Synthesis of coumarin-theophylline hybrids as a new class of anti-tubercular and anti-microbial agents.

Autor: Mangasuli SN; Department of Studies in Chemistry, Karnatak University, Dharwad, 580003, India., Hosamani KM; Department of Studies in Chemistry, Karnatak University, Dharwad, 580003, India. Electronic address: dr_hosamani@yahoo.com., Devarajegowda HC; Department of Physics, Yuvaraja's College, University of Mysore, Mysore 570005, India., Kurjogi MM; Department of Studies in Microbiology & Biotechnology, Karnatak University, Dharwad, 580003, India., Joshi SD; Novel Drug Design and Discovery Laboratory, Department of Pharmaceutical Chemistry, S.E.T's College of Pharmacy, Sangolli Rayanna Nagar, Dharwad, 580002 Karnataka, India.
Jazyk: angličtina
Zdroj: European journal of medicinal chemistry [Eur J Med Chem] 2018 Feb 25; Vol. 146, pp. 747-756. Date of Electronic Publication: 2018 Jan 10.
DOI: 10.1016/j.ejmech.2018.01.025
Abstrakt: A series of novel coumarin-theophylline hybrids were synthesized and examined for their anti-tubercular activity in vitro against Mycobacterium tuberculosis H 37 Rv, anti-microbial activity in vitro against gram-positive bacteria (Staphylococcus aureus) and gram-negative bacterias (Escherichia coli, Salmonella typhi) as well as fungi (Candida albicans). The compound (3a) has shown excellent anti-tubercular activity with MIC of 0.12 μg/mL. Electron donating compounds (3a, 3f) have displayed significant anti-microbial activity. The compounds have also been precisely elucidated using single crystal X-ray diffraction techniques. Molecular docking study has been performed against 4DQU enzyme of Mycobacterium tuberculosis showed good binding interactions and is in agreement with the in vitro results.
(Copyright © 2018. Published by Elsevier Masson SAS.)
Databáze: MEDLINE
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