/articlelanding/2018/ob/c7ob03059b
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Topical chemotherapy is applied with a cream such as Efudex (5-fluorouracil), Carac (5-fluorouracil),or Aldara (imiquimod). It is a highly effective treatment for pre-cancerous lesions such as Actinic Keratoses (AK). As an alternative treatment to surgery, topical chemotherapy can treat some superficial Basal Cell carcinomas (BCCa) and superficial Squamous Cell carcinomas (SCCa). This treatment is best reserved for early superficial skin cancers and can be unpredictable. 5-fluorouracil creams such as Efudex and Carac are the real chemotherapeutic drugs, killing abnormal cells directly. Imiquimod (Aldara) works differently by summoning forth immune cells that do the killing. It is called an immune response modifier. Imiquimod has also been applied to other skin cancers such as Bowens carcinoma in-situ and melanoma in-situ. An appointment with your physician will help to determine the answer to this question. Not all forms of skin cancer can be treated with the use of topical chemotherapy. The ...
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Imiquimod is an immune response modifier. Imiquimod topical is used to treat actinic keratosis (a condition caused by too much sun exposure) on the face and scalp. Imiquimod topical (for the skin) is also used to treat a minor form of skin cancer called superficial basal cell carcinoma, when surgery would not be an...
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Imiquimod, Fluorouracil, or Observation in Treating HIV-Positive Patients With High-Grade Anal Squamous Skin Lesions - Full...Imiquimod, Fluorouracil, or Observation in Treating HIV-Positive Patients With High-Grade Anal Squamous Skin Lesions - Full...
PRIMARY OBJECTIVES:. I. To assess the efficacy of intra-anal imiquimod 2.5% for treatment of anal high-grade squamous intraepithelial lesions (HSIL) compared to observation only.. II. To assess the efficacy of intra-anal topical 5-fluorouracil (fluorouracil) 5% for treatment of anal HSIL compared to observation only.. SECONDARY OBJECTIVES:. I. To assess the safety and tolerability of intra-anal imiquimod 2.5% and topical 5-fluorouracil 5%.. II. To compare the efficacy of intra-anal imiquimod 2.5% and topical 5-fluorouracil 5%.. III. To assess for partial response of intra-anal imiquimod 2.5% or topical 5-fluorouracil 5% as compared to observation only.. IV. To evaluate the effect of intra-anal imiquimod 2.5% and topical 5-fluorouracil 5% on human papilloma virus (HPV) persistence.. V. To evaluate anal HSIL outcomes at week 44. VI. To evaluate the effect of behavioral patterns including tobacco smoking and sexual activity on treatment efficacy, tolerability and HPV.. OUTLINE: Patients are ...
https://clinicaltrials.gov/ct2/show/NCT02059499?term=%22+January+13%2C++2014%22%3A%22+February+12%2C++2014%22%5BFIRST-RECEIVED-DATE%5DAND+HIV%5BCONDITION%5D&rank=11
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https://en.wikipedia.org/wiki/Harry_L._Fisher
PrimaquinePrimaquine
... is an analog of pamaquine which was the first drug of the 8-aminoquinoline class; tafenoquine is another such drug. ...
https://en.wikipedia.org/wiki/Primaquine
JTC-801 - Википедија, слободна енциклопедијаJTC-801 - Википедија, слободна енциклопедија
Shinkai, H; Ito, T; Iida, T; Kitao, Y; Yamada, H; Uchida, I (2000). „4-Aminoquinolines: novel nociceptin antagonists with ...
https://sr.wikipedia.org/wiki/JTC-801
Mass drug administrationMass drug administration
Two doses of the 8-aminoquinoline plasmoquine were given weekly to workers and their families in two camps. The prevalences of ... For example, the widespread use of 8-aminoquinolines in areas where Glucose-6-phosphate dehydrogenase deficiency is common ...
https://en.wikipedia.org/wiki/Mass_drug_administration
പ്രോസ്റ്റാഗ്ലാൻഡിൻ EP3 റിസപ്റ്റർ - വിക്കിപീഡിയപ്രോസ്റ്റാഗ്ലാൻഡിൻ EP3 റിസപ്റ്റർ - വിക്കിപീഡിയ
Tenoxicam; 4-Aminoquinolines: Antrafenine. *Floctafenine. *Glafenine; Quinazolines: Fluproquazone. *Proquazone; Aminonicotinic ...
https://ml.wikipedia.org/wiki/പ്രോസ്റ്റാഗ്ലാൻഡിൻ_EP3_റിസപ്റ്റർ
Stateville Penitentiary Malaria StudyStateville Penitentiary Malaria Study
Most were 8-aminoquinoline compounds, analogs of pamaquine, an existing alternative to quinine that was unfavorable due to its ... primarily from the 8-aminoquinoline group of compounds. The study marked the first human test of the antimalarial drug ...
https://en.wikipedia.org/wiki/Stateville_Penitentiary_Malaria_Study
History of malariaHistory of malaria
Resochin (7-chloro-4- 4- (diethylamino) - 1 - methylbutyl amino quinoline) and a similar compound Sontochin (3-methyl Resochin ...
