Quinolines substituted in any position by one or more amino groups.
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)
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.
Substances that are toxic to blood in general, including the clotting mechanism; hematotoxins may refer to the hematopoietic system.
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)
A phospholipid-interacting antimalarial drug (ANTIMALARIALS). It is very effective against PLASMODIUM FALCIPARUM with very few side effects.
A 4-aminoquinoline compound with anti-inflammatory properties.
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.
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.
A species of protozoa that is the causal agent of falciparum malaria (MALARIA, FALCIPARUM). It is most prevalent in the tropics and subtropics.
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.
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.
Preclinical testing of drugs in experimental animals or in vitro for their biological and toxic effects and potential clinical applications.
Global conflict primarily fought on European continent, that occurred between 1914 and 1918.
Global conflict involving countries of Europe, Africa, Asia, and North America that occurred between 1939 and 1945.
1861-1865 conflict between the Union (Northern states) and the 11 Southern states that seceded and were organized as the Confederate States of America.
Hostile conflict between organized groups of people.
Time period from 1901 through 2000 of the common era.
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.
Covalent attachment of HALOGENS to other compounds.
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.
A group of compounds that contain the structure SO2NH2.
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. A hard and rare metal of the platinum group, atomic number 45, atomic weight 102.905, symbol Rh. (Dorland, 28th ed)
A metallic element with the atomic symbol Ir, atomic number 77, and atomic weight 192.22.
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.
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)
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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OBJECTIVES: To conduct a systematic review to determine clearance rates and adverse effects of topical imiquimod or fluorouracil therapy in the treatment of nonmelanoma skin cancers such as basal (BCC) and squamous cell carcinoma (SCC), and to develop recommendations for the use of topical imiquimod or fluorouracil to treat BCC and SCC.. DATA SOURCES: MEDLINE, CANCERLIT, and Cochrane databases.. STUDY SELECTION: Prospective, retrospective, and case studies in English containing a minimum of 4 subjects and a 6-month follow-up or posttreatment histologic evaluation.. DATA EXTRACTION: We calculated the rate of clearance and adverse effects for BCC subtypes and invasive and in situ SCC treated with topical imiquimod or fluorouracil.. DATA SYNTHESIS: Clearance rates varied by drug regimen, and most of the studies lacked long-term follow-up. Imiquimod use produced the following clearance rates: 43% to 100% for superficial BCC, 42% to 100% for nodular BCC, 56% to 63% for infiltrative BCC, 73% to 88% ...
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In most mammals, prolactin (PRL) is essential for maintaining lactation, and yet the short-term suppression of PRL during established lactation by bromocriptine has produced inconsistent effects on milk yield in cows and goats. To assess the effect of the long-term inhibition of PRL release in lactating dairy cows, 5 Holstein cows in early lactation received daily intramuscular injections of 1mg of the PRL-release inhibitor quinagolide for 9 wk. Four control cows received the vehicle (water) only. During the last week of the treatments, one udder half was milked once a day (1×) and the other twice a day (2×). Blood samples were harvested at milking in wk -1, 1, 4, and 8. The daily injections of quinagolide reduced milking-induced PRL release but not the basal PRL concentration. Quinagolide induced a faster decline in milk production, which was about 5.3 kg/d lower in the quinagolide-treated cows during the last 4 wk of treatment. During wk 9, the inhibition of milk production by quinagolide was
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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 ...
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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IMIQUIMOD, 1 INDICATIONS AND USAGE Aldara Cream is indicated for the topical treatment of: •Clinically typical, nonhyperkeratotic, nonhypertrophic actinic keratoses (AKs) on the face or scalp in immunocompetent
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.. ...
Treatment: ALDARA from your local pharmacy. 1.Apply 3 times per week (such as Monday, Wednesday, and Friday) for no longer than 16 weeks. 2. Apply the cream from one Aldara packet to the treatment area, and rub in the cream until it disappears. 3. Do not cover the treated skin areas with any type of plastic bandaging, and avoid nylon underwear. 4. You may wear cotton gauze or underwear over the treated area. 5. Use the medicine before going to bed and leave it on for 6 to 10 hours. Then wash off the medicine with water and a mild soap.. 6. When treating genital warts around the vagina, avoid getting the cream on the more sensitive inner layers of vaginal tissue. This could result in vaginal swelling or irritation and painful urination.. 7. Aldara is not a cure for molluscum or genital warts and it may not keep you from spreading this condition to others through vaginal, anal, or oral sex. You may develop new lesions during treatment with Aldara. ...
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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! ...
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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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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 ...
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. ...
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 ...
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 ...
A novel and efficient regioselective C-H fluorination of 8-aminoquinoline amides and sulfonamides at C5 position was achieved. Using selectfluor as
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...
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 ...
