Amidines substituted with a benzene group. Benzamidine and its derivatives are known as peptidase inhibitors.
Amide derivatives of phosphoric acid such as compounds that include the phosphoric triamide (P(=O)(N)(N)(N)) structure.
A plant genus of the family ASTERACEAE. Arctiin (LIGNANS) is in the seed.
A strong corrosive acid that is commonly used as a laboratory reagent. It is formed by dissolving hydrogen chloride in water. GASTRIC ACID is the hydrochloric acid component of GASTRIC JUICE.
A cell line derived from cultured tumor cells.
All of the processes involved in increasing CELL NUMBER including CELL DIVISION.
Control of drug and narcotic use by international agreement, or by institutional systems for handling prescribed drugs. This includes regulations concerned with the manufacturing, dispensing, approval (DRUG APPROVAL), and marketing of drugs.
The unconsolidated mineral or organic matter on the surface of the earth that serves as a natural medium for the growth of land plants.
Woody, usually tall, perennial higher plants (Angiosperms, Gymnosperms, and some Pterophyta) having usually a main stem and numerous branches.
A plant family of the order Caryophyllales, subclass Caryophyllidae, class Magnoliopsida.
The presence of bacteria, viruses, and fungi in the soil. This term is not restricted to pathogenic organisms.
A functional system which includes the organisms of a natural community together with their environment. (McGraw Hill Dictionary of Scientific and Technical Terms, 4th ed)
Total mass of all the organisms of a given type and/or in a given area. (From Concise Dictionary of Biology, 1990) It includes the yield of vegetative mass produced from any given crop.
A nonmetallic element with atomic symbol C, atomic number 6, and atomic weight [12.0096; 12.0116]. It may occur as several different allotropes including DIAMOND; CHARCOAL; and GRAPHITE; and as SOOT from incompletely burned fuel.
A food group comprised of EDIBLE PLANTS or their parts.
The fleshy or dry ripened ovary of a plant, enclosing the seed or seeds.
The edible portions of any animal used for food including domestic mammals (the major ones being cattle, swine, and sheep) along with poultry, fish, shellfish, and game.
Exclusive legal rights or privileges applied to inventions, plants, etc.
A plastic substance deposited by insects or obtained from plants. Waxes are esters of various fatty acids with higher, usually monohydric alcohols. The wax of pharmacy is principally yellow wax (beeswax), the material of which honeycomb is made. It consists chiefly of cerotic acid and myricin and is used in making ointments, cerates, etc. (Dorland, 27th ed)
Articles of food which are derived by a process of manufacture from any portion of carcasses of any animal used for food (e.g., head cheese, sausage, scrapple).
A condition in which the FORAMEN OVALE in the ATRIAL SEPTUM fails to close shortly after birth. This results in abnormal communications between the two upper chambers of the heart. An isolated patent ovale foramen without other structural heart defects is usually of no hemodynamic significance.
Suspensions of killed or attenuated microorganisms (bacteria, viruses, fungi, protozoa), antigenic proteins, synthetic constructs, or other bio-molecular derivatives, administered for the prevention, amelioration, or treatment of infectious and other diseases.
A contagious disease caused by canine adenovirus (ADENOVIRUSES, CANINE) infecting the LIVER, the EYE, the KIDNEY, and other organs in dogs, other canids, and bears. Symptoms include FEVER; EDEMA; VOMITING; and DIARRHEA.
Vaccines in which the infectious microbial nucleic acid components have been destroyed by chemical or physical treatment (e.g., formalin, beta-propiolactone, gamma radiation) without affecting the antigenicity or immunogenicity of the viral coat or bacterial outer membrane proteins.
Diseases of the domestic dog (Canis familiaris). This term does not include diseases of wild dogs, WOLVES; FOXES; and other Canidae for which the heading CARNIVORA is used.
Suspensions of attenuated or killed viruses administered for the prevention or treatment of infectious viral disease.
Recombinant DNA vectors encoding antigens administered for the prevention or treatment of disease. The host cells take up the DNA, express the antigen, and present it to the immune system in a manner similar to that which would occur during natural infection. This induces humoral and cellular immune responses against the encoded antigens. The vector is called naked DNA because there is no need for complex formulations or delivery agents; the plasmid is injected in saline or other buffers.
Two or more vaccines in a single dosage form.
The use of statistical methods in the analysis of a body of literature to reveal the historical development of subject fields and patterns of authorship, publication, and use. Formerly called statistical bibliography. (from The ALA Glossary of Library and Information Science, 1983)
Critical and exhaustive investigation or experimentation, having for its aim the discovery of new facts and their correct interpretation, the revision of accepted conclusions, theories, or laws in the light of newly discovered facts, or the practical application of such new or revised conclusions, theories, or laws. (Webster, 3d ed)
Copies of a work or document distributed to the public by sale, rental, lease, or lending. (From ALA Glossary of Library and Information Science, 1983, p181)
Disciplines concerned with the interrelationships of individuals in a social environment including social organizations and institutions. Includes Sociology and Anthropology.
Rare autosomal recessive congenital malformation syndrome characterized by cryptophthalmos, SYNDACTYLY and UROGENITAL ABNORMALITIES. Other anomalies of bone, ear, lung, and nose are common. Mutations on FRAS1 and FREM2 are associated with the syndrome.
Research that involves the application of the natural sciences, especially biology and physiology, to medicine.
Single or multi-sheet notices made to attract attention to events, activities, causes, goods, or services. They are for display, usually in a public place and are chiefly pictorial.
A chemical element having an atomic weight of 106.4, atomic number of 46, and the symbol Pd. It is a white, ductile metal resembling platinum, and following it in abundance and importance of applications. It is used in dentistry in the form of gold, silver, and copper alloys.
Organic compounds containing the radical -CSNH2.
The facilitation of a chemical reaction by material (catalyst) that is not consumed by the reaction.
The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.
A non-essential amino acid occurring in natural form as the L-isomer. It is synthesized from GLYCINE or THREONINE. It is involved in the biosynthesis of PURINES; PYRIMIDINES; and other amino acids.
Any member of the group of ENDOPEPTIDASES containing at the active site a serine residue involved in catalysis.
The study of natural phenomena by observation, measurement, and experimentation.
Peptide hydrolases that contain at the active site a SERINE residue involved in catalysis.
Exogenous or endogenous compounds which inhibit SERINE ENDOPEPTIDASES.
Clotting time of PLASMA recalcified in the presence of excess TISSUE THROMBOPLASTIN. Factors measured are FIBRINOGEN; PROTHROMBIN; FACTOR V; FACTOR VII; and FACTOR X. It is used for monitoring anticoagulant therapy with COUMARINS.
A quantitative measure of the frequency on average with which articles in a journal have been cited in a given period of time.
A novel composition, device, or process, independently conceived de novo or derived from a pre-existing model.
Body of knowledge related to the use of organisms, cells or cell-derived constituents for the purpose of developing products which are technically, scientifically and clinically useful. Alteration of biologic function at the molecular level (i.e., GENETIC ENGINEERING) is a central focus; laboratory methods used include TRANSFECTION and CLONING technologies, sequence and structure analysis algorithms, computer databases, and gene and protein structure function analysis and prediction.
The thin, highly vascular membrane covering most of the posterior of the eye between the RETINA and SCLERA.
The layer of pigment-containing epithelial cells in the RETINA; the CILIARY BODY; and the IRIS in the eye.
The single layer of pigment-containing epithelial cells in the RETINA, situated closely to the tips (outer segments) of the RETINAL PHOTORECEPTOR CELLS. These epithelial cells are macroglia that perform essential functions for the photoreceptor cells, such as in nutrient transport, phagocytosis of the shed photoreceptor membranes, and ensuring retinal attachment.
Enzymes that catalyze the rearrangement of geometry about double bonds. EC 5.2.