https://en.wikipedia.org/wiki/History_of_malaria
Amoebic liver abscessAmoebic liver abscess
Later when synthetic derivatives of quinine were introduced, chloroquine phosphate, a 4-aminoquinoline was found to be less ...
https://en.wikipedia.org/wiki/Amoebic_liver_abscess
Mizoroki-Heck vs. Reductive HeckMizoroki-Heck vs. Reductive Heck
The authors rely on an 8-aminoquinoline directing group to control the regioselectivity of migratory insertion and stabilize ...
https://en.wikipedia.org/wiki/Mizoroki-Heck_vs._Reductive_Heck
Malaria prophylaxisMalaria prophylaxis
... the first synthetic antimalarial compound-Atabrin and this was followed by Resochin and Sontochin derived from 4-aminoquinoline ...
https://en.wikipedia.org/wiki/Malaria_prophylaxis
List of MeSH codes (D03)List of MeSH codes (D03)
... aminoquinolines MeSH D03.438.810.050.060 - amodiaquine MeSH D03.438.810.050.180 - chloroquine MeSH D03.438.810.050.180.350 - ...
https://en.wikipedia.org/wiki/List_of_MeSH_codes_(D03)
8-Aminoquinoline - Wikipedia8-Aminoquinoline - Wikipedia
8-Aminoquinoline is a form of aminoquinoline with an amine at the 8-position of quinoline. ... The 8-aminoquinoline family of drugs contains three members, primaquine, tafenoquine and pamaquine[1] and are used in the ... The 8-aminoquinoline drugs must not be given to patients with G6PD deficiency, because they cause potentially fatal haemolysis ... "Short report: The activity of pamaquine, an 8-aminoquinoline drug, against sporozoite-induced infections of Plasmodium vivax ( ...
https://en.wikipedia.org/wiki/8-Aminoquinoline
Aminoquinoline - WikipediaAminoquinoline - Wikipedia
Depending upon the location of the amino group, they can be divided into: 4-Aminoquinoline 8-Aminoquinoline This set index page ... Aminoquinolines are derivatives of quinoline, most notable for their roles as antimalarial drugs. ...
https://en.wikipedia.org/wiki/Aminoquinoline
4-Aminoquinoline - Wikipedia4-Aminoquinoline - Wikipedia
4-Aminoquinoline is a form of aminoquinoline with the amino group at the 4-position of the quinoline. The compound has been ... "4-Aminoquinoline 578-68-7 , TCI America". www.tcichemicals.com. Retrieved 2020-03-06. v t e. ... Bourne SA, De Villiers K, Egan TJ (2006). "Three 4-aminoquinolines of antimalarial interest". Acta Crystallogr C. 62 (Pt 2): ... Bray PG, Hawley SR, Ward SA (1996). "4-Aminoquinoline resistance of Plasmodium falciparum: insights from the study of ...
https://en.wikipedia.org/wiki/4-Aminoquinoline
3-Aminoquinoline 98% | Sigma-Aldrich3-Aminoquinoline 98% | Sigma-Aldrich
3-Aminoquinoline 0.98; CAS No.: 580-17-6; Synonyms: 3-AQ; 3-Quinolinamine; Linear Formula: C9H8N2; Empirical Formula: C9H8N2; ... 3-Aminoquinoline was used:. • in liquid matrix for matrix-assisted laser desorption/ionization mass spectrometry (MALDI-MS) for ...
https://www.sigmaaldrich.com/catalog/product/aldrich/232289?lang=en®ion=US
5-Aminoquinoline 99.0 %, TCI America | Fisher Scientific5-Aminoquinoline 99.0 %, TCI America | Fisher Scientific
5-Aminoquinoline 99.0 %, TCI America 5G Chemicals:Organic Compounds:Organoheterocyclic compounds:Quinolines and derivatives: ... 5-aminoquinoline,5-quinolinamine,quinoline, 5-amino,5-quinolylamine,quinolin-5-ylamine,unii-yyj34z13sh,5-amino-quinoline,ccris ... 5-aminoquinoline,5-quinolinamine,quinoline, 5-amino,5-quinolylamine,quinolin-5-ylamine,unii-yyj34z13sh,5-amino-quinoline,ccris ...
https://www.fishersci.com/shop/products/5-aminoquinoline-tci-america-3/A095925G
WO2018196823 2-AMINO-QUINOLINE DERIVATIVESWO2018196823 2-AMINO-QUINOLINE DERIVATIVES
EN) 2-AMINO-QUINOLINE DERIVATIVES. (FR) DÉRIVÉS DE 2-AMINO-QUINOLÉINE. Abstract: (EN) Described herein are 2-amino-quinoline ... in need thereof by administering a therapeutically effective amount of a 2-amino-quinoline derivative.. (FR) Linvention ...
https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2018196823
The American Journal of Tropical Medicine and Hygiene | A Role for 8-Aminoquinolines in Falciparum Malaria?The American Journal of Tropical Medicine and Hygiene | A Role for 8-Aminoquinolines in Falciparum Malaria?
Much attention was paid to the apparent absence of 4-aminoquinoline resistance in much of Central America (less Panama) and in ... There was considerable discussion of Plasmodium falciparum resistance to the 4-aminoquinolines and to mefloquine. The ... A Role for 8-Aminoquinolines in Falciparum Malaria? * Author(s): * Publisher: The American Society of Tropical Medicine and ... Much attention was paid to the apparent absence of 4-aminoquinoline resistance in much of Central America (less Panama) and in ...
http://www.ajtmh.org/content/journals/10.4269/ajtmh.1985.34.651
Hybrid antimalarials; the reaction of 8-amino-quinolines with nitrodiolsHybrid antimalarials; the reaction of 8-amino-quinolines with nitrodiols
... dc.contributor.advisor. VanderWerf, Calvin A.. ...
https://kuscholarworks.ku.edu/handle/1808/24716?show=full
5-Position-selective C-H trifluoromethylation of 8-aminoquinoline derivatives - Organic & Biomolecular Chemistry (RSC...5-Position-selective C-H trifluoromethylation of 8-aminoquinoline derivatives - Organic & Biomolecular Chemistry (RSC...
We developed a copper-catalyzed 5-position-selective C-H trifluoromethylation of 8-aminoquinoline derivatives. The reaction ... 5-Position-selective C-H trifluoromethylation of 8-aminoquinoline derivatives Y. Kuninobu, M. Nishi and M. Kanai, Org. Biomol. ... On the other hand, the trifluoromethylation of 8-aminoquinolines was also promoted by other Lewis acids as well as a copper ... These results indicated that the trifluoromethylation of 8-aminoquinolines proceeded via a Friedel-Crafts-type reaction. ...
https://pubs.rsc.org/en/Content/ArticleLanding/2016/OB/C6OB01325B
2,6-dimethyl-N-[(2-oxo-1-propyl-indol-3-ylidene)amino]quinoline-4-carboxamide2,6-dimethyl-N-[(2-oxo-1-propyl-indol-3-ylidene)amino]quinoline-4-carboxamide
... amino]quinoline-4-carboxamide
https://scitoys.com/scichem/jqp059/6764728.html
NY D87815 - The tariff classification of 8-Aminoquinoline (CAS 578-66-5) from China and Tricyclic Olefin from Italy. - United...NY D87815 - The tariff classification of 8-Aminoquinoline (CAS 578-66-5) from China and Tricyclic Olefin from Italy. - United...
RE: The tariff classification of 8-Aminoquinoline (CAS 578-66-5) from China and Tricyclic Olefin from Italy.. Dear Mr. von ... In your letter dated February 4, 1999, you requested a tariff classification ruling for 8-Aminoquinoline which you have stated ... The applicable subheading for 8-Aminoquinoline will be 2933.40.7000, Harmonized Tariff Schedule of the United States (HTS), ...
http://www.faqs.org/rulings/rulings1999NYD87815.html
Method for Inducing Protection in Animal Against Cyanide Poisoning Using 8-Aminoquinolines.Method for Inducing Protection in Animal Against Cyanide Poisoning Using 8-Aminoquinolines.
It is based upon the use or administration of therapeutically effective amount of certain 8-aminoquinoline compositions which ... It is based upon the use or administration of therapeutically effective amount of certain 8-aminoquinoline compositions which ... Title : Method for Inducing Protection in Animal Against Cyanide Poisoning Using 8-Aminoquinolines. ...
http://oai.dtic.mil/oai/oai?verb=getRecord&metadataPrefix=html&identifier=ADD013956
2-(4-bromophenyl)-6-methyl-N-[(2-oxo-1-propyl-indol-3-ylidene)amino]quinoline-4-carboxamide2-(4-bromophenyl)-6-methyl-N-[(2-oxo-1-propyl-indol-3-ylidene)amino]quinoline-4-carboxamide
... amino]quinoline-4-carboxamide
https://scitoys.com/scichem/jqp049/6829437.html
Exploring QSAR for Antimalarial Activities and Drug Distribution within Blood of a Series of 4-Aminoquinoline Drugs Using...Exploring QSAR for Antimalarial Activities and Drug Distribution within Blood of a Series of 4-Aminoquinoline Drugs Using...
S. Ray, B. Madrid, P. Catz et al., "Development of a new generation of 4-aminoquinoline antimalarial compounds using predictive ... Exploring QSAR for Antimalarial Activities and Drug Distribution within Blood of a Series of 4-Aminoquinoline Drugs Using ... "Synthesis of ring-substituted 4-aminoquinolines and evaluation of their antimalarial activities," Bioorganic and Medicinal ... "Incorporation of an intramolecular hydrogen-bonding motif in the side chain of 4-aminoquinolines enhances activity against drug ...
https://www.hindawi.com/journals/jchem/2013/560415/ref/
Plasmodium Falciparum Malaria in Panama Resistant to 4-Aminoquinoline Drugs* | The American Journal of Tropical Medicine and...Plasmodium Falciparum Malaria in Panama Resistant to 4-Aminoquinoline Drugs* | The American Journal of Tropical Medicine and...
