title: Design, synthesis and evaluation of 6-(4-((substituted-1H-1,2,3-triazol-4-yl)methyl)piperazin-1-yl)phenanthridine analogues as antimycobacterial agents.
abstract: Focus in this Letter is made to design and synthesize a series of nineteen new 6-(4-((substituted-1H-1,2,3-triazol-4-yl)methyl)piperazin-1-yl)phenanthridine analogues employing click chemistry and evaluated for their anti-tubercular activity against Mycobacterium tuberculosis H37Rv. Among the tested compounds, 7f and 7 j exhibited good activity (MIC = 3.125 μg/mL), while 8a displayed excellent activity (MIC = 1.56 μg/mL) against the growth of M. tuberculosis H37Rv. In addition, 7f, 7 j and 8a compounds were subjected to cytotoxic studies against mouse macrophage (RAW264.7) cell lines and the selectivity index values are >15 indicating suitability of compounds for further drug development.
authors.affiliation: Department of Chemistry, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, R.R. District 500078, Andhra Pradesh, India.
authors.forename: Hunsur Nagendra
authors.initials: HN
authors.lastname: Nagesh
authors.forename: Kalaga Mahalakshmi
authors.initials: KM
authors.lastname: Naidu
authors.forename: Damarla Harika
authors.initials: DH
authors.lastname: Rao
authors.forename: Jonnalagadda Padma
authors.initials: JP
authors.lastname: Sridevi
authors.forename: Dharmarajan
authors.initials: D
authors.lastname: Sriram
authors.forename: Perumal
authors.initials: P
authors.lastname: Yogeeswari
authors.forename: Kondapalli Venkata Gowri
authors.initials: KV
authors.lastname: Chandra Sekhar
mesh_terms: D000818:Animals; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D057930:Click Chemistry; D015195:Drug Design; D051379:Mice; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D010617:Phenanthridines / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D000077489:Piperazine; D010879:Piperazines / Q000737:chemistry*; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry*
chemical_list: D000995:Antitubercular Agents; D010617:Phenanthridines; D010879:Piperazines; D014230:Triazoles; D000077489:Piperazine
keywords: Anti-tubercular activity; Click chemistry; Phenanthridine; Piperazine; Triazole