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Synthesis and Antitubercular Activity Evaluation of Novel Unsymmetrical Cyclohexane‐1,2‐diamine Derivatives
Authors:Beena  Seema Joshi  Nitin Kumar  Saqib Kidwai  Ramandeep Singh  Diwan S. Rawat
Affiliation:1. Department of Chemistry, University of Delhi, Delhi, India;2. Translational Health Science and Technology Institute, Vaccine and Infectious Disease Research Centre, Gurgaon, India
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 MIC99. 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.
Keywords:Bromhexine  Cyclohexane‐1,2‐diamine  Hemolysis  Mycobacterium tuberculosis  Tuberculosis
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