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

被引：53

作者：

Morjan, Rami Y. ^{[1
]}

Mkadmh, Ahmed M. ^{[2
]}

Beadham, Ian ^{[3
]}

Elmanama, Abdelrauof A. ^{[4
]}

Mattar, Mohammed R. ^{[1
]}

Raftery, James ^{[5
]}

Pritchard, Robin G. ^{[5
]}

Awadallah, Adel M. ^{[1
]}

Gardiner, John M. ^{[6
]}

机构：

[1] Islamic Univ Gaza, Fac Sci, Dept Chem, Gaza, Israel

[2] Alaqsa Univ, Fac Sci Appl, Dept Chem, Gaza, Israel

[3] Manchester Metropolitan Univ, Dept Chem, Manchester M15 6BH, Lancs, England

[4] Islamic Univ Gaza, Fac Sci, Med Technol Dept, Gaza, Israel

[5] Univ Manchester, Sch Chem, Manchester M13 9PL, Lancs, England

[6] Univ Manchester, Manchester Inst Biotechnol, Sch Chem & EPS, Manchester M1 7DN, Lancs, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 24期

关键词：

Hydrazides; N-acylhydrazone; 1,3,4-Oxadiazole; N-acetyl-1,3,4-oxadiazoles; Antibacterial; BIOLOGICAL-ACTIVITIES; DESIGN; ANTIBIOTICS; INHIBITORS;

D O I：

10.1016/j.bmcl.2014.10.029

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 mu g respectively. (C) 2014 Published by Elsevier Ltd.

引用

页码：5796 / 5800

页数：5

共 33 条

[1]

Adibi H., 2012, J REP PHARM SCI, V1, P60, DOI [10.5455/medarh.2012.66.89-91, DOI 10.5455/MEDARH.2012.66.89-91]

[2]

[Anonymous], GLOB TUB REP 2013

[3] Oxadiazoles in Medicinal Chemistry [J].

Bostrom, Jonas ;

Hogner, Anders ;

Llinas, Antonio ;

Wellner, Eric ;

Plowright, Alleyn T. .

JOURNAL OF MEDICINAL CHEMISTRY, 2012, 55 (05) :1817-1830

[4] TUBERCULOSTATIC HYDRAZIDES AND THEIR DERIVATIVES [J].

BUUHOI, NP ;

XUONG, ND ;

NAM, NH ;

BINON, F ;

ROYER, R .

JOURNAL OF THE CHEMICAL SOCIETY, 1953, (MAY) :1358-1364

[5]

Cakir Bilge, 2001, Journal of Faculty of Pharmacy of Gazi University, V18, P99

[6] Synthesis, characterization and biological activity of some new 1,3,4-oxadiazole bearing 2-flouro-4-methoxy phenyl moiety [J].

Chandrakantha, B. ;

Shetty, Prakash ;

Nambiyar, Vijesh ;

Isloor, Nishitha ;

Isloor, Arun M. .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2010, 45 (03) :1206-1210

[7] Anticonvulsant properties of various acetylhydrazones, oxamoylhydrazones and semicarbazones derived from aromatic and unsaturated carbonyl compounds [J].

Dimmock, JR ;

Vashishtha, SC ;

Stables, JP .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2000, 35 (02) :241-248

[8] A sensitive and quick microplate method to determine the minimal inhibitory concentration of plant extracts for bacteria [J].

Eloff, JN .

PLANTA MEDICA, 1998, 64 (08) :711-713

[9] Synthesis of malarial plasmepsin inhibitors and prediction of binding modes by molecular dynamics simulations [J].

Ersmark, K ;

Nervall, M ;

Hamelink, E ;

Janka, LK ;

Clemente, JC ;

Dunn, BM ;

Blackman, MJ ;

Samuelsson, B ;

Aqvist, J ;

Hallberg, A .

JOURNAL OF MEDICINAL CHEMISTRY, 2005, 48 (19) :6090-6106

[10] Antibiotics for Emerging Pathogens [J].

Fischbach, Michael A. ;

Walsh, Christopher T. .

SCIENCE, 2009, 325 (5944) :1089-1093

← 1 2 3 4 →