... [25]. PDE4 inhibitors are effective in inhibiting microvascular leakage induced by a variety of proinflammatory mediators [26]. There is also evidence that, as well as enhancing nonadrenergic noncholinergic (NANC) relaxation [27], PDE4 inhibitors may have direct bronchodilatory effects [28, 29]. No ...
Synopsis of Some Recent Tactical Application of Bioisosteres in
... 3.1.7. Deploying Fluorine To Modulate Basicity in KSP Inhibitors. The high electronegativity of F reduces the basicity of proximal amines while increasing the acidity of acids (data summarized quantitatively in Table 4).43 The strategic deployment of a fluorine atom to modulate basicity was probed i ...
... 3.1.7. Deploying Fluorine To Modulate Basicity in KSP Inhibitors. The high electronegativity of F reduces the basicity of proximal amines while increasing the acidity of acids (data summarized quantitatively in Table 4).43 The strategic deployment of a fluorine atom to modulate basicity was probed i ...
Selective Inhibition of Brain Na,K-ATPase by Drugs
... sedative (diazepam) and antihistaminic (promethazine) drugs on Na,K-ATPase activity of plasma membranes was studied in rat brain synaptosomes. Methyldigoxin in a concentration of 0.1 mmol/l inhibits enzyme activity by 80 %. Verapamil, propranolol and promethazine in concentrations of 20, 20 and 2 mm ...
... sedative (diazepam) and antihistaminic (promethazine) drugs on Na,K-ATPase activity of plasma membranes was studied in rat brain synaptosomes. Methyldigoxin in a concentration of 0.1 mmol/l inhibits enzyme activity by 80 %. Verapamil, propranolol and promethazine in concentrations of 20, 20 and 2 mm ...
Identification of GZD824 as an Orally Bioavailable Inhibitor That
... investigate the potential impact of R1 and R2 on Abl kinase inhibition (Table 1). Although many studies have demonstrated that the “flag-methyl” group at the R2 position is critical for compound 1 and many other Bcr-Abl inhibitors to maintain their kinase inhibition, compound 10b, in which the methyl ...
... investigate the potential impact of R1 and R2 on Abl kinase inhibition (Table 1). Although many studies have demonstrated that the “flag-methyl” group at the R2 position is critical for compound 1 and many other Bcr-Abl inhibitors to maintain their kinase inhibition, compound 10b, in which the methyl ...
Anti-platelet agents
... • May potentiate the action of aspirin in preventing strokes in patients ...
... • May potentiate the action of aspirin in preventing strokes in patients ...
Perspectives and challenges of interferon-free therapy for chronic hepatitis C Zeuzem
... [31]. Very promising clinical data have been recently published for sofosbuvir (GS-7977), another NI effective against all HCV genotypes. In HCV genotype 1, 2, and 3 infected patients, short durations of sofosbuvir-based triple therapy resulted in SVR rates of 90–100% [32,33]. These data indicate th ...
... [31]. Very promising clinical data have been recently published for sofosbuvir (GS-7977), another NI effective against all HCV genotypes. In HCV genotype 1, 2, and 3 infected patients, short durations of sofosbuvir-based triple therapy resulted in SVR rates of 90–100% [32,33]. These data indicate th ...
Nicotinamide adenine dinucleotide metabolism as an
... significant structural differences among the enzymes. These include a movement of a β-strand by ∼ 2 Å and the replacement of several small residues in the tunnel in NMPRTase by larger residues in the other two PRTases. In fact, single-site mutations in the tunnel of NMPRTase can abolish the binding ...
... significant structural differences among the enzymes. These include a movement of a β-strand by ∼ 2 Å and the replacement of several small residues in the tunnel in NMPRTase by larger residues in the other two PRTases. In fact, single-site mutations in the tunnel of NMPRTase can abolish the binding ...
042299 Antiviral Drugs
... LEVEN drugs approved by the Food and Drug Administration for the treatment of viral infections (other than those caused by human immunodeficiency virus type 1 [HIV-1] or those complicating such infection) will be reviewed in this article. They are seven nucleoside analogues, two closely related 10-c ...
... LEVEN drugs approved by the Food and Drug Administration for the treatment of viral infections (other than those caused by human immunodeficiency virus type 1 [HIV-1] or those complicating such infection) will be reviewed in this article. They are seven nucleoside analogues, two closely related 10-c ...
