Novel amino-pyrazolone, amino-isoxazolone and amino-pyrimidinone derivatives were prepared from ethyl 4-phenylsulfonyl-2-(2-phenylsulfonylethyl)-2-cyanobutyrate (1), ethyl 4-arylsulfonyl-3-aryl-2-cyanobutyrate (7) and ethyl 4-arylmethylsulfonyl-3-aryl-2-cyanobutyrate (8). The lead molecules have been tested for their antimicrobial activity and antioxidant property.
A stability-indicating ultraperformance liquid chromatographic method has been developed for the quantitative determination of degradation products and process-related impurities of daclatasvir in a pharmaceutical dosage form. Chromatographic separation was achieved on a polar Waters ACQUITY BEH phenyl 100 × 2.1 mm, 1.7-μm column using the gradient program consisting of mobile phase A: 0.03 M sodium perchlorate with 0.002 M of 1-octanesulfonic acid sodium salt (pH 2.5 buffer) and mobile phase B: 0.03 M sodium perchlorate with 0.02 M of 1-octanesulfonic acid sodium salt (pH 2.5 buffer) with acetonitrile in the ratio of 20:80% v/v. A flow rate of 0.4 mL/min is maintained under ultraviolet detection at 305 nm. The run time was 15 min, within which daclatasvir, its related impurities and unknown degradants were well resolved. The method was found to produce symmetric and sharp peaks with good separation between process-related impurities and degradation impurities. Samples were subjected to hydrolysis (acid and base), oxidative, photolytic and thermal stress conditions to prove the stability-indicating nature of the method. The unknown degradation products were identified by PDA/QDa mass detector. This mass spectrum reveals protonated molecular ion peaks [M + H]+ at m/z DP1-582.4 in acid and base hydrolyses and m/z DP2-778.5 in peroxide hydrolysis. The method was validated in terms of specificity, precision, linearity, accuracy, limit of detection, limit of quantification and robustness as per ICH guidelines.
A new class of sulfone-linked bis heterocycles, methyl-3-(4 -aryl-1 H-pyrazol-3 -ylsulfonyl)-4-aryl-3H-pyrrole-3-carboxylate (8), methyl-3-(1 -phenyl-3 ,5 -diaryl-1 H-pyrazol-4 -ylsulfonyl)-4-aryl-3H-pyrrole-3-carboxylate (9) and methyl-3-(3 ,5 -diarylisoxazol-4 -ylsulfonyl)-4-aryl-3H-pyrrole-3-carboxylate (10) were prepared by the regioselective reaction of methyl-3-aryl-2-(E-arylethenesulfonyl)acrylate (2) with tosylmethyl isocyanide followed by fuctionalization of olefin moiety with 1,3-dipolar reagents. The lead compounds were tested for their antimicrobial activity.
A new class of bis heterocycles-sulfone linked pyrazolyl oxadiazoles and thiadiazoles were developed from Z-styrylsulfonylacetic acid. The pyrazolyl thiadiazoles exhibited excellent antimicrobial activity whereas pyrazolyl oxadiazoles displayed good antioxidant activity.
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