Design, synthesis and antimycobacterial evaluation of 1-(4-(2-substitutedthiazol-4-yl)phenethyl)-4-(3-(4-substitutedpiperazin-1-yl)alkyl)piperazine hybrid analogues.

Autor: Nagesh HN; Department of Chemistry, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, R.R. District, 500078, Telangana, India., Suresh A; Department of Chemistry, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, R.R. District, 500078, Telangana, India., Sairam SD; Department of Chemistry, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, R.R. District, 500078, Telangana, India., Sriram D; Department of Pharmacy, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, R.R. District, 500078, Telangana, India., Yogeeswari P; Department of Pharmacy, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, R.R. District, 500078, Telangana, India., Chandra Sekhar KV; Department of Chemistry, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, R.R. District, 500078, Telangana, India. Electronic address: kvgc@hyderabad.bits-pilani.ac.in.
Jazyk: angličtina
Zdroj: European journal of medicinal chemistry [Eur J Med Chem] 2014 Sep 12; Vol. 84, pp. 605-13. Date of Electronic Publication: 2014 Jul 21.
DOI: 10.1016/j.ejmech.2014.07.067
Abstrakt: A series of twenty six new 1-(4-(2-substitutedthiazol-4-yl)phenethyl)-4-(3-(4-substitutedpiperazin-1-yl)alkyl)piperazine analogues were synthesized by seven steps and evaluated for their anti-tubercular activity against Mycobacterium tuberculosis H37Rv strain. Among the tested compounds, 7j, 7p, and 7r exhibited moderate activity (MIC = 6.25 μg/mL) and compounds 7a, 7f, 7g, 7n and 7v exhibited good activity (MIC = 3.125 μg/mL), while 7h displayed excellent activity (MIC = 1.56 μg/mL) by inhibiting 99% growth of M. tuberculosis H37Rv strain. In addition, all the active compounds were subjected to cytotoxic studies against mouse macrophage (RAW264.7) cell lines and the selectivity index values for most of the compounds is >10 indicating suitability of compounds in an endeavour to attain lead molecule for further drug development.
(Copyright © 2014 Elsevier Masson SAS. All rights reserved.)
Databáze: MEDLINE
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