Multi-Choice Questions: Analgesia Toxicology and
... E: L-Penicillamine frequently causes pyridoxine deficiency. Q10: A primarily bacteriostatic antibiotic is. A: Metronidazole B: Chloramphenicol C: Penicillin D: Vancomycin E: Gentamicin Q11: If penicillin together with tetracycline is tested for synergy and is found in combination to achieve MIC at 3 ...
... E: L-Penicillamine frequently causes pyridoxine deficiency. Q10: A primarily bacteriostatic antibiotic is. A: Metronidazole B: Chloramphenicol C: Penicillin D: Vancomycin E: Gentamicin Q11: If penicillin together with tetracycline is tested for synergy and is found in combination to achieve MIC at 3 ...
R E V I E W A R T I... Quinolones in 2005: an update
... Second-step resistance mutations may then accumulate in the secondary drug target enzymes and will further affect quinolone resistance [51]. The precise effect of mutations in the gyrase and topoisomerase IV genes on the resistance phenotype may differ between bacterial species [52], but depends als ...
... Second-step resistance mutations may then accumulate in the secondary drug target enzymes and will further affect quinolone resistance [51]. The precise effect of mutations in the gyrase and topoisomerase IV genes on the resistance phenotype may differ between bacterial species [52], but depends als ...
(12)Indian Patent Application ______________________________________________________________
... provide an effective therapeutic treatment in immune-mediated diseases, e.g. intestinal disorders, such as autoimmune and inflammatory diseases or conditions. T lymphocyte (T cell) infiltration into the small intestine and colon has been linked specifically to the pathogenesis of Coeliac diseases, f ...
... provide an effective therapeutic treatment in immune-mediated diseases, e.g. intestinal disorders, such as autoimmune and inflammatory diseases or conditions. T lymphocyte (T cell) infiltration into the small intestine and colon has been linked specifically to the pathogenesis of Coeliac diseases, f ...
In Vitro Metabolism of Quinidine: The (3S)-3
... did not possess any inhibitory potential toward the two reactions when introduced in concentrations up to 100 mM: prednisone, prednisolone, estradiol, citalopram, desmethylcitalopram, dapsone, flucytosine, cocaine, metronidazole, naringin, and triazolam. None of the 10 following isozyme specific inh ...
... did not possess any inhibitory potential toward the two reactions when introduced in concentrations up to 100 mM: prednisone, prednisolone, estradiol, citalopram, desmethylcitalopram, dapsone, flucytosine, cocaine, metronidazole, naringin, and triazolam. None of the 10 following isozyme specific inh ...
LETTERS
... To the Editor: The meta-analysis by Dr Mukherjee and colleagues1 compared the risk of MI of the selective COX-2 inhibitors rofecoxib and celecoxib from data2,3 reported to the US Food and Drug Administration with that of placebo from a meta-analysis of aspirin for primary prevention.4 The results of ...
... To the Editor: The meta-analysis by Dr Mukherjee and colleagues1 compared the risk of MI of the selective COX-2 inhibitors rofecoxib and celecoxib from data2,3 reported to the US Food and Drug Administration with that of placebo from a meta-analysis of aspirin for primary prevention.4 The results of ...
Nano-vectors for the Ocular Delivery of Nucleic Acid
... AS-ODNs are synthetic molecules composed of 13 to about 25 nucleotides, which are complementary to mRNA strands in a region of a coding sequence designed as sense strand [1]. They bind to specific intracellular mRNA strands and stop translation of the mRNA, and hence synthesis of protein expressed b ...
... AS-ODNs are synthetic molecules composed of 13 to about 25 nucleotides, which are complementary to mRNA strands in a region of a coding sequence designed as sense strand [1]. They bind to specific intracellular mRNA strands and stop translation of the mRNA, and hence synthesis of protein expressed b ...
The Influence of Conformational Isomerism on Drug
... make specific agonists or antagonists, to eliminate toxic or unnecessary effects, and to increase the duration of action. In addition, it can be used to improve the understanding of specific drug-receptor interactions. In cases where a drug binds to only one receptor, there are still some advantages ...
