A REVIEW ON CURRENT INDUSTRIAL TRENDS FOR SYNTHESIS OF MEDICINAL... Review Article SMITA JAIN, I.G. RATHISH, R. SANKARAN*
... starting point for drug discovery [29]. Library construction is somewhat typical in this approach as it includes known ligands of at least one and preferably several members of the target family. Since a portion of ligands that were designed and synthesized to bind to one family member will also bin ...
... starting point for drug discovery [29]. Library construction is somewhat typical in this approach as it includes known ligands of at least one and preferably several members of the target family. Since a portion of ligands that were designed and synthesized to bind to one family member will also bin ...
Rifampicin Antagonizes the Effect of Chloroquine on Chloroquine
... food vacuole. However, this postulation is unable to explain how verapamil and other reversal agents are able to increase CQ inside the food vacuole and counter resistance. Another factor to consider is the fact that RIF is a known CYP3A4 inducer, which is documented to affect metabolism of quinine ...
... food vacuole. However, this postulation is unable to explain how verapamil and other reversal agents are able to increase CQ inside the food vacuole and counter resistance. Another factor to consider is the fact that RIF is a known CYP3A4 inducer, which is documented to affect metabolism of quinine ...
Simon Chiu and others(1981)11dec7
... Our studies demonstrate the antagoSimultaneous administration of PLG manic depression may be related to its nism of neuroleptic-induced dopamine with haloperidol or chlorpromazine, ability to stabilize the oscillations of doreceptor supersensitivity by the neurohowever, antagonized the elevation in ...
... Our studies demonstrate the antagoSimultaneous administration of PLG manic depression may be related to its nism of neuroleptic-induced dopamine with haloperidol or chlorpromazine, ability to stabilize the oscillations of doreceptor supersensitivity by the neurohowever, antagonized the elevation in ...
Laboratory Testing for HIV Tropism
... Maraviroc (Selzentry™, Pfizer) is the first coreceptor antagonist to be approved by FDA. Maraviroc is a selective, slowly reversible, small-molecule antagonist of the interaction between human cell surface CCR5 and HIV-1 gp120, also necessary for HIV-1 cell infection. Blocking this interaction preve ...
... Maraviroc (Selzentry™, Pfizer) is the first coreceptor antagonist to be approved by FDA. Maraviroc is a selective, slowly reversible, small-molecule antagonist of the interaction between human cell surface CCR5 and HIV-1 gp120, also necessary for HIV-1 cell infection. Blocking this interaction preve ...
A New Approach to Drug Discovery and Development
... of several compounds into clinical trials.3 Early clinical ...
... of several compounds into clinical trials.3 Early clinical ...
B-lactam antibiotics
... this group of antibiotics is derived from its complex structure, which includes in the molecules • Macrocycle lacton ring, • one or more deoxysugars. The lactone rings are usually 14, 15 or 16-membered. ...
... this group of antibiotics is derived from its complex structure, which includes in the molecules • Macrocycle lacton ring, • one or more deoxysugars. The lactone rings are usually 14, 15 or 16-membered. ...
Original article Anti-hepatitis B virus activity in vitro of combinations
... LdT is an l-nucleoside analogue of thymidine and has been shown to be more efficacious than 3TC at reducing serum HBV DNA in clinical trials [10]. However, its long-term usage also resulted in virological breakthrough from rtM204V and rtM204I mutations [10]. ETV, a deoxyguanosine analogue, has parti ...
... LdT is an l-nucleoside analogue of thymidine and has been shown to be more efficacious than 3TC at reducing serum HBV DNA in clinical trials [10]. However, its long-term usage also resulted in virological breakthrough from rtM204V and rtM204I mutations [10]. ETV, a deoxyguanosine analogue, has parti ...
Open PDF File - Array BioPharma
... Literature compounds with a greater than 10-fold preference for AAG demonstrated a greater than three-fold decrease in the free fraction with increasing AAG levels: ritonavir, imatinib, nelfinavir, docetaxel, chlorpromazine, imipramine, erythromycin, and propranolol. Test compounds that had a modera ...
... Literature compounds with a greater than 10-fold preference for AAG demonstrated a greater than three-fold decrease in the free fraction with increasing AAG levels: ritonavir, imatinib, nelfinavir, docetaxel, chlorpromazine, imipramine, erythromycin, and propranolol. Test compounds that had a modera ...
Molecular determinants of drug–receptor binding kinetics
... to be influenced more by short-range drug–receptor interactions such as hydrogen bonds, salt bridges and van der Waals (especially hydrophobic) contacts [22,23]. Binding of a charged acetylcholinesterase inhibitor, for instance, was 50-fold faster, and unbinding 10-fold slower, than that of a near ...
... to be influenced more by short-range drug–receptor interactions such as hydrogen bonds, salt bridges and van der Waals (especially hydrophobic) contacts [22,23]. Binding of a charged acetylcholinesterase inhibitor, for instance, was 50-fold faster, and unbinding 10-fold slower, than that of a near ...