Quantifying GPIIb/IIIa receptor binding using 2 monoclonal antibodies: discriminating abciximab and small molecular weight antagonists. (1/203)

BACKGROUND: Dosing of glycoprotein (GP) IIb/IIIa receptor antagonists is frequently based on the inhibition of platelet aggregation, which may be influenced by the agonist used or concurrent medications. Here we describe a monoclonal antibody-based technique to quantify total and ligand-occupied GPIIb/IIIa receptors. METHODS AND RESULTS: In vitro binding of monoclonal antibodies, LYP18 (Mab1) and 4F8 (Mab2), to the GPIIb/IIIa complex, was characterized using purified receptor and to platelets by flow cytometry. Patients undergoing coronary angioplasty received a single 20 mg dose of the oral GPIIb/IIIa antagonist, xemilofiban, or matching placebo, and antibody binding was compared with inhibition of platelet aggregation. Mab1 and Mab2 were bound to purified GPIIb/IIIa and to unoccupied, inactivated receptor on platelets. Mab2 identified the beta3 subunit, whereas Mab1 was complex-specific. Neither antibody interfered with the other's binding, suggesting that they identified distinct sites. Mab1 identified 53 300+/-5423 GPIIb/IIIa sites per platelet, whereas Mab2 identified 50 120+/-5066 sites per platelet. Mab1 binding was inhibited by abciximab in a dose dependent manner (IC50, 0.85+/-0.1 microg/mL), whereas Mab2 binding was unaffected. In contrast, the 2 small molecular weight antagonists, SC-57101A (IC50, 0.22+/-0.06 micromol/L) and eptifibatide (IC50, 0.35+/-0.14 micromol/L) inhibited Mab2 but not Mab1 binding. In patients treated with xemilofiban, Mab1 binding was unaltered but Mab2 binding decreased from 37 930+/-2061 sites per platelet at baseline to 8318+/-870 sites per platelet 6 hours after dosing (P<0.0001). Platelet aggregation to adenosine diphosphate (20 micromol/L) fell to 3+/-3% of baseline in line with the inhibition of Mab2 binding (correlation coefficient 0.8, P<0.0001). CONCLUSIONS: Mab1 and Mab2 bind to GPIIb/IIIa and are differentially displaced by abciximab and small molecular weight antagonists. These antibodies may be used to monitor receptor number and occupancy during administration of a GPIIb/IIIa antagonist.  (+info)

Lesions and identification of crystalline precipitates of glycoprotein IIb-IIIa antagonists in the rat kidney. (2/203)

Two glycoprotein IIb-IIIa antagonists (xemilofiban, SC-54684A, and orbofiban, SC-57099B), which are platelet aggregation inhibitors, caused crystalline precipitates in the kidney tubules of rats at high dosages. Dogs were not affected. Depending on the degree of the precipitation, which was dosage dependent, and the location, which differed somewhat between the two compounds, the lesions varied from acute obstruction with tubule cell necrosis, nephron dilation, and sudden death with no inflammation to severe chronic pyogranulomatous inflammation. In order to understand the relevance of the lesions, it was important to identify the precipitates. This was technically challenging because the crystals were water soluble (dissolving in routine fixing and staining techniques) and were present in insufficient quantity to physically isolate. Techniques were devised to evaluate the crystals in situ in unstained frozen sections prepared without directly embedding the tissues in supporting medium, which interfered with the analyses. The crystals were analyzed in situ by infrared and Raman spectroscopy and time-of-flight secondary ion mass spectroscopy (TOF-SIMS). Uroliths found in the renal pelvis of one animal were analyzed by liquid chromatography/mass spectrometry. The resulting spectra showed that the crystals were the de-esterified acids of the parent compounds. This knowledge allowed us to predict that the crystalline precipitates would not be a hazard to humans because of the large multiples of the human dosage at which they occurred and because of differences in renal physiology between rats, dogs, and humans.  (+info)

Potent selective nonpeptidic inhibitors of human lung tryptase. (3/203)

Human lung tryptase, a homotetrameric serine protease unique to mast cell secretory granules, has been implicated in the pathogenesis of asthma. A hypothesis that tethered symmetrical inhibitors might bridge two adjacent active sites was explored via a rationally designed series of bisbenzamidines. These compounds demonstrated a remarkable distanced-defined structure-activity relationship against human tryptase with one series possessing subnanomolar potencies. Additional evidence supporting the concept of active-site bridging is also presented.  (+info)

