Structure-based design of hyaluronidase inhibitors
... Hyaluronic acid (hyaluronan), along with chondroitin-, keratan- and dermatane sulfate, heparin and heparan sulfate, is a member of the family of glycosaminoglycanes which are mostly linear polymers of high molecular weight composed of aminosugars (N-acetylglucosamine or N-acetylgalactosamine) and ur ...
... Hyaluronic acid (hyaluronan), along with chondroitin-, keratan- and dermatane sulfate, heparin and heparan sulfate, is a member of the family of glycosaminoglycanes which are mostly linear polymers of high molecular weight composed of aminosugars (N-acetylglucosamine or N-acetylgalactosamine) and ur ...
Potential Anti-HIV Activity of Jatropha curcas Linn. Leaf Extracts
... been found [9,10]. Although several studies have shown the antimicrobial activity, there are a very limited number of previous reports on the specific anti-HIV activity of Jatropha curcas Linn. One such study showed that Jatropha curcas Linn. had specific in vitro anti-RT enzyme activity and that th ...
... been found [9,10]. Although several studies have shown the antimicrobial activity, there are a very limited number of previous reports on the specific anti-HIV activity of Jatropha curcas Linn. One such study showed that Jatropha curcas Linn. had specific in vitro anti-RT enzyme activity and that th ...
Neuraminidase inhibitors as anti
... and hydrophobic interactions with NA. These two interactions help to anchor the scaffold of sialic acid, thus providing a structural frame for introducing additional interactions that would lead to more potent inhibitors. The NA active site can be further divided into three major binding pockets bas ...
... and hydrophobic interactions with NA. These two interactions help to anchor the scaffold of sialic acid, thus providing a structural frame for introducing additional interactions that would lead to more potent inhibitors. The NA active site can be further divided into three major binding pockets bas ...
The impact of polypharmacology on chemical biology Albert Antolín Hernández
... drug promiscuity and with ongoing academic efforts to rationally design multitarget drugs. Drug discovery is, slowly, becoming a more holistic endeavor. Unfortunately, this holistic perspective is not permeating to other disciplines. Since the 1990s, the field of chemical biology has emerged to use ...
... drug promiscuity and with ongoing academic efforts to rationally design multitarget drugs. Drug discovery is, slowly, becoming a more holistic endeavor. Unfortunately, this holistic perspective is not permeating to other disciplines. Since the 1990s, the field of chemical biology has emerged to use ...
carbapenam and monobactam - Home
... Meropenem is not hydrolyzed by DHP-I and is resistant to most β-lactamases, including a few carbapenemases that hydrolyze ...
... Meropenem is not hydrolyzed by DHP-I and is resistant to most β-lactamases, including a few carbapenemases that hydrolyze ...
Macrolids
... dosage reduction (eg, a 500-mg loading dose, then 250 mg once or twice daily) is recommended for patients with creatinine clearances less than 30 mL/min. Clarithromycin has drug interactions similar to erythromycin (can inhibit cytochrome P450 enzymes). The advantages of clarithromycin compared with ...
... dosage reduction (eg, a 500-mg loading dose, then 250 mg once or twice daily) is recommended for patients with creatinine clearances less than 30 mL/min. Clarithromycin has drug interactions similar to erythromycin (can inhibit cytochrome P450 enzymes). The advantages of clarithromycin compared with ...
Antiviral efficacy of nine nucleoside reverse transcriptase inhibitors
... susceptibility of FIV to many RT-targeted antiviral compounds used in the treatment of HIV-infected patients. The nucleoside reverse transcriptase inhibitor (NRTI) zidovudine is the only antiviral drug which has been evaluated thoroughly against FIV and is sometimes used in the treatment of naturall ...
... susceptibility of FIV to many RT-targeted antiviral compounds used in the treatment of HIV-infected patients. The nucleoside reverse transcriptase inhibitor (NRTI) zidovudine is the only antiviral drug which has been evaluated thoroughly against FIV and is sometimes used in the treatment of naturall ...
Clinical Trials - Ritonavir
... Phenotypic and genotypic changes in HIV isolates treated with ritonavir were monitored in phase I/II trials over a period of 3 to 32 weeks. The clinical relevance of phenotypic and genotypic changes associated with ritonavir therapy has not been established. Some HIV mutations were also found in pat ...
... Phenotypic and genotypic changes in HIV isolates treated with ritonavir were monitored in phase I/II trials over a period of 3 to 32 weeks. The clinical relevance of phenotypic and genotypic changes associated with ritonavir therapy has not been established. Some HIV mutations were also found in pat ...
