title: Design, synthesis and antimycobacterial evaluation of 1-(4-(2-substitutedthiazol-4-yl)phenethyl)-4-(3-(4-substitutedpiperazin-1-yl)alkyl)piperazine hybrid analogues.
abstract: 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.
authors: Department of Chemistry, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, R.R. District, 500078, Telangana, India.
authors: Hunsur Nagendra
authors: HN
authors: Nagesh
authors: Department of Chemistry, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, R.R. District, 500078, Telangana, India.
authors: Amaroju
authors: A
authors: Suresh
authors: Department of Chemistry, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, R.R. District, 500078, Telangana, India.
authors: Sirigina Devesh Sathya Sri
authors: SD
authors: Sairam
authors: Department of Pharmacy, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, R.R. District, 500078, Telangana, India.
authors: Dharmarajan
authors: D
authors: Sriram
authors: Department of Pharmacy, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, R.R. District, 500078, Telangana, India.
authors: Perumal
authors: P
authors: Yogeeswari
authors: 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.
authors: Kondapalli Venkata Gowri
authors: KV
authors: Chandra Sekhar
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D051379:Mice; D008807:Mice, Inbred BALB C; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D010879:Piperazines
keywords: Alkyl linker; Antimycobacterial activity; Piperazine; Thiazole