Design and evaluation of novel bivalent thrombin inhibitors based on amidinophenylalanines. (4/203)

Two bivalent thrombin inhibitors were synthesized, which consist of a benzamidine-based active-site-blocking segment, a fibrinogen recognition exosite inhibitor and a peptidic linker connecting these fragments. BZA-1 hirulog contains an Nalpha-(2-naphthylsulfonyl)-S-3-amidinophenylalanyl-is onipecotic acid residue connected via the carboxyl group to the linker segment. The active-site-directed moiety of BZA-2 hirulog [Nalpha-(2-naphthylsulfonyl-glutamyl)-R-4-amidinophenylal anyl-piperid ide] was coupled to the linker via the side chain of the glutamic acid. Both BZA-hirulogs contain almost identical linker-exo site inhibitor parts, except for the substitution of a glycine as the first linker residue in BZA-1 hirulog by a gamma-amino butyric acid in BZA-2 hirulog, thus increasing flexibility and linker length by two additional atoms. BZA-1 hirulog showed moderate potency (Ki = 0. 50 +/- 0.14 nM), while BZA-2 hirulog was characterized as a slow, tight binding inhibitor of thrombin (Ki = 0.29 +/- 0.08 pM). The stability in human plasma of both analogs was strongly improved compared with hirulog-1. For BZA-2 hirulog a significantly reduced plasma clearance was observed after intravenous injection in rats compared with BZA-1 hirulog and hirulog-1. The X-ray structure of the BZA-2 hirulog in complex with human alpha-thrombin was solved and confirmed the expected bivalent binding mode.  (+info)

Draculin, the anticoagulant factor in vampire bat saliva, is a tight-binding, noncompetitive inhibitor of activated factor X. (5/203)

The kinetic mechanism of action of Draculin on activated Factor X (FXa) is established. Draculin inhibits activated Factor X within seconds of incubation at near equimolar concentration (2-6 times on molar basis). Fitting the data to the equation for a tight-binding inhibitor gives a value for K(i)(K(d)) = 14.8+/-1.5 nM. The formation of the Draculin-FXa complex can be explained by a two-step mechanism, where for the first, reversible step, k(on) = 1.117 (+/- 0.169, S.E.M.) x 10(6) M(-1)s(-1) and k(off) = 15.388 (+/- 1.672) x 10(-3) s(-1), while for the second, irreversible step, which is concentration-independent, k(2) = 0.072 s(-1). K(d) obtained from k(off)/k(on) = 13.76 nM. Lineweaver-Burk plot shows a noncompetitive behavior. This noncompetitive mode of inhibition of Draculin is supported by the observation that Draculin, at concentrations giving complete inhibition, does not impair binding of p-aminobenzamidine to FXa. Moreover, under the same conditions, Draculin induces <14% decrease of the fluorescence intensity of the p-aminobenzamidine-FXa complex. We conclude that Draculin is a noncompetitive, tight-binding inhibitor of FXa, a characteristic so far unique amongst natural FXa inhibitors.  (+info)

In vivo and in vitro comparison of the short-term hematopoietic toxicity between hydroxyurea and trimidox or didox, novel ribonucleotide reductase inhibitors with potential anti-HIV-1 activity. (6/203)

Inhibitors of the cellular enzyme ribonucleotide reductase (hydroxyurea, [HU]) have been proposed as a new therapeutic strategy for the treatment of HIV type-1 (HIV-1) infection. However, HU use may be limited by the frequent development of hematopoietic toxicity. We report here short-term hematopoietic toxicity in mice receiving HU when compared to either of two more potent enzyme inhibitors, didox (DX) and trimidox (TX). High dose HU, DX, and TX monotherapy (500, 460, and 220 mg/kg/day respectively) was administered by daily i.p. injection (Monday-Friday) to C57BL/6 mice for 10 weeks. Effects on hematopoiesis were established by quantitating peripheral blood indices (hematocrit, hemoglobin, mean corpuscular volume, mean cell hemoglobin, mean corpuscular hemoglobin concentration, RBC, and WBC) and numbers of colony-forming units-granulocyte-macrophage (CFU-GM) and BFU-E from bone marrow and spleen. HU produced rapid induction of a macrocytic hypochromic anemia and altered white blood cell kinetics associated with myelosuppression defined as reduced marrow organ cellularity and induction of splenic extramedullary hematopoiesis. Compared to HU, TX and DX induced fewer changes in peripheral blood indices and CFU-GM and BFU-E per hematopoietic organ. In vitro human and murine marrow CFU-GM and BFU-E colony formations were assayed in the presence of dose escalation HU, DX, or TX (0, 1, 10, 50, 100, and 200 microM). HU inhibited colony formation more than either DX or TX. These in vivo and in vitro studies suggest that novel ribonucleotide reductase inhibitors TX and DX may provide an effective alternative to HU in HIV-1 therapy because they demonstrate reduced hematopoietic toxicity.  (+info)

Different effects of trypsin inhibitors on intestinal gene expression of secretin and on pancreatic bicarbonate secretion in CCK-A-receptor-deficient rats. (7/203)

The effects of oral administration of two synthetic trypsin inhibitors (camostate and ONO-3403) and soybean trypsin inhibitor (SBTI) on cholecystokinin (CCK), secretin gene expression and pancreatic secretion were examined in CCK-A-receptor-deficient (OLETF) rats. The rats were fed chow containing 0.1% trypsin inhibitors for 7 days. To examine pancreatic secretion, the rats were prepared with cannulae to drain the bile and pancreatic juice separately, a duodenal cannula and an external jugular vein cannula. The animals were maintained in Bollman cages and the experiments were conducted 4 days after surgery. The levels of CCK mRNA were significantly increased by each treatment. The levels of secretin mRNA were significantly increased by camostate and SBTI, but not by ONO-3403. Bicarbonate secretion was significantly increased in rats treated with camostate and ONO-3403, but not SBTI, while protein secretion was not affected by any treatment. These observations suggest that increased bicarbonate secretion produced by synthetic trypsin inhibitors in CCK-A-receptor-deficient rats may not be due to secretin but due to ONO-3403 in the circulation.  (+info)

Glycoprotein IIb/IIIa antagonists induce apoptosis in rat cardiomyocytes by caspase-3 activation. (8/203)

The platelet integrin glycoprotein (GP) IIb/IIIa, which mediates platelet aggregation, has been the target for novel antiplatelet agents, the GPIIb/IIIa antagonists. Several GPIIb/IIIa antagonists have been developed based on the peptide RGDS present in adhesion proteins, including the principle ligand fibrinogen. The apoptosis enzyme, procaspase-3, contains an RGD-recognition sequence and is activated by RGDS. We examined the effects of RGDS and several GPIIb/IIIa antagonists on cell death and procaspase-3 activation in rat neonatal cardiomyocytes. These antagonists do not recognize rat integrins, yet RGDS, orbofiban, and xemilofiban induced dose-dependent apoptosis and procaspase-3 activation in cardiomyocytes over 72 h, particularly under hypoxic conditions. Scrambled peptide, the monoclonal antibody 7E3 or integrelin (a peptide containing a KGD sequence), had little or no effect. Immunoprecipitation of procaspase-3 followed by treatment with the compounds showed that procaspase-3 was activated directly by RGDS, orbofiban, xemilofiban, and by monoclonal 7E3 antibody, the latter demonstrating that compounds must enter cells to induce apoptosis through caspase activation. Integrelin had no effect. Binding studies with (3)H-SC52012B, a GPIIb/IIIa antagonist analogue of orbofiban, showed no specific binding to cardiomyocytes, but the radioligand accumulated intracellularly over 72 h. (3)H-SC52012B also bound directly to human recombinant caspase-3 (K(d), 59 +/- 2 nm), and this was prevented by orbofiban, xemilofiban, and the monoclonal 7E3 antibody but not by integrelin. Finally confocal microscopy showed that RGDS co-localized with caspase-3 inside the cell. These data show that RGDS and its mimetics induce cardiomyocyte apoptosis by direct activation of procaspase-3.  (+info)

The binding of 2,5-bis(4-amidinophenyl)furan (APF) to calf thymus DNA, [poly(dA-dT)]2, and [poly(dG-dC)]2 has been studied with flow linear dichroism and circular dichroism spectroscopy. The electronic excited states of the APF chromophore were first characterized using experimental and quantum mechanical methods: it is shown that the low-energy absorption band (320-400 nm) originates from only a single electronic transition which is polarized along the long axis of the molecule, information that is crucial for the structural interpretation of the linear and circular dichroism spectra of the APF-DNA complexes. By contrast, in the unsymmetric analogue 4,6-diamidino-2-phenylindole (DAPI) two overlapping transitions, with somewhat divergent polarizations, both contribute to the first absorption band. Upon binding to DNA the spectroscopic behavior of APF strongly resembles that of DAPI. The linear dichroism data show that the drug binds to calf thymus DNA and [poly(dA-dT)]2 with an angle of 46-degrees +/-
A previously healthy 53-year-old man had keratitis of the right eye for six months, unresponsive to topical medical therapy. Acanthamoeba was grown from tissue obtained by corneal biopsy and from aqueous from an anterior chamber tap. The patient was treated with propamidine isethionate 0.1% drops and dibromopropamidine isethionate 0.15% ointment, and after two and a half months the ocular inflammation was continuing to resolve. This case supports a role for the diamidines in the treatment of acanthamoebic keratitis. ...
4-(TRIFLUOROMETHYL)BENZAMIDOXIME chemical properties, What are the chemical properties of 4-(TRIFLUOROMETHYL)BENZAMIDOXIME 22179-86-8, What are the physical properties of 4-(TRIFLUOROMETHYL)BENZAMIDOXIME ect.
1M6F: Strong Binding in the DNA Minor Groove by an Aromatic Diamidine With a Shape That Does Not Match the Curvature of the Groove
1MAY: Inhibition of trypsin and thrombin by amino(4-amidinophenyl)methanephosphonate diphenyl ester derivatives: X-ray structures and molecular models.
Literature References: Platelet fibrinogen receptor (GPIIb/IIIa) antagonist. Prodrug converted in vivo to the active acid form. Prepn: P. R. Bovy et al., WO 9307867; eidem, US 5344957 (1993, 1994 both to Monsanto; Searle); J. Cossy et al., Bioorg. Med. Chem. Lett. 7, 1699 (1997). Structure-activity study: J. A. Zablocki et al., J. Med. Chem. 38, 2378 (1995). Pharmacology: N. S. Nicholson et al., Circulation 91, 403 (1995). Clinical pharmacokinetics: D. J. Kereiakes et al., ibid. 94, 906 (1996). Clinical evaluation in unstable angina: C. Simpfendorfer et al., ibid. 96, 76 (1997). ...
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Propamidine is an antiseptic and disinfectant. Propamidine isethionate, the salt of propamidine with isethionic acid, is used in the treatment of Acanthamoeba infection. Perrine D, Chenu JP, Georges P, Lancelot JC, Saturnino C, Robba M (February 1995). Amoebicidal efficiencies of various diamidines against two strains of Acanthamoeba polyphaga. Antimicrob. Agents Chemother. 39 (2): 339-42. doi:10.1128/aac.39.2.339. PMC 162538 . PMID 7726493 ...
TY - PAT. T1 - Synthesis and Antiprotozoal Activity of Dicationic 3.5 Diphenylisoxazoles. AU - Tidwell,Richard R.. AU - Bakunova,Svetlana M.. AU - Bakunov,Stanislav. AU - Patrick,Donald A.. N1 - Status: published applicationnumber: 11/415,982 usclass: 514/378 ; 548/247 applicationnumber: 11/415,982. PY - 1800. Y1 - 1800. N2 - Novel dicationic 3,5-diphenylisoxazole compounds are described. Synthetic routes to these novel compounds are provided. Several of the compounds displayed in vitro activity versus Trypanosoma brucei brucei and Plasmodium falciparum comparable to that of furamidine. A majority of the novel compounds also were less toxic to VERO cells than furamidine.. AB - Novel dicationic 3,5-diphenylisoxazole compounds are described. Synthetic routes to these novel compounds are provided. Several of the compounds displayed in vitro activity versus Trypanosoma brucei brucei and Plasmodium falciparum comparable to that of furamidine. A majority of the novel compounds also were less toxic to ...
Product information for Brolene Eye Drops 10ml. Contains the active ingredient Propamidine Isetionate 0.1% w/v?which is a disinfectant and antibacterial. Used for the treatment of minor eye infections.. Ingredients. Active Ingredient: Propamidine Isetionate 0.1% w/v, Other Ingredients: Benzalkonium Chloride (Preservative), Ammonium Chloride, Sodium Chloride, Sodium Hydrochloride and Water for injections, See enclosed leaflet for further information. Storage. Store below 25 C.. Contents are sterile until opened and should be used within 4 weeks of opening (7 days in a hospital).. Preparation and Usage. For the treatment of minor eye infections in adults and children. Dose: Apply one or two drops into the affected eye up to four times daily.. Always read the leaflet before using the medicine.. Safety Warnings. If symptoms do not improve consult your doctor.. Do not use if you are allergic to any of the ingredients.. Keep out of the sight and reach of children.. Do not use with hard or soft contact ...
This invention relates to novel tricyclic pteridinones, their aza analogs and their pharmaceutically acceptable salts. Further encompassed by the invention is a novel process for the production of the tricyclic pteridinones and their aza analogs. The compounds of the invention exhibit cardiovascular properties, particularly mixed vasodilation and selective venous and arterial dilation. Pharmaceutical compositions are proposed for the compounds.
sample_1: ATC2521, [U-100% 13C; U-100% 15N], 1 ± 0.2 mM; TRIS 10 ± 0.2 mM; glycerol 5 ± 0.2 %; Benzamidine 1 ± 0.2 mM; sodium chloride 300 ± 0.2 mM; sodium azide 0.01 ± 0.1 %. sample_2: ATC2521, [U-100% 13C; U-100% 15N], 1 ± 0.2 mM; TRIS 10 ± 0.2 mM; glycerol 5 ± 0.2 %; Benzamidine 1 ± 0.2 mM; sodium chloride 300 ± 0.2 mM; sodium azide 0.01 ± 0.1 %. sample_conditions_1: ionic strength: 0.3 M; pH: 7.0; pressure: 1 atm; temperature: 298 K ...
sample_1: ATU1203, [U-13C; U-15N], 0.5 mM; MOPS 10 mM; sodium chloride 450 mM; DTT 10 mM; benzamidine 10 mM; NaN3 0.01%; ZnSO4 10 uM. sample_conditions_1: ionic strength: 450 mM; pH: 6.5; pressure: 1 atm; temperature: 298 K ...
SWISS-MODEL Template Library (SMTL) entry for 4n8z.1. In situ lysozyme crystallized on a MiTeGen micromesh with benzamidine ligand
0023]The term allergic inflammatory diseases, as used herein, refers to non-specific inflammatory diseases caused by a variety of allergens, and includes allergic rhinitis, asthma, allergic conjunctivitis, allergic dermatitis, atopic dermatitis, contact dermatitis, urticaria, anaphylaxis, insect allergy, food allergy, and drug allergy. The preventive and therapeutic efficacy of the N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy} benzamidine compound on allergic inflammatory diseases was confirmed in a mouse model of asthma which was induced by chronic exposure to ovalbumin. The benzamidine compound was administered for a period of 18 days, starting on the day of immunization with ovalbumin. 15 days after immunization, experimental animals were challenged with ovalbumin, and sacrificed three days later to investigate lung weight, changes in the cellular profile of bronchoalvelar lavage fluid and peripheral blood samples, and histopathological changes in lung tissue. ...
Pentamidine is an antimicrobial medication used to treat African trypanosomiasis, leishmaniasis, babesiosis, and to prevent and treat pneumocystis pneumonia (PCP) in people with poor immune function.[1] In African trypanosomiasis it is used for early disease before central nervous system involvement, as a second line option to suramin.[1] It is an option for both visceral leishmaniasis and cutaneous leishmaniasis.[1] Pentamidine can be given by injection into a vein or muscle or by inhalation.[1] Common side effects of the injectable form include low blood sugar, pain at the site of injection, nausea, vomiting, low blood pressure, and kidney problems.[1] Common side effects of the inhaled form include wheezing, cough, and nausea.[1] It is unclear if doses should be changed in those with kidney or liver problems.[1] Pentamidine is not recommended in early pregnancy but may be used in later pregnancy.[1] Its safety during breastfeeding is unclear.[2] Pentamidine is in the aromatic diamidine family ...
Abstract. Copper-catalyzed cross-coupling reactions of amidine salts with aryl iodides give monoarylated amidines in good yields under ligand-free conditions. DMF was the superior solvent for the N-arylation of benzamidines, while MeCN was used in the formation of N-aryl amidines in good yield.. ...
This invention is directed to benzamidine derivatives substituted by amino acid and hydroxy acid derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.
Some compounds articulated around a piperazine or an ethylenediamine linker have been evaluated in vitro to determine their activity in the presence of a 3T6 fibroblast cell line and an axenic culture of Pneumocystis carinii, respectively. The most efficient antifungal derivatives, namely N,N′-bis(benzamidine-4-yl)ethane-1,2-diamine (compound 6, a diamidine) and N-(benzamidine-4-yl)-N′-phenylethane-1,2-diamine (compound 7, a monoamidine), exhibited no cytotoxicity and were evaluated in vivo in a rat model. Only the diamidine 6 emerged as a promising hit for further studies.
The Fukuoka Farming Mailing List was created to discuss Masanobu Fukuokas revolutionary method of natural farming. Discussion of Fukuokas books, ongoing projects in Fukuoka Farming, creating and dispersing seed balls, and anything else to do with Masanobu Fukuoka, his life and work are all encouraged. This list was primarily created as a place for people interested in Fukuokas methods to network and share resources. Lets help change the way people think about growing food.
The Fukuoka Farming Mailing List was created to discuss Masanobu Fukuokas revolutionary method of natural farming. Discussion of Fukuokas books, ongoing projects in Fukuoka Farming, creating and dispersing seed balls, and anything else to do with Masanobu Fukuoka, his life and work are all encouraged. This list was primarily created as a place for people interested in Fukuokas methods to network and share resources. Lets help change the way people think about growing food.
O-Benzoylated benzamidoximes give 1,2,4-oxadiazoles (yields above 90%) in water-alcoholic media of pH = 2.45 to 6.20. The cyclization rate has been studied with 28 derivatives containing different substituents. The reaction is accelerated by electron-donor substituents at 4-position of benzamidoxime and by electron-acceptor substituents at 4-position of benzoyl. The dependence of the rate constants vs σ values of the substituents fulfils the two-parameter Hammett equation at a 99% probability level. The activation parameters have been determined, and effects of polarity of medium, kinetic isotopic effect, and the reaction mechanism are discussed.. ...
The synthesis and evaluation of structural analogues and isosteres are of central importance in medicinal and agricultural chemistry. The sulfonamide functional group represents one of the most important amide isosteres in contemporary drug design, and about 500 such compounds have overcome both the pharmacological and regulatory hurdles that precede studies in humans. The mono aza analogues of sulfonamides, that is, sulfonimidamides, are rapidly gaining popularity as a novel functional group among synthetic chemists involved in the design of biologically active compounds for both pharmaceutical and agrochemical applications. Herein, we review these recent developments to showcase the promise of this functional group.. ...
Looking for online definition of amidine in the Medical Dictionary? amidine explanation free. What is amidine? Meaning of amidine medical term. What does amidine mean?
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Microwave reactions of primary and secondary amines with imidoylbenzotriazoles 6a-w gave diversely substituted amidines 7a-Aa in 76-94% yields. Convenient preparations of a variety of amides 5a-Ab (87-96%) and imidoylbenzotriazoles 6a-w (56-95%) have also been developed using microwave irradiation under mild conditions and short reaction times. These results demonstrate further the advantages of microwave synthesis and introduce a new application of imidoylbenzotriazoles in the preparation of polysubstituted amidines.
In order to evaluate performs of lightly cross-linked highly porous amidoxime resins in uranium-adsorption systems utilizing natural seawater motions, uranium uptake by the resins from seawater was studied by different approaches, such as simulated sea current exposure tests, towing trials, and/or mooring trials. In general, the efficiency of uranium uptake became higher with a decrease in the thickness of packing layers, indicating important roles of fluidization of the resin particles. On the basis of these fundamental data, mooring tests in the natural sea current were designed and conducted. By mooring flat adsorption beds (base area 260 cm2, height 3.0 cm) packed with 780 mL of the resin for 40 h, promising uranium uptake as high as 44 mg/kg of resin (9.9 mg/L of resin) was achieved under sea conditions in which the velocity of sea currents and the vertical velocity of waves were 5.5-49.7 cm/s and 3.4-27 cm/s, respectively. ...
Sigma-Aldrich offers abstracts and full-text articles by [Yang Liu, Catharine J Collar, Arvind Kumar, Chad E Stephens, David W Boykin, W David Wilson].
Grundy, Joanna, Coles, Martyn P and Hitchcock, Peter B (2004) Ambiphilic Ligands from the 1,4-benzenebis(amidine) Framework. New Journal of Chemistry, 28 (10). 1195 - 1197. ISSN 1144-0546 Full text not available from this repository ...
