Antibacterial activities of novel nicotinic acid hydrazides and their conversion into N-acetyl-1,3,4-oxadiazoles

Synthesis of a series of novel N-acylhydrazones of nicotinic acid hydrazides 3a-j via condensation of nicotinic acid hydrazide 1 with the corresponding aldehydes and ketones is described. The series 3a-j was evaluated for in vitro antibacterial activity against two gram negative (Pseudomonas aerugin...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2014-12, Vol.24 (24), p.5796-5800
Hauptverfasser: Morjan, Rami Y, Mkadmh, Ahmed M, Beadham, Ian, Elmanama, Abdelrauof A, Mattar, Mohammed R, Raftery, James, Pritchard, Robin G, Awadallah, Adel M, Gardiner, John M
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Sprache:eng
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Zusammenfassung:Synthesis of a series of novel N-acylhydrazones of nicotinic acid hydrazides 3a-j via condensation of nicotinic acid hydrazide 1 with the corresponding aldehydes and ketones is described. The series 3a-j was evaluated for in vitro antibacterial activity against two gram negative (Pseudomonas aeruginosa and Klebsiella pneumoniae) and two gram positive (Streptococcus pneumoniae and Staphylococcus aureus) bacteria. The zone of inhibition was measured using the disk diffusion method, and in vitro minimum inhibitory concentration indicating that compounds 3a and 3e were effective against P. aeruginosa with MICs of 0.220 and 0.195 μg respectively.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2014.10.029