The direct separation of dipeptidyl peptidase IV (DPP‐4) inhibitors such as Sitagliptin (STG), Linagliptin (LIG), and Saxagliptin (SAG) enantiomers in normal phase conditions have been achieved on immobilized polysaccharide‐based chiral stationary phases (CSPs), as well as on the macrocyclic glycopeptide vancomycin chiral stationary phase (Chirobiotic V2) under polar ionic mode. The enantiomers of these targets could be separated completely (resolution factor Rs > 2) using the Chirobiotic V2 column in polar ionic mode with the mobile phase (MeOH/AcOH/TEA 100/0.3/0.1 v/v/v) in an isocratic elution at 1.0 ml min−1. The effect of the mobile phase composition on separation, including buffer salts, acid–base modifiers, and analyte structures, was evaluated. The developed technique was validated in the polar ionic mode according to the International Conference on Harmonization (ICH) Q2R1 guidelines in terms of accuracy, precision, selectivity, linearity, limit of detection (LOD), and limit of quantification (LOQ). The calibration curve was linear in a concentration range from LOQ to 3.75 μg/ml. The LOD and LOQ of STG, LIG, and SAG were 0.15 and 0.45, 0.15 and 0.50, 0.16 and 0.50, respectively. The proposed method is said to be selective, accurate, and precise. Finally, the validated method was used successfully for the quantitative determination of DPP‐4 enantiomers in pharmaceutical analytes.
A series of 3-aryl indazoles 4a-4j were obtained by Pd catalyzed Suzuki coupling reaction. All the substrates were obtained in good yields under moderate reaction conditions. Next, the prepared compounds 4a-4j were screened for
their antibacterial activity. The anti-bacterial activities of the prepared compounds were investigated against three
bacterial strains i.e. Xanthomonas campestris, Escherichia coli, Bacillus megaterium. The anti-bacterial evaluation studies of
these 3-aryl indazoles revealed that some of these test compounds possess moderate in vitro antibacterial activity.
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