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Virtual screening of synthesized thiazole derivatives for M. tuberculosis and dTDP-rhamnose inhibitors

Title: Virtual screening of synthesized thiazole derivatives for M. tuberculosis and dTDP-rhamnose inhibitors
Authors: Dighe, Rajendra Dnyandeo; Bairagi, Vinod A; Pathade, Parag A; Sonawane, Yogesh T
Source: Journal of Drug Delivery and Therapeutics; Vol. 9 No. 1 (2019): Volume 9, Issue 1 Jan-Feb 2019; 207-210 ; 2250-1177
Publisher Information: Vinita Nagar, Society of Pharmaceutical Technocrats, 1/7756, Street no. 1, East Gorakh Park, Shahdara, Delhi, India 110032
Publication Year: 2019
Collection: Journal of Drug Delivery and Therapeutics (JDDT)
Description: To determine antimycobacterium and dTDP rhamnose inhibitor activity of the synthesized azetidinone, thiazolidinone derivatives of thiazole, we studied different derivatives for the activity. One pot synthesis of 2-amino-4-methylthiazole-5-carboxylic acid ethyl ester has been carried out and synthesized different derivative compounds. Compounds were tested for antimicrobial activity against different strains of microorganism and antitubercular activity against M. tuberculosis H37Rv. Compounds 7c, 7d, 7i, 8d, 8e, 8g and 8h, were showed antimicrobial activity against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Salmonella typhosa using Gentamycin as standard, while 7b, 7e, 7f, 7i, 8b, 8e, 8f and 8i showed very strong antimycobacterial activity using rifampicine as a standard. Thiazole derivatives especially with carbonyl group scaffold inhibit an enzyme RmlC, which is an essential component for the biosynthesis of dTDP-rhamnose and produce good antimycobacterium and antimicrobial activity. Keywords: Thiazole, thiazolidinone derivatives, azetidinone derivative, well diffusion method, broth microdilution assay, antitubercular activity, antimicrobial activity.
Document Type: article in journal/newspaper
File Description: application/pdf
Language: English
Relation: http://jddtonline.info/index.php/jddt/article/view/2324/1667; http://jddtonline.info/index.php/jddt/article/view/2324
DOI: 10.22270/jddt.v9i1.2324
Availability: http://jddtonline.info/index.php/jddt/article/view/2324; https://doi.org/10.22270/jddt.v9i1.2324
Rights: Copyright (c) 2019 Journal of Drug Delivery and Therapeutics
Accession Number: edsbas.E6912AF3
Database: BASE