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

被引：51

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 50 条

[21] Synthesis, antimicrobial and cytotoxic activities of some novel thiazole clubbed 1,3,4-oxadiazoles
Desai, N. C.
Bhatt, Nayan
Somani, Hardik
Trivedi, Amit
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2013, 67 : 54 - 59
[22] Conversion of 2(3H)-furanones into 1,3,4-oxadiazoles
Elgazwy, ASSH
Zaki, MY
Eid, NN
Hashem, AI
HETEROATOM CHEMISTRY, 2003, 14 (06) : 570 - 574
[23] Biological study on novel coumarinyl 1,3,4-oxadiazoles
Molnar, Maja
Amic, Ana
Pavic, Valentina
Kovac, Tihomir
Kovac, Marija
Has-Schon, Elizabeta
TURKISH JOURNAL OF CHEMISTRY, 2018, 42 (01) : 146 - +
[24] Syntheses and insecticidal activities of novel 2,5-disubstituted 1,3,4-oxadiazoles
Zheng, XM
Li, Z
Wang, YL
Chen, WD
Huang, QC
Liu, CX
Song, GH
JOURNAL OF FLUORINE CHEMISTRY, 2003, 123 (02) : 163 - 169
[25] A convergent synthesis of 1,3,4-oxadiazoles from acyl hydrazides under semiaqueous conditions
Tokumaru, Kazuyuki
Johnston, Jeffrey N.
CHEMICAL SCIENCE, 2017, 8 (04) : 3187 - 3191
[26] New 2-benzylsulfanyl-nicotinic acid based 1,3,4-oxadiazoles: Their synthesis and biological evaluation
Patel, Navin B.
Purohit, Amit C.
Rajani, Dhanji P.
Moo-Puc, Rosa
Rivera, Gildardo
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2013, 62 : 677 - 687
[27] SYNTHESIS OF SOME SUBSTITUTED 1,3,4-OXADIAZOLES, THEIR ANTIBACTERIAL AND ANTIAMEBIC ACTIVITY
KACHROO, PL
GUPTA, R
GUPTA, SC
GUPTA, AK
NATIONAL ACADEMY SCIENCE LETTERS-INDIA, 1990, 13 (04): : 125 - 126
[28] One-pot Synthesis of 2,5-Disubstituted-1,3,4-oxadiazoles Based on the Reaction of N,N-Dimethyl Amides with Acid Hydrazides
Li, Qiang
Tao, Yi
Xu, Dongfang
Zhang, Haobing
Duan, Liping
JOURNAL OF THE CHINESE CHEMICAL SOCIETY, 2014, 61 (06) : 665 - 670
[29] SYNTHESIS OF SOME NEW HETEROCYCLIC 1,3,4-OXADIAZOLES WITH ANTIBACTERIAL ACTIVITY
GHATTAS, AG
ELSHERIEF, HA
RAHMAN, AEA
MAHMOUD, AM
PHARMAZIE, 1982, 37 (06): : 410 - 412
[30] Synthesis and Antineoplastic Evaluation of Novel Unsymmetrical 1,3,4-Oxadiazoles
Nieddu, Valentina
Pinna, Giansalvo
Marchesi, Irene
Sanna, Luca
Asproni, Battistina
Pinna, Gerard A.
Bagella, Luigi
Murineddu, Gabriele
JOURNAL OF MEDICINAL CHEMISTRY, 2016, 59 (23) : 10451 - 10469

← 1 2 3 4 5 →