This is the first report of 4-aminoquinoline drug resistance in P. falciparum malaria in a country north of Colombia in the ... 4-aminoquinoline drugs. The cure rate was only 22%. Failures were represented by relapses, persistence of the parasitemia, or ... Plasmodium Falciparum Malaria in Panama Resistant to 4-Aminoquinoline Drugs * * Martin D. Young, Carl M. Johnson ... This is the first report of 4-aminoquinoline drug resistance in P. falciparum malaria in a country north of Colombia in the ...
http://www.ajtmh.org/content/journals/10.4269/ajtmh.1972.21.13
Primaquine or other 8-aminoquinoline for reducing P. falciparum transmission - GOV.UKPrimaquine or other 8-aminoquinoline for reducing P. falciparum transmission - GOV.UK
Graves, P.M.; Gelband, H.; Garner, P. Primaquine or other 8-aminoquinoline for reducing P. falciparum transmission. Cochrane ...
https://www.gov.uk/dfid-research-outputs/primaquine-or-other-8-aminoquinoline-for-reducing-p-falciparum-transmission
6-Chloro-8-aminoquinoline | CAS 5470-75-7 | SCBT - Santa Cruz Biotechnology6-Chloro-8-aminoquinoline | CAS 5470-75-7 | SCBT - Santa Cruz Biotechnology
Buy 6-Chloro-8-aminoquinoline (CAS 5470-75-7), a derivative used in the preparation fungitoxic analogs, from Santa Cruz. MF: ... 6-Chloro-8-aminoquinoline A derivative used in the preparation fungitoxic analogs *Home. ... 6-Chloro-8-aminoquinoline (CAS 5470-75-7) *bvseo_sdk, java_sdk, bvseo-3.2.0 ... 6-Chloro-8-aminoquinoline is a di-substituted quinoline derivative used in the preparation fungitoxic analogs. ...
https://www.scbt.com/scbt/product/6-chloro-8-aminoquinoline-5470-75-7/
C5-regioselective C-H fluorination of 8-aminoquinoline amides and sulfonamides with selectfluor under metal-free conditions -...C5-regioselective C-H fluorination of 8-aminoquinoline amides and sulfonamides with selectfluor under metal-free conditions -...
A novel and efficient regioselective C-H fluorination of 8-aminoquinoline amides and sulfonamides at C5 position was achieved. ... C5-regioselective C-H fluorination of 8-aminoquinoline amides and sulfonamides with selectfluor under metal-free conditions ... C5-regioselective C-H fluorination of 8-aminoquinoline amides and sulfonamides with selectfluor under metal-free conditions Y. ... A novel and efficient regioselective C-H fluorination of 8-aminoquinoline amides and sulfonamides at C5 position was achieved. ...
http://pubs.rsc.org/en/content/articlelanding/2018/ob/c7ob03059b
Research: In vitro sensitivity of Plasmodium falciparum clinical isolates to 4-aminoquinolines in Northeast Nigeria |...Research: In vitro sensitivity of Plasmodium falciparum clinical isolates to 4-aminoquinolines in Northeast Nigeria |...
Research: In vitro sensitivity of Plasmodium falciparum clinical isolates to 4-aminoquinolines in Northeast Nigeria. July 29, ... Home » Research: In vitro sensitivity of Plasmodium falciparum clinical isolates to 4-aminoquinolines in Northeast Nigeria ... Widespread drug-resistant Plasmodium falciparum strains have challenged the pivotal role played by 4- aminoquinolines, ...
https://malariaworld.org/mwj/2016/research-vitro-sensitivity-plasmodium-falciparum-clinical-isolates-4-aminoquinolines
In Vivo and In Vitro Efficacy of Amodiaquine against Plasmodium falciparum in an Area of Continued Use of 4-Aminoquinolines...In Vivo and In Vitro Efficacy of Amodiaquine against Plasmodium falciparum in an Area of Continued Use of 4-Aminoquinolines...
In Vivo and In Vitro Efficacy of Amodiaquine againstPlasmodium falciparumin an Area of Continued Use of 4-Aminoquinolines in ... or second-line treatment in areas with similar patterns of 4-aminoquinoline resistance should be reassessed. ...
https://insights.ovid.com/joid/200906010/01451459-200906010-00004
NF-κB Phosphorylation Inhibition Prevents Articular Cartilage Degradation in Osteoarthritis Rats via 2-Aminoquinoline - Get...NF-κB Phosphorylation Inhibition Prevents Articular Cartilage Degradation in Osteoarthritis Rats via 2-Aminoquinoline - Get...
