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Yogesh D.B.,NIMS University | Shenoy D.B.,NIMS University | Srinivasa G.R.,Alkem Laboratories | Nagaraja G.,NIMS University | Baig F.,NIMS University
Der Pharma Chemica | Year: 2012

The (2-butyl -5-amino-3-benzofuranyl) 4-methoxy phenyl methanone amino acids have been synthesized by the reaction of (2-butyl -5-amino-3-benzofuranyl) 4-methoxy phenyl methanone with different hydrophobic amino acids were described (DBMY1-9). All the compounds were synthesized by conventional method and characterized by IR, 1H NMR and mass spectral data. The synthesized compounds were tested for antimicrobial activity against Staphylococcus aureus, Escherichia coli and pseudomonas aeruginosa. Among the synthesized compounds (2-butyl -5-amino-3-benzofuranyl) 4-methoxy phenyl methanone amino acids (DBMY-3,7,2) was found the most active derivative against S. aureus, E. coli and P. aeruginosa and The compounds DBMY-2, 3, 4 was found the most active derivative against Candida albicans and Asperigillus fumigatus respectively. The other Compounds exhibited moderate activity against the other test microorganisms. Source

Humnabadkar V.,Astrazeneca | Madhavapeddi P.,Astrazeneca | Basavarajappa H.,Astrazeneca | Basavarajappa H.,Indiana University | And 9 more authors.
Journal of Biomolecular Screening | Year: 2015

Mycobacterium tuberculosis (Mtb) DNA gyrase ATPase was the target of a tuberculosis drug discovery program. The low specific activity of the Mtb ATPase prompted the use of Mycobacterium smegmatis (Msm) enzyme as a surrogate for lead generation, since it had 20-fold higher activity. Addition of GyrA or DNA did not significantly increase the activity of the Msm GyrB ATPase, and an assay was developed using GyrB alone. Inhibition of the Msm ATPase correlated well with inhibition of Mtb DNA gyrase supercoiling across three chemical scaffolds, justifying its use. As the IC50 of compounds approached the enzyme concentration, surrogate assays were used to estimate potencies (e.g., the shift in thermal melt of Mtb GyrB, which correlated well with IC50s >10 nM). Analysis using the Morrison equation enabled determination of Kiapps in the sub-nanomolar range. Surface plasmon resonance was used to confirm these IC50s and measure the Kds of binding, but a fragment of Mtb GyrB had to be used. Across three scaffolds, the dissociation half life, t1/2, of the inhibitor-target complex was ≤8 min. This toolkit of assays was developed to track the potency of enzyme inhibition and guide the chemistry for progression of compounds in a lead identification program. © 2014 Society for Laboratory Automation and Screening. Source

Shreenivas M.T.,Kuvempu University | Kumara Swamy B.E.,Kuvempu University | Srinivasa G.R.,Alkem Laboratories | Sherigara B.S.,Kuvempu University
Der Pharma Chemica | Year: 2011

A series of 4'-(2-n-Butyl-4-chloro-5-hydroxymethyl-imidazol-1-yl-methyl-biphenyl-2-caboxylic acid- (4-phenyl/ substituted phenyl thiazole)-amide (VI a-g) were prepared. The structures of aminothiazole derivatives were confirmed on the basis of spectral data. The newly synthesized title compounds were screened for their in vitro antibacterial activity. Some of the compounds exhibited encouraging results. Source

Van De Merbel N.,Bioanalytical Laboratory | Savoie N.,Algorithme Pharma Inc. | Yadav M.,Alkem Laboratories | Ohtsu Y.,Astellas Pharma Inc. | And 5 more authors.
AAPS Journal | Year: 2014

This paper provides a comprehensive overview of stability-related aspects of quantitative bioanalysis and recommends science-based best practices, covering small and large molecules as well as chromatographic and ligand-binding assays. It addresses general aspects, such as the use of reference values, transferability and treatment of failing stability results, and also focuses on specific types of stability assessment: bench-top, freeze/thaw and long-term frozen stability, stock stability, extract stability, stability in whole blood, tissue and urine, and stability of endogenous analytes, in special matrix types and in incurred samples. © 2014 American Association of Pharmaceutical Scientists. Source

Shreenivas M.T.,Kuvempu University | Kumara Swamy B.E.,Kuvempu University | Manjunatha J.G.,Kuvempu University | Chandra U.,Kuvempu University | And 3 more authors.
Der Pharma Chemica | Year: 2011

In the present research work a series of isoxazole derivatives have been synthesized. The isoxazole derivatives are prepared starting from ethylacetoacetate with triethyl orthoformate followed by cyclization and hydrolysis of ester to form 5-Methylisoxazole-4-carboxylic acid. Further the acid is converted into acid chloride followed by condensation leads to a new series of 5-methyl-N-(substituted aryl) isoxazole-4- carboxamides (9 a-f, 13 a-c). The structures of newly synthesized compounds are confirmed on the basis of IR, 1H NMR of spectral data. The newly synthesized title compounds were screened for their in vitro antimicrobial activity. The compounds N-(2-chloro-5-nitrophenyl)-5-methylisoxazole-4-carboxamide (9 e) and N-(4-cyano-3-(trifluoro-methyl)-phenyl)-5-methylisoxazole-4-carbox-amide (9 f) are shown good antibacterial and anti fungal activity. The electrochemical reduction was carried out by using cyclic voltammetric technique and the effects of scan rate, sulphuric acid concentration and substitutents were studied. The overall electrode process was diffusion-controlled. Source

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