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Informed choice is of ethical and practical importance in mammography screening. To assess the level to which decisions regarding such screening are informed is thus imperative, but no specific instrument has been available to measure informed choice in the German mammography screening programme. The aims of this study were to develop the Informed Choice in Mammography Screening Questionnaire (IMQ) and to find first evidence for the factor structure, reliability and validity of its different components. The IMQ was sent to 17.349 women aged 50 in Westphalia-Lippe, Germany. The instrument has been developed after consideration of (1) the results of qualitative interviews on decision making in the mammography screening programme, (2) relevant literature on other informed choice instruments and (3) a qualitative study on influencing factors. The IMQ comprises 3 scales (attitude, norms, and barriers), 1 index (knowledge) and singular items covering intention to participate and sociodemographic variables. To
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Orf is a self-limiting disease, which means it will get better on its own without treatment. It usually clears up within three to six weeks. It may be useful to cover the lesion with a sterile (hygienic) dressing and immobilise your finger to help reduce discomfort. Read more about applying plasters and other dressings.. You should see your GP if the lesion isnt healing, you develop a fever (high temperature) or youre in severe pain, as some people also develop a bacterial infection. This may require treatment with antibiotics. In rare cases the lesion may not go away and a minor surgical procedure may be required to remove it.. Although theres some evidence to suggest that using topical imiquimod cream may help to reduce lesions, you should speak to your GP or pharmacist for advice first.. ...
Hi fifi65 and welcome to the online community. I havent had this treatment but noticed your post hadnt had any replies yet. Im sorry to hear how painful youre finding using Aldara (Imiquimod) cream is.. You should have been given a leaflet from you hospital when they prescribed this treatment telling you how to apply it and what to expect. I dont know which hospital you attended but have found this information from Royal Berkshire Hospital for you if you havent been given any information. The leaflet says to be guided by how severely you react and to stop using it if your reaction is severe and you are unable to tolerate it. However, its important to use the cream as your hospital prescribed it.. If you have had a severe reaction to the cream then Id recommend getting in touch with your team as soon as possible so that they can advise you what to do.. x ...
Like a tourist without a map, tumor-fighting T cells have a hard time finding their destination without directions. According to Clark et al. (page 2221), dismantling these directions helps skin cancer cells hide from killer T cells.. To enter the skin, T cells must grab on to the adhesive molecule E-selectin, which is expressed on the endothelial cells lining blood vessels in the skin. The authors now find that many of the vessels in skin cancer lesions lack E-selectin, causing beneficial T cells to pass by unaware. The tumors were instead populated by suppressive regulatory (T reg) cells, perhaps coaxed in by the tumor to safeguard against killer cells that somehow gain access. Both tactics have also been seen in other types of human cancer.. Reversing the suppressive effect of T reg cells is one of the beneficial effects of topical immune-stimulating drugs like the TLR agonist imiquimod, which is effective in treating certain types of skin cancer. Indeed, Clark et al. found that imiquimod ...
For those of you who do not know about Aldara -- it is a highly-promoted cream made by 3M Pharmaceuticals and used for skin cancer and genital warts, and now even for freckles. It is known to cause severe autoimmune disease and can even kill. See www.doctorsaredangerous.com for details. Aldara and TGN1423 (the killer drug made by German firm, TeGenero, and tested by the American firm, Parexel Research Co), are not precisely the same, but they are both designed to stimulate and manipulate the immune system into performing hazardous things, and the consequences for both are identical when things go wrong. A number of clinical documents have referred to TGN1412 as an IRM. IRMs are well known by many in the medical community to be extremely dangerous, uncontrollable and unpredictable. Independent scientists warn that IRMs should never be used on humans, under any circumstances. Im sure those men in London who were paid 2000 pounds to participate in the trial would agree. Texan Richard Beasley, and ...
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J-113,397 LY-2940094 SB-612,111 Shinkai H, Ito T, Iida T, Kitao Y, Yamada H, Uchida I (November 2000). "4-Aminoquinolines: ...
... is in the 8-aminoquinoline family of medications. How it works is unclear but it is effective both in the liver and ...
... is a 4-aminoquinoline compound related to chloroquine. Amodiaquine was first made in 1948. It is on the World ...
... is in the antimalarial and 4-aminoquinoline families of medication. Hydroxychloroquine was approved for ... label advises that hydroxychloroquine should not be prescribed to individuals with known hypersensitivity to 4-aminoquinoline ...
2ohl: X-ray crystal structure of beta secretase complexed with 2-aminoquinoline ...
Lee, S. J.; Makaravage, K. J.; Brooks, A. F.; Scott, P. J. H.; Sanford, M. S. "Cu‐Mediated Aminoquinoline‐Directed ... "Copper-Mediated Aminoquinoline-Directed Radiofluorination of Aromatic C−H Bonds with K18F". Angewandte Chemie International ...