NF-κB Phosphorylation Inhibition Prevents Articular Cartilage Degradation in Osteoarthritis Rats via 2-Aminoquinoline - Get ... Treatment with 2-aminoquinoline led to a significant reduction in inflammatory cytokine expression in osteoarthritis rats in a ... The 2-aminoquinoline treatment supressed PGE2, MMP-13, and substance P levels in osteoarthritis rats. Moreover, the expression ... The rats in treatment groups received 5, 10, 15, or 20 mg/kg doses of 2-aminoquinoline on day 2 of monosodium iodoacetate ...
https://www.medscimonit.com/download/index/idArt/920346
Spectrophotometric Determination of Palladium(Ⅱ) with 5-(3-Carboxylphenylazo)-8-Aminoquinoline--《PRECIOUS METALS》1998年03期Spectrophotometric Determination of Palladium(Ⅱ) with 5-(3-Carboxylphenylazo)-8-Aminoquinoline--《PRECIOUS METALS》1998年03期
8-aminoquinoline (m-CPAQ) was synthesized. Palladium(Ⅱ) reacts with m-CPAQ to form a violet-blue ternary complex in the ... A new reagent 5-(3-carboxylphenylazo)-8-aminoquinoline (m-CPAQ) was synthesized. Palladium(Ⅱ) reacts with m-CPAQ to form a ... Spectrophotometric Determination of Palladium(Ⅱ) with 5-(3-Carboxylphenylazo)-8-Aminoquinoline. Huang Zhangjie, Shen Tao, Xu ... 8-aminoquinoline-5-azo)-8-hydroxy-3, 6-naphthalenedisulfonic acid with copper[J];Metallurgical Analysis;2002-02. ...
http://en.cnki.com.cn/Article_en/CJFDTOTAL-GJSZ803.010.htm
6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure...6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure...
6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure- ... 6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure- ... 6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure- ... Novel 6-acylamino-2-aminoquinoline melanin-concentrating hormone 1 receptor (MCH1R) antagonists were identified by sequential ...
https://eprints.soton.ac.uk/62175/
Multivariate Modeling of Cytochrome P450 Enzymes for 4- Aminoquinoline Antimalarial Analogues using Genetic- Algorithms...Multivariate Modeling of Cytochrome P450 Enzymes for 4- Aminoquinoline Antimalarial Analogues using Genetic- Algorithms...
Multivariate Modeling of Cytochrome P450 Enzymes for 4- Aminoquinoline Antimalarial Analogues using Genetic- Algorithms ... by chloroquine and a new series of 4-aminoquinoline derivatives in order to obtain a set of predictive in-silico models using ...
https://www.ajol.info/index.php/tjpr/article/view/99883
A pyrazine amide - 4-aminoquinoline hybrid and its rhodium and iridium pentamethylcyclopentadienyl complexes; evaluation of...A pyrazine amide - 4-aminoquinoline hybrid and its rhodium and iridium pentamethylcyclopentadienyl complexes; evaluation of...
The synthesis and characterization of N-(2-((7-chloroquino-lin-4-yl)amino)ethyl)pyrazine-2-carboxamide (L), an aminoquinoline ... The synthesis and characterization of N-(2-((7-chloroquino-lin-4-yl)amino)ethyl)pyrazine-2-carboxamide (L), an aminoquinoline ... A pyrazine amide - 4-aminoquinoline hybrid and its rhodium and iridium pentamethylcyclopentadienyl complexes; evaluation of ... an aminoquinoline - pyrazinamide hybrid, and the complexes (N-(2-((7-chloroquino-lin-4-yl)amino)ethyl)pyrazine-2-carboxamide)( ...
https://lup.lub.lu.se/search/publication/35421630-063b-4912-8fec-acc169c403fb
AMINOQUINOLINE | Semantic ScholarAMINOQUINOLINE | Semantic Scholar
Aminoquinoline based highly sensitive fluorescent sensor for lead(II) and aluminum(III) and its application in live cell ... A method for aminoquinoline-directed, cobalt-promoted dimerization of benzamides has been developed. Reactions proceed in ... An operationally simple and general method for copper-catalyzed, aminoquinoline-assisted amination of β-C(sp(2))-H bonds of… ... A method for cobalt-catalyzed, aminoquinoline-directed ortho-functionalization of sp2 C-H bonds with alkenes has been developed ...
https://www.semanticscholar.org/topic/AMINOQUINOLINE/1204982
8-Aminoquinoline | definition of 8-Aminoquinoline by Medical dictionary8-Aminoquinoline | definition of 8-Aminoquinoline by Medical dictionary
What is 8-Aminoquinoline? Meaning of 8-Aminoquinoline medical term. What does 8-Aminoquinoline mean? ... Looking for online definition of 8-Aminoquinoline in the Medical Dictionary? 8-Aminoquinoline explanation free. ... aminoquinoline. (redirected from 8-Aminoquinoline). Also found in: Wikipedia. aminoquinoline. [ah-me″no-kwin´o-lēn] a ... the 4-aminoquinoline and 8-aminoquinoline derivatives are groups of antimalarial agents. ...
https://medical-dictionary.thefreedictionary.com/8-Aminoquinoline
A pyrazine amide - 4-aminoquinoline hybrid and its rhodium and iridium pentamethylcyclopentadienyl complexes; evaluation of...A pyrazine amide - 4-aminoquinoline hybrid and its rhodium and iridium pentamethylcyclopentadienyl complexes; evaluation of...
