Di Bella M, Monzani A, Andrisano M G, Fabio U, Quaglio G P
Farmaco Sci. 1979 Mar;34(3):189-98. doi: 10.1002/chin.197930260.
The antimicrobial activity of a series of fluoro derivatives of benzothiadiazine and sulfonamides was studied. The compounds tested can be grouped as: a) 3-alkylmercapto derivatives of 6-trifluoromethyl-1,2,4-benzothiadiazine-1,1-dioxide (III leads to VI); the 3-mercapto precursor (VII) and the related 3-picolinic salt (VIII); b) 3-trifluoromethyl derivatives of 1,2,4-benzothiadiazine-1,1-dioxide and of its benzene substituted derivatives (IX leads to XVI); c) trifluoroacetylaminobenzenesulfonamides (XVII leads to XXV). Two of the 3-alkylmercapto compounds [(V) and (VI)] showed marked inhibitory activity against some strains of Staphylococcus, Streptococcus and Diplococcus. None of the compounds tested proved active against Gram-negative schizomycetes (genera Salmonella, Shigella, Escherichia, Proteus, Pseudomonas, Enterobacter, Klebsiella, Serratia, Yersinia, Providencia) or against yeasts (Candida).
研究了一系列苯并噻二嗪和磺酰胺的氟衍生物的抗菌活性。所测试的化合物可分为:a)6-三氟甲基-1,2,4-苯并噻二嗪-1,1-二氧化物的3-烷基巯基衍生物(III至VI);3-巯基前体(VII)和相关的3-吡啶盐(VIII);b)1,2,4-苯并噻二嗪-1,1-二氧化物及其苯取代衍生物的3-三氟甲基衍生物(IX至XVI);c)三氟乙酰氨基苯磺酰胺(XVII至XXV)。3-烷基巯基化合物中的两种[(V)和(VI)]对某些葡萄球菌、链球菌和双球菌菌株表现出显著的抑制活性。所测试的化合物均未证明对革兰氏阴性裂殖菌(沙门氏菌属、志贺氏菌属、大肠杆菌属、变形杆菌属、假单胞菌属、肠杆菌属、克雷伯氏菌属、沙雷氏菌属、耶尔森氏菌属、普罗威登斯菌属)或酵母(念珠菌属)有活性。