2. Academic Validation
  3. Design, synthesis and evaluation of diarylpiperazine derivatives as potent anti-tubercular agents

Design, synthesis and evaluation of diarylpiperazine derivatives as potent anti-tubercular agents

  • Eur J Med Chem. 2015 Nov 13:105:238-44. doi: 10.1016/j.ejmech.2015.10.024.
Ashok Penta 1,  Scott Franzblau 2,  Baojie Wan 2,  Sankaranarayanan Murugesan 3
Affiliations

Affiliations

  • 1 Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology & Science, Pilani, 333031, India.
  • 2 Institute for Tuberculosis Research, MC-964 College of Pharmacy, University of Illino's at Chicago, 833 S. Wood St, Chicago, IL, 60621-7231, USA.
  • 3 Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology & Science, Pilani, 333031, India. Electronic address: murugesan@pilani.bits-pilani.ac.in.
PMID: 26498570 DOI: 10.1016/j.ejmech.2015.10.024
Abstract

Molecular hybridization is an emerging approach to design novel ligands by combination of two or more pharmacophoric subunits of known bioactive compounds. In the present study, we have designed a novel series of diarylpiperazine analogues, synthesized, characterized using FTIR, (1)H NMR, Mass, Elemental analysis and evaluated their in-vitro anti-tubercular activity. Among the reported sixteen diarylpiperazines, eleven analogues exhibited significant anti-tubercular activity against Mycobacterium tuberculosis H37Rv strain with MIC values below 6.25 μg/mL and good selectivity index. Structure activity relationship studies concluded that, ortho-para directing group (except para chloro) substitution on ortho and para position of piperazine attached phenyl ring favored anti-tubercular activity.

Keywords

Mycobacterium tuberculosis; Piperazine; β-carboline.

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