Ikigori (ubuke: Ibigori ; izina ryubumenyi mu kilatini Zea mays ; izina mu cyongereza: Maize cyangwa Corn ; izina mu gifaransa: Maïs ) ni ikimera nikiribwa. Abahinzi bo mu murenge wa Gashali ho mu Karere ka Karongi mu ntara yiburengerazuba, bararira ayo kwarika kubera ko imbuto yindobanure yibigori bateye mbere itabashije kuva mu butaka kubera imvura yabaye nkeya muri ako gace ko mu cyahoze ari Superefegitura ya Birambo. Twibutse ko intungamubiri ziri mu bigori ubariye ku magarama 100 ari izi zikurikira : amazi angana na garama 10,3. Garama 362 za kalisiyumu, Karoli muri garama 100 zingana na 8,1. Harimo kandi amagarama 76,9 byibinyasukari, gararama 3,6 bya Lipide, gr 6,16 bya Vitamine A, 0,385 bya vitamine B1 NA Miligarama 0,201 za B2, miligarama 3,632 za vitamine B3 na PP, Miligarama 241 za acide gras, miligarama 304 zumunyu ngugu na7,3 gr za Fibre, 6gr zumunyu ngugu wa Feri, 3,5garama za Potasiyumu, 2,87 garama za manyeziyumu, 127gr za sodiyumu na 35garama za fosifori. Ikigori ni ...
DB 185 is a dicationic aromatic compound related to pentamidine with a broad spectrum and potent fungicidal activity against many species of fungus, including
The new dicationic dinuclear complexes [Ni(μ-Cl)2(N,OH)2]Cl2 (11, N,OH = 2-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)-propan-2-ol; 12, N,OH ...
Enterokinase siRNA (h), shRNA and Lentiviral Particle Gene Silencers are designed to knockdown gene expression of human Enterokinase
Amphiphilic dicationic surfactants, known as gemini surfactants, are currently studied for gene delivery purposes. The gemini surfactant molecule is composed of two hydrophilic
Eleven compounds of substituted 4-(5-arylthiophen-2-yl)benzamidines 4a-k were synthesized from their corresponding mononitriles via treatment with lithium trimethylsilylamide and subsequent de-protection with ethanol/hydrogen chloride. In vitro antiproliferative activities of the new monocationic arylthiophenes were evaluated against 60 human cell lines at NCI, USA. This class of compounds displayed promising submicromolar antiproliferative activities with the most potent compound being 4i (GI and TGI of 0.20 and 0.37 M, respectively). On the other hand, most of the tested compounds exhibited LC at concentrations much higher than those they had GI at; ∼10 (for 4b) up to 228 (for 4e) which indicates lower lethality and efficient growth inhibition. Cancer cell lines, HCC-2998 colon, SNB-75 CNS, MDA-MB-435 melanoma, and MCF-7 breast cancer were the most responsive, with GI of 0.156, 0.165, 0.163, and 0.168 M, respectively. The p-chlorophenyl derivatives 4e and 4i discerned themselves with GI ...
Hello, Im reading the book: The Natural Way of Farming: The Theory and Practice of Green Philosophy (Masanobu Fukuoka) Mr. Fukuoka does not plow or a
Corresponding author. Mailing address: Institute of Biomedical and Life Sciences, Division of Infection and Immunity, Joseph Black Building, University of Glasgow, Glasgow G12 8QQ, United Kingdom. Phone and fax: 44-141-3303753. E-mail: H.de-Koning{at}bio.gla.ac.uk ...
My wife and I started gardening in Fukuoka (Japan) in 2003. There was nothing but muddy clayey sloping land. At the beginning we made several structure such as steps and paths, and planted turf, fruit trees, roses, herbs etc. In 2010, we visited several famous English gardens, including Sissinghurst Castle Garden, Mottisfont Abbey Garden and Hidcote Manor Garden. We were shocked by the glory of those gardens. Since then, we have been trying to make little but glorious gardens by ourselves. ...
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Usually imines refer to compounds with the connectivity R2C=NR, as discussed below. In the older literature, imine refers to the aza analogue of an epoxide. Thus, ethyleneimine is the three-membered ring species C2H4NH.[6]. Imines are related to ketones and aldehydes by replacement of the oxygen with an NR group. When R = H, the compound is a primary imine, when R is hydrocarbyl, the compound is a secondary imine. Imines exhibit diverse reactivity and are commonly encountered throughout chemistry.[4] When R3 is OH, the imine is called an oxime, and when R3 is NH2 the imine is called a hydrazone. A primary imine in which C is attached to both a hydrocarbyl and a H is called a primary aldimine; a secondary imine with such groups is called a secondary aldimine.[7] A primary imine in which C is attached to two hydrocarbyls is called a primary ketimine; a secondary imine with such groups is called a secondary ketimine .[8]. ...
Palladium-catalysed coupling between aryl- or heteroaryl-bromides, alkoxides, aryloxides or thioalkoxides. and isocyanides gives aryl-imidates and -thioimidates in high yield. Amidines can be synthesised in a one-pot procedure via imidates.. Full text not available from this repository.. ...
This milestone report summarizes the data obtained in FY16 on the major task of quantifying the binding strength of amidoxime-related ligands. Thermodynamic studies of the interaction between U(VI) and amidoxime ligand HL III were studied to quantify the binding ability of U(VI) with amidoxime-related ligands and help to select grafting/reaction conditions so that higher yield of preferred amidoxime-related ligands is obtained. Besides the thermodynamic task, structural studies on vanadium complexation with amidoxime ligand were conducted to help understand the extremely strong sorption of vanadium on poly(amidoxime) sorbents. Data processing and summarization of the vanadium system are in progress and will be included in the next milestone report. ...
Poster Presented at the 2012 American Thoracic Society (ATS) Conference Jun 4, 2012 - MiniVax, Inc. (MiniVax), a company focused on the development of novel tre
A broad range, bacterial, 100X concentrated, ready-to-use protease inhibitor cocktail of AEBSF, 1,10-Phenathroline, Benzamidine, Iodoacetamide, Pepstain A and PMSF that offers greater protection for recombinant proteins expressed and purified from bacteri
Glycans at the surface of cellular membranes modulate biological activity via multivalent association with extracellular messengers. The lack of tuneable simplified models mimicking this dynamic environment complicates basic studies of these phenomena. We here present a series of mixed reversible self-assembled monolayers (rSAMs) that addresses this deficiency. Mixed rSAMs were prepared in water by simple immersion of a negatively charged surface in a mixture of sialic acid- and hydroxy-terminated benzamidine amphiphiles. Surface compositions derived from infrared reflection-absorption spectroscopy (IRAS) and film thickness information (atomic force microscopy, ellipsometry) suggest the latter to be statistically incorporated in the monolayer. These surfaces affinity for the lectin hemagglutinin revealed a strong dependence of the affinity on the presentation, density, and mobility of the sialic acid ligands. Hence, a spacer length of 4 ethylene glycol and a surface density of 15% resulted in a ...
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This is over a week late, but Ive been crazy busy. During all the mayhem, I was able to squeeze in one showing of MOON SAGA~Yoshitsune Hiden~ and one visit to the GACKT X KIMONO Project exhibit. I went to the kimono exhibit on Tuesday the 14th with two friends. Admittedly, I only went to…
