On April 30, 2019, Luna, Breanna L.; Garcia, Javier A.; Huang, Min; Ewing, Peter J.; Valentine, Sonya C.; Chu, Yi-Ming; Ye, Qi-Zhuang; Xu, H. Howard published an article.Quality Control of 2-Methylisothiazol-3(2H)-one hydrochloride The title of the article was Identification and characterization of novel isothiazolones with potent bactericidal activity against multi-drug resistant Acinetobacter baumannii clinical isolates. And the article contained the following:
Acinetobacter baumannii has emerged as a globally important nosocomial pathogen characterized by an increased multi-drug resistance (MDR), leaving limited options for treating its infection. To identify novel antibacterial compounds with activity against clin. isolates of A. baumannii, we performed high-throughput screening against a chem. library of 42,944 compounds using nonpathogenic Escherichia coli MG1655 and identified 55 hit compounds The antibacterial activities of 30 pure compounds were determined against MDR clin. isolates of A. baumannii obtained from Los Angeles County hospitals. Two isothiazolones identified, 5-chloro-2-(4-chloro-3-methylphenyl)-4-methyl-3(2H)-isothiazolone and 5-chloro-2-(4-chlorophenyl)-4-methyl-3(2H)-isothiazolone (I), possess novel structure and exhibited consistent, potent and cidal activity against all 46 MDR A. baumannii clin. isolates and reference strains. Addnl., structure-activity relation anal. involving several addnl. isothiazolones supports the link between a chloro-group on the heterocyclic ring or a fused benzene ring and the cidal activity. Attempts to obtain isothiazolone resistant mutants failed, consistent with the rapid cidal action and indicative of a complex mechanism of action. While cytotoxicity was observed with I, it had a therapeutic index value of 28 suggesting future therapeutic potential. Our results indicate that high-throughput screening of compound libraries followed by in vitro biol. evaluations is a viable approach for the discovery of novel antibacterial agents to contribute in the fight against MDR bacterial pathogens. The experimental process involved the reaction of 2-Methylisothiazol-3(2H)-one hydrochloride(cas: 26172-54-3).Quality Control of 2-Methylisothiazol-3(2H)-one hydrochloride
The Article related to antibacterial activity isothiazolone derivative structure acinetobacter, acinetobacter baumannii, antimicrobial susceptibility testing, cytotoxicity, high-throughput screening, isothiazolone, time-kill assay and other aspects.Quality Control of 2-Methylisothiazol-3(2H)-one hydrochloride
Referemce:
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com