title: Synthesis and antitubercular activity evaluation of novel unsymmetrical cyclohexane-1,2-diamine derivatives.
abstract: A library of unsymmetrical cyclohexane-1,2-diamine derivatives were synthesized and evaluated for their activity against Mycobacterium tuberculosis H37Rv in vitro. Out of the 46 compounds synthesized, eight compounds (11h, 13a, 13e, 13f, 14a, 14c, 14d, and 15d) were found to be active at or below 6.25 µM concentration, with negligible toxicity to human red blood cells at a concentration much higher than the MIC(99) . Compound 13a was the best active compound showing inhibition at 3.125-6.25 µM, and was found to be non-hemolytic up to 500 µg/mL concentration.
authors.affiliation: Department of Chemistry, University of Delhi, Delhi, India.
authors.lastname: Beena
authors.forename: Seema
authors.initials: S
authors.lastname: Joshi
authors.forename: Nitin
authors.initials: N
authors.lastname: Kumar
authors.forename: Saqib
authors.initials: S
authors.lastname: Kidwai
authors.forename: Ramandeep
authors.initials: R
authors.lastname: Singh
authors.forename: Diwan S
authors.initials: DS
authors.lastname: Rawat
mesh_terms: D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D003510:Cyclohexanes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D003959:Diamines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D013329:Structure-Activity Relationship; D018675:Toxicity Tests / Q000379:methods
chemical_list: D000995:Antitubercular Agents; D003510:Cyclohexanes; D003959:Diamines