"Copper-Mediated Aminoquinoline-Directed Radiofluorination of Aromatic C−H Bonds with K18F". Angewandte Chemie International ...
"Formation of derivatives of dioxindole from esters of mesoxalic acid and aromatic amines or amino quinolines". Compt. Rend. 156 ...
... is an 8-aminoquinoline drug formerly used for the treatment of malaria. It is closely related to primaquine. ... Sweeney AW, Blackburn CR, Rieckmann KH (August 2004). "Short report: the activity of pamaquine, an 8-aminoquinoline drug, ...
Preprint published on July 15, 2020 stated: "the 4-aminoquinoline drugs are relatively weak antivirals ... Thus, to provide the ...
Bogert, M. T.; Fisher, H. L. (1912). "The Preparation and Properties of 5-Aminoquinoline-6-Carboxylic Acid and Certain Related ... His PhD dissertation focused on the preparation and properties of 5-aminoquinoline-6-carboxylic acid and related compounds. ...
... is an analog of pamaquine which was the first drug of the 8-aminoquinoline class; tafenoquine is another such drug. ...
Shinkai, H; Ito, T; Iida, T; Kitao, Y; Yamada, H; Uchida, I (2000). „4-Aminoquinolines: novel nociceptin antagonists with ...
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 ...
Tenoxicam; 4-Aminoquinolines: Antrafenine. *Floctafenine. *Glafenine; Quinazolines: Fluproquazone. *Proquazone; Aminonicotinic ...
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 ...
Resochin (7-chloro-4- 4- (diethylamino) - 1 - methylbutyl amino quinoline) and a similar compound Sontochin (3-methyl Resochin ...
Later when synthetic derivatives of quinine were introduced, chloroquine phosphate, a 4-aminoquinoline was found to be less ...
The authors rely on an 8-aminoquinoline directing group to control the regioselectivity of migratory insertion and stabilize ...
... the first synthetic antimalarial compound-Atabrin and this was followed by Resochin and Sontochin derived from 4-aminoquinoline ...
... aminoquinolines MeSH D03.438.810.050.060 - amodiaquine MeSH D03.438.810.050.180 - chloroquine MeSH D03.438.810.050.180.350 - ...
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 ( ...
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. ...
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 ...
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 ...
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 ...
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 ...
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 ...
... dc.contributor.advisor. VanderWerf, Calvin A.. ...
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. ...
... amino]quinoline-4-carboxamide
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), ...
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. ...
... amino]quinoline-4-carboxamide
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 ...
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 ...
Graves, P.M.; Gelband, H.; Garner, P. Primaquine or other 8-aminoquinoline for reducing P. falciparum transmission. Cochrane ...
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. ...
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. ...
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, ...
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. ...
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 ...
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. ...
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 ...
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 ...
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)( ...
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 ...
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. ...
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 ...
3-Aminoquinoline/ACM580176 can be provided in Alfa Chemistry. We are dedicated to provide our customers the best products and ...
Aralen Phosphate - Get up-to-date information on Aralen Phosphate side effects, uses, dosage, overdose, pregnancy, alcohol and more. Learn more about Aralen Phosphate
  • 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)
  • 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)
  • 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)
  • 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)
  • 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)
  • 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)
  • 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)
  • 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)
  • 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)
  • 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)
  • 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)
  • Five-coordinate bis(8-aminoquinoline) nitrosylcobalt complexes. (nii.ac.jp)
  • Much attention was paid to the apparent absence of 4-aminoquinoline resistance in much of Central America (less Panama) and in Hispaniola. (ajtmh.org)
  • 6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. (soton.ac.uk)
  • 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)
  • In vitro oxidation and acetylation of 5-aminoquinoline by rabbit liver enzyme preparation has been investigated. (bvsalud.org)
  • Metabolism of 5-aminoquinoline with liver cytosol enzyme. (bvsalud.org)
  • 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)
  • 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)
  • 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)
  • Both introduction of a hydrophobic substituent next to the cyano group and aminoquinoline methylation considerably improved isoform selectivity. (rcsb.org)
  • 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)
  • 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)
  • The endoperoxide OZ439, currently in Phase II clinical trials, and a new 8-aminoquinoline , NPC-1161B, also demonstrated transmission-blocking potential. (thefreedictionary.com)
  • 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)
  • 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)
  • 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)
  • The present study investigated the effect of 2-aminoquinoline on knee articular cartilage degradation in an osteoarthritis rat model. (medscimonit.com)
  • 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)
  • Aminoquinoline based highly sensitive fluorescent sensor for lead(II) and aluminum(III) and its application in live cell imaging. (semanticscholar.org)