Introduction to Fragment-Based Drug Discovery
... people to refer to “fragment-assisted drug discovery,” in which information from fragments is applied to more traditional drug discovery programs [12]. In addition to covering chemical space more efficiently, the hit rate for screening smaller compounds should in theory be higher than for larger com ...
... people to refer to “fragment-assisted drug discovery,” in which information from fragments is applied to more traditional drug discovery programs [12]. In addition to covering chemical space more efficiently, the hit rate for screening smaller compounds should in theory be higher than for larger com ...
Articles - The Vespiary
... somewhat offset by the more effective hydrogen-bonding of the constrained heterocyclic oxygens) would enhance their in vivo activity. Nevertheless, in the behavioral assays, the rank order of potency for this series decreased with increasing molecular hydrophobicity. In view of the somewhat greater ...
... somewhat offset by the more effective hydrogen-bonding of the constrained heterocyclic oxygens) would enhance their in vivo activity. Nevertheless, in the behavioral assays, the rank order of potency for this series decreased with increasing molecular hydrophobicity. In view of the somewhat greater ...
Product Information: Elvitegravir
... CLINICAL TRIALS The efficacy of VITEKTA is primarily based on the analyses through 96 weeks from one randomized, double-blind, active-controlled study, Study 0145, in treatment experienced, HIV-1 infected patients (N=702). In Study 0145, patients were randomized in a 1:1 ratio to receive either VITE ...
... CLINICAL TRIALS The efficacy of VITEKTA is primarily based on the analyses through 96 weeks from one randomized, double-blind, active-controlled study, Study 0145, in treatment experienced, HIV-1 infected patients (N=702). In Study 0145, patients were randomized in a 1:1 ratio to receive either VITE ...
Drug Discovery Strategies Today
... A series of measurements ranging from genetic/genomic through to clinical are made and a comparison between normal versus perturbed (eg diseased/drug treated/toxin administration) populations is performed. Complex datasets are integrated and a variety of informatic, biostatistical and knowledge asse ...
... A series of measurements ranging from genetic/genomic through to clinical are made and a comparison between normal versus perturbed (eg diseased/drug treated/toxin administration) populations is performed. Complex datasets are integrated and a variety of informatic, biostatistical and knowledge asse ...
Antifungal Pharmacology - LSU School of Medicine
... Molecular Aspects • FKS1 encodes glucan synthase • GNS1 encodes an enzyme involved in fatty acid elongation • Resistance is observed following laboratory derived mutations in FKS1 or GNS1 • Other mechanisms (?) ...
... Molecular Aspects • FKS1 encodes glucan synthase • GNS1 encodes an enzyme involved in fatty acid elongation • Resistance is observed following laboratory derived mutations in FKS1 or GNS1 • Other mechanisms (?) ...
Computer-Aided Drug Design of Bioactive Natural Products (PDF
... approaches have become versatile tools for facilitating and accelerating drug design and development [44, 45]. The conceptual framework of drug discovery and development and the roles of computational approaches in each step are illustrated in (Fig. 1). Target identification is the process in which ...
... approaches have become versatile tools for facilitating and accelerating drug design and development [44, 45]. The conceptual framework of drug discovery and development and the roles of computational approaches in each step are illustrated in (Fig. 1). Target identification is the process in which ...
Study of the Pepsin Enzymatic Activity in in
... edition Brazilian Pharmacopoeia, monograph no. 180.1 from ANVISA. Vankel VK 7000, apparatus 2 (paddle), temperature of 37.0 °C and stirring speed of 50 rpm were used. The dissolution medium was simulated gastric fluid with pepsin, which was prepared with 2 g of sodium chloride, varying concentration ...
... edition Brazilian Pharmacopoeia, monograph no. 180.1 from ANVISA. Vankel VK 7000, apparatus 2 (paddle), temperature of 37.0 °C and stirring speed of 50 rpm were used. The dissolution medium was simulated gastric fluid with pepsin, which was prepared with 2 g of sodium chloride, varying concentration ...
Rx FACTS October 2003
... Desogestrel - ethinyl estradiol 0.15-0.03 mg Drospirenone - ethinyl estradiol 3.0-0.3 mg Ethynodiol - ethinyl estradiol 1-0.035 mg Ethynodiol - ethinyl estradiol 1-0.05 mg Levonorgestrel - ethinyl estradiol 0.1-0.02 mg Levonorgestrel - ethinyl estradiol 0.15-0.03 mg Norethindrone - ethinyl estradiol ...
... Desogestrel - ethinyl estradiol 0.15-0.03 mg Drospirenone - ethinyl estradiol 3.0-0.3 mg Ethynodiol - ethinyl estradiol 1-0.035 mg Ethynodiol - ethinyl estradiol 1-0.05 mg Levonorgestrel - ethinyl estradiol 0.1-0.02 mg Levonorgestrel - ethinyl estradiol 0.15-0.03 mg Norethindrone - ethinyl estradiol ...
Psychology 472 Pharmacology of Psychoactive Drugs
... other compounds (salt) • Also removes other drugs and products • BCPs, Lithium, some hallucinogens, ...