The aminoquinoline - pyrazinamide hybrid N-(2-((7-chloroquinolin-4-yl)amino)ethyl)pyrazine-2-carboxamide and its complexes with ... The most successfully deployed aminoquinoline anti-malarial drug is chloroquine, see Fig. 1. It was used massively on a global ... The synthesis and characterization of N-(2-((7-chloroquinolin-4-yl)amino)ethyl)pyrazine-2-carboxamide (L), an aminoquinoline - ... In this study, we have set out to investigate the possibilities of aminoquinoline hybrids with pharmacophores from tuberculosis ...
http://www.scielo.org.mx/scielo.php?script=sci_arttext&pid=S1870-249X2017000200158&lng=es&nrm=iso&tlng=en
3-Aminoquinoline - Alfa Chemistry3-Aminoquinoline - Alfa Chemistry
3-Aminoquinoline/ACM580176 can be provided in Alfa Chemistry. We are dedicated to provide our customers the best products and ...
https://www.alfa-chemistry.com/3-aminoquinoline-cas-580-17-6-item-321777.htm
Aralen Phosphate - Side Effects, Uses, Dosage, Overdose, Pregnancy, Alcohol | The Medicine ShoppeAralen Phosphate - Side Effects, Uses, Dosage, Overdose, Pregnancy, Alcohol | The Medicine Shoppe
Aralen Phosphate - Get up-to-date information on Aralen Phosphate side effects, uses, dosage, overdose, pregnancy, alcohol and more. Learn more about Aralen Phosphate
https://www.medicineshoppe.com/aralen-phosphate
DerivativesAntimalarialPlasmodiumQuinolineCompoundsPrimaquineChloroquineMalariaAmodiaquineSynthesisInhibitorsComplexesResistancePotentAmideVitroMetabolismConcomitantCytosolChemistrySelectivityResistantG6PDClinicalClassReactionEffectivePresentGroupsHighly
Derivatives9
  • Aminoquinolines are derivatives of quinoline, most notable for their roles as antimalarial drugs. (wikipedia.org)
  • A variety of derivatives of 4-aminoquinoline are antimalarial agents useful in treating erythrocytic plasmodial infections. (wikipedia.org)
  • We developed a copper-catalyzed 5-position-selective C-H trifluoromethylation of 8-aminoquinoline derivatives. (rsc.org)
  • To develop QSAR modeling of the inhibition of cytochrome P450s (CYPs) by chloroquine and a new series of 4-aminoquinoline derivatives in order to obtain a set of predictive in-silico models using genetic algorithms-multiple linear regression (GA-MLR) methods. (ajol.info)
  • Core-shell mesoporous silica nanospheres encapsulated with Rhodamine 101 into the solid core and 8-aminoquinoline derivatives (AQ) into the mesoporous shell were used as [Zn.sup.2+] ratiometric fluorescent sensor [40]. (thefreedictionary.com)
  • The synthesis of a novel series of aminoquinoline derivatives 1a-p and their antiproliferative activities against A375 human melanoma cell line were described. (elsevier.com)
  • We report here the synthesis of a novel series of aminoquinoline derivatives 1a-p based on the structural features of Sorafenib (Nexavar)3 (Figure 1) and their antiproliferative activities and selectivities against human melanoma cell line and fibroblast cell line. (kist.re.kr)
  • This review will be focused on the synthesis, in vitro and in vivo studies of hybrid compounds containing 4- and 8-aminoquinoline derivatives. (mdpi.com)
  • We synthesized both truncated and polar 2-aminoquinoline derivatives and assayed them against recombinant NOS enzymes. (rcsb.org)
Antimalarial4
  • Development of a new generation of 4-aminoquinoline antimalarial compounds using predictive pharmacokinetic and toxicology models," Journal of Medicinal Chemistry , vol. 53, pp. 3685-3695, 2010. (hindawi.com)
  • Antimalarial drugs containing 4-aminoquinoline scaffolds are good precursors for hybridization with other antimalarials and metal-based compounds via selected functionalities [ 8 ]. (mdpi.com)
  • In Vivo and In Vitro Activities and ADME-Tox Profile of a Quinolizidine-Modified 4-Aminoquinoline: A Potent Anti-P. falciparum and Anti-P. vivax Blood-Stage Antimalarial. (ox.ac.uk)
  • In the present work, we studied the in vitro and in vivo antimalarial efficacy and ADME-Tox profile of a molecular hybrid (AM1) between 4-aminoquinoline and a quinolizidine moiety derived from lupinine (Lupinus luteus). (ox.ac.uk)
Plasmodium7
  • There was considerable discussion of Plasmodium falciparum resistance to the 4-aminoquinolines and to mefloquine. (ajtmh.org)
  • Fifty Panamanian patients with 69 attacks of Plasmodium falciparum malaria were treated with chloroquine and amodiaquine, 4-aminoquinoline drugs. (ajtmh.org)
  • Widespread drug-resistant Plasmodium falciparum strains have challenged the pivotal role played by 4- aminoquinolines, including chloroquine (CQ), which has been delisted for the treatment of malaria in most parts of the world. (malariaworld.org)
  • A new 8-aminoquinoline tafenoquine is on clinical trial as a potential replacement for primaquine to treat Plasmodium vivax malaria (Shanks 2001) and holds promise as a prophylactic against Plasmodium falciparum (Shanks 2001). (thefreedictionary.com)
