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Hajjaj H. M. Abdu-Allah,Bahaa G. M. Youssif,Mostafa H. Abdelrahman,Mohammed K. Abdel-Hamid,Rudraraju Srilakshmi Reshma,Perumal Yogeeswari,Tarek Aboul-Fadl,Dharmarajan Sriram 대한약학회 2017 Archives of Pharmacal Research Vol.40 No.2
The antitubercular drug; para-aminosalicylicacid (PAS) was used as the core scaffold for the design of aseries of 1H-1,2,3-triazolylsalicylhydrazones upon couplingwith triazole and arylhydrazone moietis to furnish asingle molecular architecture. The obtained derivativeswere screened against Mycobacterium tuberculosis H37Rvrevealing good to high activity for the active compounds(MIC values of 0.39–1.5 lg/mL) compared to the marketeddrugs isoniazid, rifampicin and ethambutol. Moreover, themost active analogue N-(1-(4-chlorobenzyl)-2-oxoindolin-3-ylidene)-2-hydroxy-4-(4-phenyl-1H-1,2,3-triazol-1-yl)-benzohydrazide (20) was found to be ten-fold more potentthan PAS and equipotent to rifampicin (MIC 0.39 lg/mL),while exhibiting low cytotoxicity with a selectivity indexof[128. In addition, this compound was shown to beactive against persistent forms of mycobacteria comparableto standard drugs in nutrient starvation model. Accordingly,we introduce compound 20 as a valuable lead forfurther development. A 3D-QSAR study was also conductedto help in explaining the observed activity and toserve as a tool for further development.