... other compounds (salt) • Also removes other drugs and products • BCPs, Lithium, some hallucinogens, ...
Prevention of Antiviral-Resistant HBV - HAL
... compliance. Recently, it was suggested that virological factors may be involved as pre-existing mutations, i.e. rtI233V, were associated with primary non response to adefovir in 3 patients (12). Cross-resistance is defined as a mutation(s) that confers resistance to more than one antiviral drug by i ...
... compliance. Recently, it was suggested that virological factors may be involved as pre-existing mutations, i.e. rtI233V, were associated with primary non response to adefovir in 3 patients (12). Cross-resistance is defined as a mutation(s) that confers resistance to more than one antiviral drug by i ...
Natural Products Chemistry
... • The laxative action of the crude drugs is always higher than from their content of anthracene der. The different anthracene der. contained by the crude drug are said to exert a synergistic action. • Thus, the naturally occurring anthracene glycosides were found superior to the synthesis of numerou ...
... • The laxative action of the crude drugs is always higher than from their content of anthracene der. The different anthracene der. contained by the crude drug are said to exert a synergistic action. • Thus, the naturally occurring anthracene glycosides were found superior to the synthesis of numerou ...
Antimicrobial Agents
... • Mode of action - The aminoglycosides irreversibly bind to the 16S ribosomal RNA and freeze the 30S initiation complex (30S-mRNAtRNA) so that no further initiation can occur. They also slow down protein synthesis that has already initiated and induce misreading of the mRNA. By binding to the 16 S r ...
... • Mode of action - The aminoglycosides irreversibly bind to the 16S ribosomal RNA and freeze the 30S initiation complex (30S-mRNAtRNA) so that no further initiation can occur. They also slow down protein synthesis that has already initiated and induce misreading of the mRNA. By binding to the 16 S r ...
4-aminoquinolines as Antimalarial Drugs
... resistance to chloroquine was reported in all African countries, yet it remained as the first-choice treatment in many African countries into the early 2000s (Trape ,2001). As no effective malarial vaccines are yet available, health services rely on drugs for treatment and prophylaxis, however effic ...
... resistance to chloroquine was reported in all African countries, yet it remained as the first-choice treatment in many African countries into the early 2000s (Trape ,2001). As no effective malarial vaccines are yet available, health services rely on drugs for treatment and prophylaxis, however effic ...
urinary tract infections associated with multidrug resistant enteric
... streptomycin, tetracycline and chloramphenicol was also significant as 30%, 29% and 27% isolates resisted upto 500µg/mL of these drugs respectively. Resistance to gentamicin (21%) and kanamycin (16%) at 500µg/mL was less significant. Most of the isolates were found sensitive to fosfomycin even at lo ...
... streptomycin, tetracycline and chloramphenicol was also significant as 30%, 29% and 27% isolates resisted upto 500µg/mL of these drugs respectively. Resistance to gentamicin (21%) and kanamycin (16%) at 500µg/mL was less significant. Most of the isolates were found sensitive to fosfomycin even at lo ...
Available
... To guide the progress of disease To identify patients supersensitive to drug 5. Phenobarbital increases metabolism of warfarin and phenytoin, steroid hormones Phenytoin increases metabolism of meperidine Rifampine and phenytoin increase metabolism of propranolol Disulfiram inhibits metabolism of al ...
... To guide the progress of disease To identify patients supersensitive to drug 5. Phenobarbital increases metabolism of warfarin and phenytoin, steroid hormones Phenytoin increases metabolism of meperidine Rifampine and phenytoin increase metabolism of propranolol Disulfiram inhibits metabolism of al ...
EXPLORING THE EFFECTS OF NEWER THREE COMPONENT AMINOBENZYLATED REACTIONS OF TRIPHENYL IMIDAZOLE MOTIF AS POTENT ANTIMICROBIAL AND ANTIINFLAMMATORY
... synthesized scaffolds elicits mild to good activity against gram positive, gram‐negative bacterial strains and fungal strains at a concentration of 250 µg/ml. Anti‐inflammatory activity revealed that all the synthesized entities showed significant activity when compared with that ...
... synthesized scaffolds elicits mild to good activity against gram positive, gram‐negative bacterial strains and fungal strains at a concentration of 250 µg/ml. Anti‐inflammatory activity revealed that all the synthesized entities showed significant activity when compared with that ...
Discovery and development of non-nucleoside reverse-transcriptase inhibitors
Non-nucleoside reverse-transcriptase inhibitors (NNRTIs) are antiretroviral drugs used in the treatment of human immunodeficiency virus (HIV). NNRTIs inhibit reverse transcriptase (RT), an enzyme that controls the replication of the genetic material of HIV. RT is one of the most popular targets in the field of antiretroviral drug development.Discovery and development of NNRTIs began in the late 1980s and in the end of 2009 four NNRTI had been approved by regulatory authorities and several others were undergoing clinical development. Drug resistance develops quickly if NNRTIs are administered as monotherapy and therefore NNRTIs are always given as part of combination therapy, the highly active antiretroviral therapy (HAART).