Antimicrobial evaluation of 4-methylsulfanyl benzylidene/3-hydroxy benzylidene hydrazides and QSAR studies

Abstract

A series of 4-methylsulfanyl benzylidene/3-hydroxy benzylidene hydrazides (1-20) was synthesized and tested for in vitro antimicrobial activity against S. aureus, B. subtilis, E. coli, C. albicans and A. niger. The results of antimicrobial studies indicated that 3-phenylacrylic acid-(3-hydroxybenzylidene)-hydrazide, 16, was the most effective as it showed both bactericidal and fungicidal properties and other compounds possessed bacteriostatic/ fungistatic activity. The multi-target QSAR model demonstrated that the topological parameter, Balaban topological index (J) is effective in describing the antimicrobial activity of synthesized substituted hydrazides.

Design, Synthesis, and Pharmacological Evaluation of N-Acylhydrazones and Novel Conformationally Constrained Compounds as Selective and Potent Orally Active Phosphodiesterase-4 Inhibitors

“…The imidazo[1,2- a ]pyridine derivative 13 was obtained with a 79% yield using regioselective cyclocondensation of 2-aminopyridine 12 with ethyl 2-chloro-acetoacetate in absolute ethanol at reflux (Scheme ). , The successive hydrazinolysis and acid-catalyzed condensation of 12 with 3,4-dimethoxybenzaldehyde gave the desired 2-methylimidazo[1,2- a ]pyridinyl NAH 7h with a 72% yield, as previously described. It is worth mentioning that some compounds of the 5 and 7 series described herein can be found in other studies with different routes of synthesis and biological activities distinct from those intended here. − …”

Synthesis of 2,5‐Disubstituted‐1,3,4‐oxadiazole Derivatives and Their Evaluation as Anticancer and Antimycobacterial Agents

“…Initially, acids ( 1, 2 ) have been smoothly transformed to their ester counterparts ( 3, 4 ) which upon hydrazinolysis with 100% hydrazine hydrate under refluxing ethanol (99.9%) yielded 5, 6 respectively in excellent yields by adopting the standard methods . Respective individual condensation between the compounds 5, 6 with appropriate aromatic aldehyde (ArCHO) for 6 h afforded the key intermediate 7, 8 which have been carried forward without further purification . Lastly, oxidative cyclisation of composites 7, 8 with molecular iodine in presence of oxidant hydrogen peroxide at 60 °C for 10 h generated the title compounds 9 , 10 (Figure ) in good yields .…”

2-Substituted-3-(5-Substituted-1,3,4-oxadiazol/thiadiazol-2-yl) Thiazolidin-4-one Derivatives: Synthesis, Anticancer, Antimicrobial, and Antioxidant Potential

“…Results were recorded as theMIC after incubating the samples at 25 ± 1 °C (7 days) for A. niger , at 25 ± 1 °C (36 h) for T. harzianum and at 37 ± 1 °C (24 h) for bacteria (s), respectively. The MIC for the tested compound was observed as the lowest concentration of the compound that prevented microorganism growth inside the test tube [ 37 ]. The antimicrobial potential screening value was calculated as amicromolar value [µM] for all the synthesized compounds by using the following equation (Equation (3)): …”