  • Activity of piperaquine and other 4-aminoquinoline antiplasmodial drugs against chloroquine-sensitive and resistant blood-stages of Plasmodium falciparum Role of beta-haematin inhibition and drug concentration in vacuolar water- and lipid-phases. (lshtm.ac.uk)
  • We examine how bis 4-aminoquinoline piperaquine (PQ) and its hydroxy-modification (OH-PQ) retain potency on chloroquine-resistant (CQ-R) Plasmodium falciparum. (lshtm.ac.uk)
  • Discordant temporal evolution of Pfcrt and Pfmdr1 genotypes and Plasmodium falciparum in vitro drug susceptibility to 4-aminoquinolines after drug policy change in French Guiana. (archives-ouvertes.fr)
Quinoline5
  • 8-Aminoquinoline is a form of aminoquinoline with an amine at the 8-position of quinoline . (wikipedia.org)
  • 4-Aminoquinoline is a form of aminoquinoline with the amino group at the 4-position of the quinoline. (wikipedia.org)
  • The applicable subheading for 8-Aminoquinoline will be 2933.40.7000 , Harmonized Tariff Schedule of the United States (HTS), which provides for heterocyclic compounds with nitrogen hetero-atom(s) only: compounds containing a quinoline or isoquinoline ring-system (whether or not hydrogenated), not further fused: other. (faqs.org)
  • 6-Chloro-8-aminoquinoline is a di-substituted quinoline derivative used in the preparation fungitoxic analogs. (scbt.com)
  • 5-amino-2-hydroxy quinoline, 5-acetyl-aminoquinoline and 5-acetylamino-2-hydroxy quinoline due to the combined action of aldehyde oxidase and N-acetyl transferase . (bvsalud.org)
Compounds5
  • Depending upon the location of the amino group, they can be divided into: 4-Aminoquinoline 8-Aminoquinoline This set index page lists chemical compounds articles associated with the same name. (wikipedia.org)
  • A patent application for 4-aminoquinoline compounds was filed in 2002 and published in 2005. (wikipedia.org)
  • 4-Aminoquinoline Compounds" (PDF). (wikipedia.org)
  • Primaquine, like all 8-aminoquinoline compounds, can result in severe haemolysis in individuals with G6PD deficiency, and screening for this enzyme defect is recommended before these medications are commenced. (thefreedictionary.com)
  • This compound belongs to the class of organic compounds known as 4-aminoquinolines. (drugbank.ca)
Primaquine8
  • The 8-aminoquinoline family of drugs contains three members, primaquine , tafenoquine and pamaquine [1] and are used in the treatment of malaria . (wikipedia.org)
  • The company said Tafenoquine is an 8-aminoquinoline chemically derived from Primaquine, with activity against all types of malaria. (thefreedictionary.com)
  • Primaquine, an 8-aminoquinoline , is a prodrug requiring hydroxylation by the CYP2D6 enzyme within hepatocytes to transform into the active form [5]. (thefreedictionary.com)
  • Despite numerous studies carried out to evaluate antirelapse potential of existing and new antimalarials such as Tafenoquine, and its combinations [6-8], Primaquine (PQ), an 8-aminoquinoline , remains at present the only agent available worldwide to prevent relapses [9]. (thefreedictionary.com)
  • CYP450 phenotyping and accurate mass identification of metabolites of the 8-aminoquinoline , anti-malarial drug primaquine. (thefreedictionary.com)
  • The objective of this systematic review was to assess the risk of adverse effects in people with G6PD deficiency given primaquine or other 8-aminoquinoline (8AQ) as a single dose or short course (less than 7 days). (lstmed.ac.uk)
  • Tafenoquine, a long-acting 8-aminoquinoline drug related to primaquine, was approved by the Food and Drug Administration (FDA) on July 20, 2018, for antirelapse therapy (Krintafel) and August 8, 2018, for chemoprophylaxis (Arakoda) ( 3 , 4 ). (cdc.gov)
  • Tafenoquine, an 8-aminoquinoline drug related to primaquine, is only the second drug of its class to receive FDA approval. (cdc.gov)
Chloroquine1
  • Chloroquine (CQ), a 4-aminoquinoline, accumulates in acidic digestive vacuoles of the malaria parasite, preventing conversion of toxic haematin to beta-haematin. (lshtm.ac.uk)
Malaria4
  • A Role for 8-Aminoquinolines in Falciparum Malaria? (ajtmh.org)
  • World Health Organization, "World malaria report," 2009, http://www.who.int/malaria/publications/atoz/9789241563901/en/index.html . (hindawi.com)
  • This is the first report of 4-aminoquinoline drug resistance in P. falciparum malaria in a country north of Colombia in the Western Hemisphere. (ajtmh.org)
  • http://www.who.int/malaria/publications/atoz/9789241549127/en/ (Accessed on September 10, 2015). (uptodate.com)
Amodiaquine1
  • These findings also suggest that the value of amodiaquine combinations as first- or second-line treatment in areas with similar patterns of 4-aminoquinoline resistance should be reassessed. (ovid.com)
Synthesis4
  • Recent developments in the design and synthesis of hybrid molecules based on aminoquinoline ring and their antiplasmodial evaluation. (semanticscholar.org)
