Antimicrobial activity of N-hydroxyalkyl 1,2-benzisothiazol-3(2H)-ones and their thiono analogues

被引:27
作者
Borgna, P
Carmellino, ML
Natangelo, M
Pagani, G
Pastoni, F
Pregnolato, M
Terreni, M
机构
[1] IST RIC FARMACOL MARIO NEGRI,LAB FARMACOL & TOSSICOL AMBIENTALE,I-20157 MILAN,ITALY
[2] COMMISS EUROPEAN COMMUNITIES,JOINT RES CTR,INST ENVIRONM,MICROBIOL LAB,I-21020 ISPRA,VA,ITALY
关键词
1,2-benzisothiazol-3(2H)-one; 1,2-benzisothiazol-3(2H)-thione; antifungal activity; antibacterial activity;
D O I
10.1016/S0223-5234(97)89857-1
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
N-Hydroxyalkyl derivatives of 1,2-benzisothiazol-3(2H)-one and 1,2-benzisothiazol-3(2H)-thione have been prepared and their antifungal and antibacterial activity evaluated. Several compounds were active against selected fungi and Gram-positive microorganisms. Interesting activity was observed against the anaerobic strain Clostridium perfringens. Generally the more active compounds belong to the class of 1,2-benzisothiazol-3(2H)-ones. The retardation matches R(M) of the compounds was also evaluated but the results obtained show that lipophilicity has only a minor effect on the antimicrobial activity.
引用
收藏
页码:919 / 925
页数:7
相关论文
共 26 条
[2]   FUEL-SOLUBLE BIOCIDES FOR CONTROL OF CLADOSPORIUM-RESINAE IN HYDROCARBON FUELS [J].
ANDRYKOVITCH, G ;
NEIHOF, RA .
JOURNAL OF INDUSTRIAL MICROBIOLOGY, 1987, 2 (01) :35-40
[3]  
BARUFFIN.A, 1968, FARMACO-ED SCI, V23, P3
[4]  
BARUFFINI A, 1968, FARMACO-ED SCI, V23, P572
[5]  
BIAGI GL, 1991, QSAR RATIONAL APPROA, V16, P83
[6]  
BORGNA P, 1983, FARMACO-ED SCI, V38, P801
[7]   ON THE REACTION BETWEEN 3H-1,2-DITHIOLO[3,4-B]-PYRIDINE-3-THIONE AND PRIMARY ALKYL AND ARYLALKLAMINES [J].
BORGNA, P ;
PREGNOLATO, M ;
INVERNIZZI, AG ;
MELLERIO, G .
JOURNAL OF HETEROCYCLIC CHEMISTRY, 1993, 30 (04) :1079-1084
[8]  
BORGNA P, 1968, FARMACO, V23, P1193
[9]   UBER 1.2-BENZISOTHIAZOLIN-THIONE-(3) UND 3-IMINO-3H-1.2-BENZODITHIOLE [J].
BOSHAGEN, H ;
FELTKAMP, H ;
GEIGER, W .
CHEMISCHE BERICHTE-RECUEIL, 1967, 100 (07) :2435-&
[10]   A SIMPLE ASSESSMENT OF PARTITION DATA FOR CORRELATING STRUCTURE AND BIOLOGICAL ACTIVITY USING THIN-LAYER CHROMATOGRAPHY [J].
BOYCE, CBC ;
MILBORROW, BV .
NATURE, 1965, 208 (5010) :537-+