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Wow! LRC Norways Sondre Moen Makes History, Smashes European Record To Win Fukuoka In 2:05:48 Moen, who ran 59:48 during his buildup, became the first non-African born male to break 2:06 on a record-eligible course as he stunned the world and Bedan Karoki. 2012 Olympic champ Stephen Kiprotich grabbed second in 2:07:10 just ahead of the Suguro Osako, who set a new Nike Oregon Project record of 2:07:19.. ...
Researchers in Italy have used Peptest to investigate if pepsin causes worsening of symptoms for patients with chronic cough & chronic respiratory disease.
A comparative study on the inhibition of bovine beta-trypsin by bis-benzamidines diminazene and pentamidine by X-ray ... A comparative study on the inhibition of bovine beta-trypsin by bis-benzamidines diminazene and pentamidine by X-ray ...
Benzamidines / chemistry * Benzamidines / metabolism * Benzamidines / pharmacokinetics* * Cations * DNA / metabolism * ...
0 (Benzamidines); 0 (Ophthalmic Solutions); 7T9IJ84C42 (propamidine isethionate); R4KO0DY52L (Chlorhexidine). [Em] M s de ... 0 (Benzamidines); 0 (Biomarkers, Tumor); 0 (LCN2 protein, human); 0 (Lipocalin-2); 9005-49-6 (Heparin); EC 3.4.- (Serine ... Eleven compounds of substituted 4-(5-arylthiophen-2-yl)benzamidines 4a-k were synthesized from their corresponding mononitriles ... 0 (Amino Acid Chloromethyl Ketones); 0 (Benzamidines); 0 (Caspase Inhibitors); 0 (Macrolides); 0 (Reactive Oxygen Species); 0 ( ...
"Hydrogen Bonding Basicity of Acetamidines and Benzamidines.". *. 21. Exner O., Budešínský M., Hnyk D., Všetecka V., Raczyńska E ...
Talhout, R. & Engberts, J.B.F.N. Thermodynamic analysis of binding of p-substituted benzamidines to trypsin. European Journal ...
Cyclic benzamidines as orally efficacious NR2B-selective NMDA receptor antagonists. Kevin T Nguyen. Department of Medicinal ... Cyclic benzamidines as orally efficacious NR2B-selective NMDA receptor antagonists. Kevin T Nguyen. Department of Medicinal ... A novel series of cyclic benzamidines was synthesized and shown to exhibit NR2B-subtype selective NMDA antagonist activity. ...
A comparative study on the inhibition of bovine beta-trypsin by bis-benzamidines diminazene and pentamidine by X-ray ... A comparative study on the inhibition of bovine beta-trypsin by bis-benzamidines diminazene and pentamidine by X-ray ...
Improved process for the preparation of salts of 4- (benzimidazolylmethylamino) -benzamidines EP1956018A1 (en) 2007-02-06. 2008 ...
Ru(II)-Catalyzed annulation of benzamidines and alkynes by C-H/N-H activation: a facile synthesis of 1-aminoisoquinolines. P. P ...
... benzamidines, isothiazolines, phthalimide derivatives, pyridine derivatives, antimicrobial surface-active compounds, guanidines ...
ReVO and ReVNPh complexes with pentadentate benzamidines - Synthesis, structural characterization and DFT valuation of isomeric ...
Benzamidines, Diabetes Mellitus, Stents, Platelet Glycoprotein GPIIb-IIIa Complex ...
Compounds included non-ionic, anionic, and cationic surface-acting agents, amines, guanidines, benzamidines, thioureas, ...
... benzamidines, pyridinones and derivatives thereof. Other scaffolds are described in, for example, Klebe, G., J. Mol. Med. 78: ...
Thomas, M., Luetchford, K., Lima, N. A., Pinheiro De Lucena-Thomas, J., Fraser, E., Badder, L. M., Hollins, A. J., Chaudhuri, J., Dale, T. C. & Ellis, M., 1 Mar 2017.. Research output: Contribution to conference › Poster ...
Studies on the DNA Duplex Adducts of Anti-cancer agents by High Field NMR. The central target of my research is aimed at determining the molecular basis for the anti-tumour activity of DNA interactive anti-cancer ligands. It is hoped that we will be able relate the structural changes in local DNA structure which are induced or entrapped by these ligands to the biochemical and biological effects and incorporate these findings into the design of future DNA interactive anti-cancer ligands.. A number of methods are available to study the structure and nature of ligand-DNA adducts, these include X-ray diffraction, high-field NMR, circular dichroism, Raman spectroscopy, UV, IR, gel electrophoresis and enzymatic probes. My research has concentrated on the use of high-field NMR coupled with molecular modelling to closely study the duplex adducts formed in the reactions of DNA alkylating ligands and DNA duplexes.. High field NMR studies are performed on the in-house Varian 600MHz and 400Mhz NMR ...
Edelmann, "N-silylated benzamidines: versatile building blocks in main group and coordination chemistry," Coordination ...
DMF was the superior solvent for the N-arylation of benzamidines, while MeCN was used in the formation of N-aryl amidines in ...
... benzamidines hydrochloride under metal-free and peroxide-free conditions.. X. Wu, Q. Gao, S. Liu, A. Wu, Org. Lett., 2014, 16, ...
Humans , Receptors, GABA-A/chemistry , Binding Sites , Benzamidines/chemistry , Benzamidines/metabolism , Benzamidines/ ... Benzamidines/metabolism , Trypsin/metabolism , Benzamidines/chemistry , Binding Sites , Chromatography, Affinity , Mathematics ... Benzamidines/metabolism , Spectrophotometry, Atomic , Thermodynamics , Trypsin/metabolism , Protein Conformation , Trypsin ...
Benzamidines/therapeutic use. *Drug Therapy, Combination. *Eptifibatide. *Heparin, Low-Molecular-Weight/therapeutic use ...
Active site mapping of trypsin, thrombin and matriptase-2 by sulfamoyl benzamidines Keywords: پرویناین serine; Active site ...
Benzamidines [D02.078.100]. *Pentamidine [D02.078.100.700]. Below are MeSH descriptors whose meaning is related to "Pentamidine ...
Humans , Receptors, GABA-A/chemistry , Binding Sites , Benzamidines/chemistry , Benzamidines/metabolism , Benzamidines/ ... Benzamidines/metabolism , Trypsin/metabolism , Benzamidines/chemistry , Binding Sites , Chromatography, Affinity , Mathematics ... Animals , Cattle , Benzamidines/chemistry , Diminazene/analogs & derivatives , Trypsin Inhibitors/chemistry , Trypsin/chemistry ...
D02.078.100 Benzamidines .. D02.078.100.700 Pentamidine .. D02.092 Amines .. D02.092.782 Polyamines .. D02.092.782.590 Pentetic ...
... as it could be argued was the case with benzamidines inhibition of kallikrein) deserves more attention (Walsh, Martin & ...
Occurrence of 3D isostructurality in fluorinated phenyl benzamidines Details. CrystEngComm 2017. Deepak Chopra Dhananjay Dey ...
Optimization of cyclic plasmin inhibitors: from benzamidines to benzylamines. J Med Chem ...
Examples of the latter compounds include the benzamidines, which block C1, C4 and C5 utilization (see, e.g., Vogt et al. ... Academic Press, New York, p. 65); and benzamidines (Vogt, W. et al Immunology 1979, 36, 138). Some of these agents function by ...
  • DMF was the superior solvent for the N -arylation of benzamidines, while MeCN was used in the formation of N -aryl amidines in good yield. (organic-chemistry.org)
  • An iodine-catalyzed oxidative C-H/N-H cross-coupling enables an efficient construction of α-ketoimides in good to excellent yields from methyl ketones and benzamidines hydrochloride under metal-free and peroxide-free conditions. (organic-chemistry.org)

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