  • Neves, "Synthesis, structure and physicochemical properties of zinc and copper complexes based on sulfonamides containing 8-aminoquinoline ligands," Quimica Nova, vol. (thefreedictionary.com)
  • Synthesis and hypotensive properties of new 4-aminoquinolines. (nih.gov)
  • Synthesis of aminoquinolines 14. (researchandmarkets.com)
Inhibitors3
  • Bosak A, Opsenica D, Šinko G, Zlatar M, Kovarik Z. Structural aspects of 4-aminoquinolines as reversible inhibitors of human acetylcholinesterase and butyrylcholinesterase. (ac.rs)
  • 400 mu M). Through detailed structure-activity study, we have identified 7-Cl and 7-CF3 substituted N-dodecylamino-4-aminoquinolines (5 and 10) as biofilm formation inhibitors with 50% biofilm inhibition at 69 mu M and 63 mu M in S. marcescens and P. aeruginosa, respectively. (ac.rs)
  • 2-Aminoquinolines showed promise as bioavailable nNOS inhibitors but suffered from low human nNOS inhibition, low selectivity versus human eNOS, and significant binding to other CNS targets. (rcsb.org)
Complexes1
  • Five-coordinate bis(8-aminoquinoline) nitrosylcobalt complexes. (nii.ac.jp)
Resistance1
  • Much attention was paid to the apparent absence of 4-aminoquinoline resistance in much of Central America (less Panama) and in Hispaniola. (ajtmh.org)
Potent1
  • 6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. (soton.ac.uk)
Amide1
  • I started noticing a particular trend in the ASAPs of some of the organic journals I follow, all involving various uses of the aminoquinoline amide as a directing group. (wordpress.com)
Vitro1
  • In vitro oxidation and acetylation of 5-aminoquinoline by rabbit liver enzyme preparation has been investigated. (bvsalud.org)
Metabolism1
  • Metabolism of 5-aminoquinoline with liver cytosol enzyme. (bvsalud.org)
Concomitant1
  • For radical cure of P. vivax and P. ovale infections, concomitant therapy with an 8-aminoquinoline compound is necessary (see CLINICAL PHARMACOLOGY - Microbiology ). (rxlist.com)
Cytosol1
  • Incubation of 5-aminoquinoline with cytosol fraction of the enzyme preparation in the presence of acetyl coenzyme -A gave rise to three different products, viz. (bvsalud.org)
Chemistry1
  • P. B. Madrid, A. P. Liou, J. L. DeRisi, and R. K. Guy, "Incorporation of an intramolecular hydrogen-bonding motif in the side chain of 4-aminoquinolines enhances activity against drug-resistant P. falciparum ," Journal of Medicinal Chemistry , vol. 49, no. 15, pp. 4535-4543, 2006. (hindawi.com)
Selectivity1
  • Both introduction of a hydrophobic substituent next to the cyano group and aminoquinoline methylation considerably improved isoform selectivity. (rcsb.org)
Resistant1
  • Our data show that 7-Cl and 7-CF3 substituted N-dodecylamino-4-aminoquinolines present the promising scaffolds for developing antivirulence and anti-biofilm formation agents against multidrug-resistant bacterial species. (ac.rs)
G6PD2
  • The 8-aminoquinoline drugs must not be given to patients with G6PD deficiency , because they cause potentially fatal haemolysis in these patients. (wikipedia.org)
  • Safety of 8-aminoquinolines given to people with G6PD deficiency: protocol for systematic review of prospective studies. (lstmed.ac.uk)
Clinical1
  • The endoperoxide OZ439, currently in Phase II clinical trials, and a new 8-aminoquinoline , NPC-1161B, also demonstrated transmission-blocking potential. (thefreedictionary.com)
Class1
  • 8-Aminoquinolines are an important class of antiparasitic agents, with broad utility and excellent efficacy, but also limitations due to hematological toxicities, primarily methemoglobinemia and hemolysis. (elsevier.com)
Reaction2
  • These results indicated that the trifluoromethylation of 8-aminoquinolines proceeded via a Friedel-Crafts-type reaction. (rsc.org)
  • Reaction of 1-substituted 3-aminoquinoline-2,4-diones with isothiocyanates. (utb.cz)
Effective2
  • It is based upon the use or administration of therapeutically effective amount of certain 8-aminoquinoline compositions which are administered orally. (dtic.mil)
  • The present study demonstrated that 2-aminoquinoline prevents articular cartilage damage in osteoarthritis rats through inhibition of inflammatory factors and downregulation of NF-kappaB activation, suggesting that 2-aminoquinoline would be effective in treatment of osteoarthritis. (medscimonit.com)
Present1
  • The present study investigated the effect of 2-aminoquinoline on knee articular cartilage degradation in an osteoarthritis rat model. (medscimonit.com)
Groups2
  • The rats in treatment groups received 5, 10, 15, or 20 mg/kg doses of 2-aminoquinoline on day 2 of monosodium iodoacetate injection. (medscimonit.com)
  • What's with aminoquinoline directing groups all of a sudden? (wordpress.com)
Highly1
  • Aminoquinoline based highly sensitive fluorescent sensor for lead(II) and aluminum(III) and its application in live cell imaging. (semanticscholar.org)