A series of fifteen novel isatin oxime ether-tethered aryl 1H-1,2,3-triazole hybrids 5a-o were designed and synthesized by employing Cu(I) catalyzed azide-alkyne [3+2] cycloaddition (CuAAC) between isatin oxime O-propargyl ether and...
A simple, sensitive, and stability indicating isocratic reverse phase high performance liquid chromatography method has been developed, optimized and validated for the separation and quantification of S-enantiomer in linagliptin (R-enantiomer) drug substance. Enantiomeric separation was achieved on a Cellulose tris(4-chloro-3-methylphenylcarbamate) stationary phase. Mobile phase consists of aqueous diammonium hydrogen phosphate buffer and acetonitrile in the ratio of 35:65 v/v. Isocratic elution was performed at a flow rate of 1.0 mL/min, the column oven temperature was set at 40°C and detection was at 226 nm. The resolution between R and S enantiomers is found to be more than 4.0. The impact of mobile phase composition, pH of buffer and temperature on the resolution has been studied. The detector response is found to be linear over the concentration range of 0.17-1.7 g/mL. LOD and LOQ levels of S-enantiomer are found to be 0.057 and 0.172 g/mL respectively. The recovery of S-enantiomer is 99.8% w/w. The proposed method is validated for specificity, precision, linearity, accuracy and robustness.
A straightforward, rapid and efficient one‐pot method was developed for the synthesis of 2,4 ‐diphenyl‐1,2 dihydroquinazoline and their analogues. The reactions were performed with different type of benzylamine and 2‐bromo benzophenone using ammonium acetate and characterized by 1H NMR, 13C NMR and Mass spectroscopic techniques. All the compounds were tested for MDA‐MB‐231, A549 and DU‐145 type of human cancer cell lines. Among the synthesized compounds, 4 j (4‐phenyl‐2‐(3,4,5‐trimethoxyphenyl)‐1,2‐dihydroquinazoline) and 4 e (2‐(3,4‐dichlorophenyl)‐4‐phenyl‐1,2‐dihydroquinazoline) molecules were found to possess good anticancer activity. The binding nature of these molecules was explored through docking studies.
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