Our current work is aimed at synthesizing novel substituted 1,2,4-triazolyl-fluoroquinolone analogs and study of their biological activity to find active promising molecules. The structural elucidation of the products was demonstrated by a variety of spectroscopic methods such as IR, 1 H-NMR, 13 C-NMR, mass and elemental analysis. The newly synthesized 1,2,4-triazole derivatives were tested in vitro for their ability to inhibit the growth of seven different microbes including S. epidermidis, S. pneumoniae, S. aureus, B. subtilis, K. pneumoniae, E. coli, and P. aeruginosa. Five FQ derivatives 5d, 5e, 5h, 5j, and 5b have demonstrated good antibacterial activity against S. pneumoniae with MICs ranging from 2.5 -22.0 μg/mL, while 5c, 5g reported comparable activity against P. aeruginosa with respect to the standard drugs moxifloxacin and ciprofloxacin. The possible mechanism of antibacterial activity of fluoroquinolones was investigated via molecular docking by using DNA gyrase of S. pneumoniae (3RAE). The pefloxacin derivatives also tended a good antibacterial ability based on the results of the molecular docking, ligand 5h with good binding affinity (À 9.92 Kcal/mol) and binding site interactions via
A series of degradation impurities of Flucloxacillin and Dicloxacillin were synthesized. The formation and a facile synthesis of each impurity were presented in detail, namely penicilloic acids of Dicloxacillin (3) (Ph.Eur. Impurity‐A), Dicloxacillin glycine analog (4), Dicloxacillin penilloic acids (5) (Ph.Eur. Impurity‐B), Dicloxacillin Pencillamide (6), N‐Acetylated penicilloic acid of Dicloxacillin (7), DCMICAA adduct of Dicloxacillin penicilloic acid (8), Flucloxacillin glycine analog (Ph.Eur. Impurity‐F) (9), penicilloic acids of Flucloxacillin (10), penilloic acids of Flucloxacillin (11), CFMICAA adduct of Flucloxacillin penicilloic acid (Flucloxacillin Ph.Eur. Impurity‐H) (12), Flucloxacillin Penicillamide (Flucloxacillin Ph.Eur. Impurity‐E) (13), and N‐Acetylated penicilloic acid of Flucloxacillin (14). These impurities are extensively characterized by various analytical techniques.
Amlodipine belongs to the class of calcium channel blocker that is used to reduce high blood pressure (hypertension). Two related substances of amlodipine namely 3‐(2‐[1.3‐dioxo‐1,3‐dihydro‐2H‐isoindol‐2‐yl]ethyl)‐5‐methyl‐(4RS)‐4(2‐chlorophenyl)‐2‐([2‐(1,3‐dioxo‐1,3‐dihydro‐2H‐isoin‐dol‐2‐yl)ethoxy]methyl)‐6‐methyl‐1,4‐dihydropyridine‐3,5‐dicarboxylate (11) and 3‐([2‐aminoethyl]‐5‐aminoethoxy)‐4‐(2‐chlorophenyl)‐1,4‐dihydro‐6‐methylpyridine‐3,5‐dicarboxylate (12) were identified. The present work describes the origin, synthesis, and characterization of these related substances.
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