Searching for New Cures for Tuberculosis: Design, Synthesis, and Biological Evaluation of 2-Methylbenzothiazoles was written by Huang, Qingqing;Mao, Jialin;Wan, Baojie;Wang, Yuehong;Brun, Reto;Franzblau, Scott G.;Kozikowski, Alan P.. And the article was included in Journal of Medicinal Chemistry in 2009.Category: chlorides-buliding-blocks The following contents are mentioned in the article:
The actual development and clin. use of new therapeutics for tuberculosis have remained stagnant for years because of the complexity of the disease process, the treatment of which at present requires the administration of drug combinations over a 6 mo period. In this study, the chem. and biol. of a series of potent 5-(2-methylbenzothiazol-5-yloxymethyl)isoxazole-3-carboxamides, e.g. I [R = Me2N, 1-piperidinyl, (S)-MeO2CCH(Ph)NH, etc.] , which proved to be active against replicating Mycobacterium tuberculosis (Mtb) H37Rv, are reported. The most potent compounds I [R = (S)- or (R)-MeO2CCH(Ph)NH] were found to inhibit Mtb growth at micromolar concentrations, with MIC values of 1.4 and 1.9 μM, resp. Impressively, all active compounds were nontoxic toward Vero cells (IC50 > 128 μM). Moreover, the best of these compounds were also tested against protozoan parasites, and some of these compounds were found to show activity, especially against Plasmodium falciparum. These studies thus suggest that certain 2-methylbenzothiazole based compounds may serve as promising lead scaffolds for further elaboration as antitubercular drugs and as possible antimalaria drugs. This study involved multiple reactions and reactants, such as (S)-Methyl 2-amino-2-(2-chlorophenyl)acetate (cas: 141109-14-0Category: chlorides-buliding-blocks).
(S)-Methyl 2-amino-2-(2-chlorophenyl)acetate (cas: 141109-14-0) belongs to organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage.Category: chlorides-buliding-blocks
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics