NITROHETEROCYCLIC ANTIMICROBIAL AGENTS .I. NITROTHIAZOLECARBOXALDEHYDE DERIVATIVES

被引:15
作者
ASATO, G
BERKELHAMMER, G
MOON, EL
机构
[1] Chemical Research and Development Laboratories, Agricultural Division, American Cyanamid Company, Princeton
关键词
D O I
10.1021/jm00303a007
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of derivatives of 2-thiazolecarboxaldehyde, 2-nitro-5-thiazolecarboxaldehyde, 5-nitro-2-thiazolecarboxaldehyde, and 4-nitro-2-thiazolecarboxaldehyde was synthesized and assayed for antimicrobial activity. Only 2,5-disubstituted thiazoles in which one substituent is a nitro group were active against microorganisms in vitro. 1-{[(5-Nitro-2-thiazolyl)methylene]amino}-2-imidazolidinone exhibited activity against Staphylococcus aureus and Escherichia coli infections in mice. © 1969, American Chemical Society. All rights reserved.
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页码:374 / +
页数:1
相关论文
共 22 条
[1]   NITRATION OF 2-METHYLTHIAZOLE [J].
ASATO, G .
JOURNAL OF ORGANIC CHEMISTRY, 1968, 33 (06) :2544-&
[2]  
Bredereck H., 1963, ANGEW CHEM-GER EDIT, V2, P738
[3]  
CARADONNA CLARY, 1964, ANN CHIM, V54, P539
[4]   CHEMOTHERAPEUTIC NITROHETEROCYCLES . NITROPYRROLE-2-CARBOXALDEHYDE DERIVATIVES [J].
COLWELL, WT ;
LANGE, JH ;
HENRY, DW .
JOURNAL OF MEDICINAL CHEMISTRY, 1968, 11 (02) :282-&
[5]  
Dodd MC, 1944, J PHARMACOL EXP THER, V82, P11
[6]   ANTIPARASITIC AGENTS .I. 2-(NITRO-HETEROCYCLIC) BENZIMIDAZOLES BENZOXAZOLES AND BENZOTHIAZOLES [J].
DUNN, GL ;
ACTOR, P ;
DIPASQUO, VJ .
JOURNAL OF MEDICINAL CHEMISTRY, 1966, 9 (05) :751-&
[7]  
GEVER G, 1953, Patent No. 2652402
[8]   CHEMOTHERAPEUTIC NITROHETEROCYCLES . DERIVATIVES OF 5-NITROTHIAZOLE-2-CARBOXALDEHYDE AND 5-NITROTHIAZOLE-2-CARBOXYLIC ACID [J].
HENRY, DW .
JOURNAL OF MEDICINAL CHEMISTRY, 1969, 12 (02) :303-&
[9]   PREPARATION OF 2-IMIDAZOLE- AND 2-THIAZOLECARBALDEHYDES [J].
IVERSEN, PE ;
LUND, H .
ACTA CHEMICA SCANDINAVICA, 1966, 20 (10) :2649-&
[10]   ANTIMICROBIALS .2. NITROFURAN ANALOGUES CONTAINING 2-HYDRAZONOMETHYL SIDE-CHAIN [J].
JOHNSTON, RG ;
KIDD, D .
JOURNAL OF THE CHEMICAL SOCIETY, 1964, (DEC) :4734-&