Product Monograph Template - Standard
... CELSENTRI should be used with caution in patients with a history of cardiovascular disease or who are at risk for cardiovascular events. Cases of myocardial ischemia and myocardial infarction were reported in 11 subjects (1.3%) receiving CELSENTRI in Phase 3 studies in treatment-experienced studies ...
... CELSENTRI should be used with caution in patients with a history of cardiovascular disease or who are at risk for cardiovascular events. Cases of myocardial ischemia and myocardial infarction were reported in 11 subjects (1.3%) receiving CELSENTRI in Phase 3 studies in treatment-experienced studies ...
Bioisosterism: A Rational Approach in Drug Design
... electronic definition of classical isosteres. A second notable characteristic of nonclassical bioisosteres is that they do not have the same number of atoms as the substituent or moiety for which they are used as a replacement. Nonclassical bioisosteres can be further divided into groups: (A) rings ...
... electronic definition of classical isosteres. A second notable characteristic of nonclassical bioisosteres is that they do not have the same number of atoms as the substituent or moiety for which they are used as a replacement. Nonclassical bioisosteres can be further divided into groups: (A) rings ...
... isoniazid, rifampicin and pyrazinamide, is made after 2 months of treatment by either continuation with therapy with rifampicin, pyrazinamide and ethambutol for another 10 months, or with rifampicin and ethambutol for a minimal period of 12 months [59, 61, 62]. Secondly, no modification of the initi ...
Minireview Low-Turnover Drug Molecules: A Current Challenge for
... approach is well-established, it requires access to often intractable authentic metabolite standards for calibration curve generation, which is typically not supported until early human clinical studies when predominant circulating metabolites are identified. Nonetheless, methodologies such as quant ...
... approach is well-established, it requires access to often intractable authentic metabolite standards for calibration curve generation, which is typically not supported until early human clinical studies when predominant circulating metabolites are identified. Nonetheless, methodologies such as quant ...
the Information Breaking Medical
... Currently, the federally mandated process for introducing a new drug in the retail market consists of three phases. Under Phase I, the FDA must be satisfied that the new drug is safe and will not harm patients. The FDA's authority to certify safety was established in the Food, Drug and Cosmetic Act ...
... Currently, the federally mandated process for introducing a new drug in the retail market consists of three phases. Under Phase I, the FDA must be satisfied that the new drug is safe and will not harm patients. The FDA's authority to certify safety was established in the Food, Drug and Cosmetic Act ...
Fragment-Based Discovery of the Pyrazol-4
... potent (IC50 ≈ 3 nM) dual Aurora A/Aurora B inhibitors. These compounds inhibited growth and survival of HCT116 cells and produced the polyploid cellular phenotype typically associated with Aurora B kinase inhibition. Optimization of cellular activity and physicochemical properties ultimately led to ...
... potent (IC50 ≈ 3 nM) dual Aurora A/Aurora B inhibitors. These compounds inhibited growth and survival of HCT116 cells and produced the polyploid cellular phenotype typically associated with Aurora B kinase inhibition. Optimization of cellular activity and physicochemical properties ultimately led to ...
Molecules that changed our Lives Synthetic Organic
... Dr. Phani: The therapeutic action of prontosil paved the way for further investigations. In 1936 Ernest Fourneau demonstrated that in the human body Prontosil breaks down to produce sulphanilamide which is the actual agent specifically lethal to streptococci. This led to the emergence of sulpha drug ...
... Dr. Phani: The therapeutic action of prontosil paved the way for further investigations. In 1936 Ernest Fourneau demonstrated that in the human body Prontosil breaks down to produce sulphanilamide which is the actual agent specifically lethal to streptococci. This led to the emergence of sulpha drug ...
ANTIBACTERIAL AND SYNERGISTIC ACTIVITY OF ETHANOLIC AJWAIN (TRACHYSPERMUM
... A time kill analysis was carried out by performing a viable count of test pathogens in the presence of MBC and 1/2 MBC concentrations of ajwain extract in terms of CFU/ml. The surviving pathogens were estimated over a period of 4h. The time kill analysis was performed using method described by Carso ...
... A time kill analysis was carried out by performing a viable count of test pathogens in the presence of MBC and 1/2 MBC concentrations of ajwain extract in terms of CFU/ml. The surviving pathogens were estimated over a period of 4h. The time kill analysis was performed using method described by Carso ...
