Synthesis and Biological Activity of Some New N1-(6-fluoro-4-oxoquinolin-8-yl)amidrazones

被引：7

作者：

Abadleh, Mohammed M. ^{[1
]}

El-Abadelah, Mustafa M. ^{[2
]}

Sabri, Salim S. ^{[2
]}

Abdallah, Qasem M. A. ^{[3
]}

Nasr, Abdelrahman ^{[3
]}

El-Badawy, Mohamed F. ^{[4
]}

机构：

[1] Taibah Univ, Coll Pharm, Al Madinah Almonawarrah 41477, Saudi Arabia

[2] Univ Jordan, Fac Sci, Dept Chem, Amman 11942, Jordan

[3] Taif Univ, Coll Pharm, Dept Pharmacol & Toxicol, At Taif, Saudi Arabia

[4] Taif Univ, Coll Pharm, Dept Microbiol & Immunol, At Taif, Saudi Arabia

来源：

LETTERS IN ORGANIC CHEMISTRY | 2014年 / 11卷 / 09期

关键词：

N1-(4-Oxoquinolin-8-yl)hydrazonoyl chloride; nitrile imines; 1,3-nucleophilic addition; amidrazones; antibacterial activity; DERIVATIVES; HALIDES; INVITRO; ACIDS;

D O I：

10.2174/1570178611666140807004701

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A selected set of new N 1- (6-fluoro-4-oxoquinolin-8-yl)amidrazone-3-carboxylates (8a-e) incorporating N-piperazines and related congeners has been synthesized by reacting the hydrazonoyl chloride, derived from 8-amino-6-fluoro-4-oxoquinloine-3-carboxylate, with the appropriate sec-cyclic amine. Their suggested structures are supported by elemental analysis, H-1 NMR, C-13 NMR and ESI-HRMS spectral data. These novel compounds (8a-e) were screened for their antitumor and antibacterial activity. While no significant antitumor activity was observed, compounds 8a, 8b and 8d have shown moderate in vitro antibacterial activity against Gram positive bacteria cells. Unlike the others, compound 8a has also shown to moderately inhibit the growth of Gram negative bacteria.

引用

页码：664 / 670

页数：7

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