... make specific agonists or antagonists, to eliminate toxic or unnecessary effects, and to increase the duration of action. In addition, it can be used to improve the understanding of specific drug-receptor interactions. In cases where a drug binds to only one receptor, there are still some advantages ...
Revised: November 2014 AN: 00887/2014 SUMMARY OF
... The safety of the product has not been established in pigs or calves when administered by the intravenous route and use of this route of administration is not recommended in these animal groups. Use of the product should be based on susceptibility testing and take into account official and local ant ...
... The safety of the product has not been established in pigs or calves when administered by the intravenous route and use of this route of administration is not recommended in these animal groups. Use of the product should be based on susceptibility testing and take into account official and local ant ...
Interactions between Acid-Reducing Agents and Antiretrovirals
... simultaneously or 10 hours after H2RA. Maximum famotidine 40 mg BID (treatmentnaïve) or 20 mg BID (treatment-experienced). If also on tenofovir, ↑ to ATV 400/100 mg QD in experienced patients. ...
... simultaneously or 10 hours after H2RA. Maximum famotidine 40 mg BID (treatmentnaïve) or 20 mg BID (treatment-experienced). If also on tenofovir, ↑ to ATV 400/100 mg QD in experienced patients. ...
Role of cytochrome P450 in drug interactions | SpringerLink
... A notice has been published about this article. See full information at: http://www.nutritionandmetabolism.com/content/5/1/27 ...
... A notice has been published about this article. See full information at: http://www.nutritionandmetabolism.com/content/5/1/27 ...
Naltrexone potentiates anti-HIV-1 activity of antiretroviral drugs in
... The introduction of highly active antiretroviral therapy, i.e. triple combination therapy that includes a protease inhibitor, has had a dramatic clinical benefit for many patients infected with human immunodeficiency virus-1 (HIV-1) (The CASCADE Collaboration, 2000; Fauci, 1999). However, a substant ...
... The introduction of highly active antiretroviral therapy, i.e. triple combination therapy that includes a protease inhibitor, has had a dramatic clinical benefit for many patients infected with human immunodeficiency virus-1 (HIV-1) (The CASCADE Collaboration, 2000; Fauci, 1999). However, a substant ...
Drugs for Parkinson`s disease
... A selective inhibitor of MAO-B, which predominates in DA-containing regions of the CNS and lacks unwanted peripheral effects of non-selective MAO inhibitors. ...
... A selective inhibitor of MAO-B, which predominates in DA-containing regions of the CNS and lacks unwanted peripheral effects of non-selective MAO inhibitors. ...
The mechanism of action of aspirin
... pigs. The purpose was to detect substances released during the anaphylactic reaction, including histamine and SRS-A, both of which had been known for many years as possible mediators of anaphylaxis. They used the technique of continuous bioassay with the cascade bioassay system developed by Vane [8] ...
... pigs. The purpose was to detect substances released during the anaphylactic reaction, including histamine and SRS-A, both of which had been known for many years as possible mediators of anaphylaxis. They used the technique of continuous bioassay with the cascade bioassay system developed by Vane [8] ...
No Slide Title
... H-bond donor group at positions 3, 4,or 5 is good for activity Term = 1 if a HBD group is at any of these positions Term = 2 if HBD groups are at two of these positions Term = 0 if no HBD group is present at these positions Each HBD group increases activity by 0.39 Equals 1 if NHSO2 is present (bad ...
... H-bond donor group at positions 3, 4,or 5 is good for activity Term = 1 if a HBD group is at any of these positions Term = 2 if HBD groups are at two of these positions Term = 0 if no HBD group is present at these positions Each HBD group increases activity by 0.39 Equals 1 if NHSO2 is present (bad ...
a study of prescription pattern of non steroidal anti
... (36%) was the commonest drug prescribed. In general non-selective NSAIDs were more commonly prescribed (79.5%) and selective COX-2 inhibitors were least prescribed (1%). High prevalence of nimesulide prescription (19.5%) was a significant finding. Co-prescription of GPAs was high (61%). Four drugs ( ...
... (36%) was the commonest drug prescribed. In general non-selective NSAIDs were more commonly prescribed (79.5%) and selective COX-2 inhibitors were least prescribed (1%). High prevalence of nimesulide prescription (19.5%) was a significant finding. Co-prescription of GPAs was high (61%). Four drugs ( ...