Quantum of Effectiveness Evidence in FDA`s Approval of
... The second way in which FDA applies ‘‘administrative flexibility’’ is by relying on an exercise of administration discretion whose source is found in a formal program or policy altering the kind of efficacy endpoint needed for approval (eg, relying on a surrogate endpoint or intermediate clinical en ...
... The second way in which FDA applies ‘‘administrative flexibility’’ is by relying on an exercise of administration discretion whose source is found in a formal program or policy altering the kind of efficacy endpoint needed for approval (eg, relying on a surrogate endpoint or intermediate clinical en ...
Hepatitis C Drug Development - HIV Research Catalyst Forum
... participate in HCV clinical trials of new drugs, as long as they show up for study visits • People with cirrhosis (serious liver scarring) are ...
... participate in HCV clinical trials of new drugs, as long as they show up for study visits • People with cirrhosis (serious liver scarring) are ...
Selective Inhibition of Brain Na,K-ATPase by Drugs
... addition of ATP, allowed to proceed for 15 min and stopped by the addition of 3 mol/l trichloracetic acid. Samples were chilled on ice for 15 min and used for the assay of released inorganic phosphate. The activity of Na,K-ATPase was obtained by subtracting the activity in the absence of Na+ and K+ ...
... addition of ATP, allowed to proceed for 15 min and stopped by the addition of 3 mol/l trichloracetic acid. Samples were chilled on ice for 15 min and used for the assay of released inorganic phosphate. The activity of Na,K-ATPase was obtained by subtracting the activity in the absence of Na+ and K+ ...
Inhibition of Purified Factor Xa Amidolytic Activity May Not Be
... proteins that are affected. The major goal for the anti-fXa small molecule drug development effort is to find pharmaceutically acceptable agents that can mimic the efficacy of warfarin without its accompanying safety problems.2 Although several secondary screens and animal models are used to optimiz ...
... proteins that are affected. The major goal for the anti-fXa small molecule drug development effort is to find pharmaceutically acceptable agents that can mimic the efficacy of warfarin without its accompanying safety problems.2 Although several secondary screens and animal models are used to optimiz ...
Thin-layer agar for detection of resistance to rifampicin, ofloxacin
... performed on solid media, and it does not require sophisticated equipment. Resistance to RMP can be considered a surrogate marker for MDR-TB, while KM and ofloxacin (OFX) are key second-line drugs for the treatment of TB in MDR-TB cases.1 The aim of the present study was to evaluate TLA for rapid de ...
... performed on solid media, and it does not require sophisticated equipment. Resistance to RMP can be considered a surrogate marker for MDR-TB, while KM and ofloxacin (OFX) are key second-line drugs for the treatment of TB in MDR-TB cases.1 The aim of the present study was to evaluate TLA for rapid de ...
Mechanisms of resistance in CML
... *BCR-ABL mutations Mutations do not always explain resistance May activate different downstream signalling pathways Very sensitive techniques may detect mutations that are not clinically relevant ...
... *BCR-ABL mutations Mutations do not always explain resistance May activate different downstream signalling pathways Very sensitive techniques may detect mutations that are not clinically relevant ...
Front Matter
... manifested itself by peripheral neuritis, emaciation, paralysis and then cardiac failure. Its Drug Discovery. A History. W. Sneader. &2005 John Wiley & Sons Ltd ...
... manifested itself by peripheral neuritis, emaciation, paralysis and then cardiac failure. Its Drug Discovery. A History. W. Sneader. &2005 John Wiley & Sons Ltd ...
Tetracycline group in children
... bioavailability[1]. Absorption is greater in the fasting state and the percentage of an oral dose absorbed on an empty stomach is low for chlortetracyclines (30%); intermediate for oxytetracycline, demeclocycline, tetracycline (60% to 80%); and high for doxycycline (95%) and minocycline (100%). High ...
... bioavailability[1]. Absorption is greater in the fasting state and the percentage of an oral dose absorbed on an empty stomach is low for chlortetracyclines (30%); intermediate for oxytetracycline, demeclocycline, tetracycline (60% to 80%); and high for doxycycline (95%) and minocycline (100%). High ...
C 1 G
... Approximate 75% of ADR in patients are classified as Type A ADR which involve lifethreatening exaggerated pharmacological activity (on-target and/or off-target) due to unanticipated increased plasma concentrations of the parent drug. This class of ADR often results from drug-drug interactions or gen ...
... Approximate 75% of ADR in patients are classified as Type A ADR which involve lifethreatening exaggerated pharmacological activity (on-target and/or off-target) due to unanticipated increased plasma concentrations of the parent drug. This class of ADR often results from drug-drug interactions or gen ...
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).