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A series of new 3-(2-substituted amino/substituted hydrazino-1,3-thiazol-4-yl)-4-hydroxy-1-methyl/phenylquinolin-2 (1H)-one hydroiodide 3a-3f and 4a-4f derivatives were prepared by heating 3-Acetyl-4-hydroxy-1-methyl/phenyl quinolin-2 (1H)-one 2a-2b with substituted thiourea and substituted thiosemicarbazide in presence of iodine in n-butanol. The title compounds were characterized on the basis of IR, 1H NMR, 13C NMR and Mass spectral (MS) studies. Further title compounds were evaluated for antibacterial and antifungal by Agar diffusion assay method where as antitubercular activity by Micro-plate Alamar Blue Assay (MABA). Among 12 synthesized novel compounds 3a, 3b, 4d exhibited promising antibacterial activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa. 3a, 3b, 3e, 4d, 4e showed good antifungal activity against Candida albicans and Aspergillus niger. 3a, 3d, 4d showed good antitubercular activity against Mycobacterium tuberculosis H37Rv strain.

Background: Poisoning with organophosphorus (OP) compounds are frequent because OP are widely used as insecticide or pesticide. OP compounds exert inhibition on acetylcholinesterase (AChE) activity by irreversibly binding to the catalytic site of the enzyme. The inhibition of AChE leads to hyperstimulation of muscarnic and nicotinic receptors due to excess of acetylcholine (ACh). Methodology:Various quinolin-2(1H)-one fused oxazole were synthesized by condensation and cyclization of chalcones with hydroxylamine hydrochloride in presence of piperidine. Synthesized compound were tested for in vitro reactivation of chlorpyrifos and methyl parathion inhibited AChE enzyme using pralidoxime (2-PAM) as standard reference. Result:Among the synthesized compounds, the compound 3b, 3f, 3g, and 5a have showed promising activity as compared to standard against chlorpyrifos inhibited AChE. However, 3f and 3gshowed good activity as compared to standard against methyl parathion inhibited AChE. th Conclusion: The derivatives having nitro and chloro substitution at 4 position gave potent activity against both OP compounds as compared to standard at concentration 0.001 M. Moreover, these quinolone fused oxazole seem to be very promising because of their sufcient reactivation potency at lower concentration-3 (10 M).

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Background: The biological effects of organophosphorus (OP) compounds are connected with the irreversible inhibition of acetylcholinesterase (AChE), an important neuromediator acetylcholine (ACh) splitting enzyme in the human body at the synaptic clefts. Due to this inhibition, AChE is unable to fulfil its physiological function resulting in the accumulation of ACh, which, in turn over stimulates the parasympathetic nerve receptors, and causes fatal cholinergic crisis. Objective: The objective of the study was to synthesize a series of Schiff base oximes and to assess their evaluating for their in vitro reactivating potency against chlorpyrifos inhibited AChE. Methods: The amino group of 4-amino acetophenone exploited by treating with substituted benzaldehyde in the presence of glacial acetic acid to form Schiff base (1a-1f). The titled compounds (2a-2f) were prepared by treating Schiff base with hydroxylamine hydrochloride in the presence of alcohol. Through structural and spectral analysis, the structure of compounds was confirmed. The synthesized compounds were evaluated for their reactivation efficacy against chlorpyrifos-inhibited rat brain AChE by Ellman's method. Results: The pralidoxime (2-PAM) was potent reactivation against chlorpyrifos-inhibited AChE at the concentration tested (0.001 M). In this case, the compounds 2a (40.4%, 60 min) and 2d (37.9%, 60 min) showed promising reactivation as compared to 2-PAM (40.6%, 60min) against chlorpyrifos-inhibited AChE. Conclusion: Compounds having chloro (2a) and nitro (2d) substitution on 4th position gave good activity against chlorpyrifos-inhibited AChE. Moreover, these Schiff base oximes seem to be very promising because of their sufficient reactivation strength at lower concentration (10-3 M).