Publications by authors named "Bhookya Shankar"

2 Publications

  • Page 1 of 1

Synthesis, anti-microbial activity, cytotoxicity of some novel substituted (5-(3-(1H-benzo[d]imidazol-2-yl)-4-hydroxybenzyl)benzofuran-2-yl)(phenyl)methanone analogs.

Chem Cent J 2018 Jan 9;12(1). Epub 2018 Jan 9.

Molecular Modelling and Medicinal Chemistry Group, Department of Chemistry, Osmania University, Hyderabad, Telangana, India.

Background: There is a dire need for the discovery and development of new antimicrobial agents after several experiments for a better resistance of microorganisms towards antimicrobial agents become a serious health problem for a few years in the past. As benzimidazole possess various types of biological activities, it has been synthesized, in the present study, a new series of (5-(3-(1H-benzo[d]imidazol-2-yl)-4-hydroxybenzyl)benzofuran-2-yl)(phenyl)methanone analogs by using the condensation and screened for its in vitro antimicrobial activity and cytotoxicity.

Results: The synthesized (5-(3-(1H-benzo[d]imidazol-2-yl)-4-hydroxybenzyl) benzofuran-2-yl)(phenyl)methanone analogs were confirmed by IR, H and C-NMR, MS spectra and HRMS spectral data. The synthesized compounds were evaluated for their in vitro antimicrobial potential against Gram-positive (Bacillus subtilis, Bacillus megaterium, Staph aureus and Streptococcus pyogenes), Gram-negative (Escherichia coli, Proteus vulgaris, Proteus mirabilis and Enterobacter aerogenes) bacterial and fungal (Aspergillus niger, Candida albicans, Fusarium oxysporum, Fusarium solani) strains by disc diffusion method and the minimum inhibitory concentration (MIC) in which it has been recorded in microgram per milliliter in comparison to the reference drugs, ciprofloxacin (antibacterial) and nystatin (antifungal). Further, the cytotoxicity (IC value) has also been assessed on human cervical (HeLa), Supt1 cancer cell lines by using MTT assay.

Conclusions: The following screened compounds (4d), (4f), (4g), (4k), (4l), (4o) and (4u) were found to be the best active against all the tested bacterial and fungal strains among all the demonstrated compounds of biological study. The MIC determination was also carried out against bacteria and fungi, the compounds (4f) and (4u) are found to be exhibited excellent potent against bacteria and fungi respectively. The compounds (4f) and (4u) were shown non-toxic in nature after screened for cytotoxicity against the cancer cell lines of human cervical (HeLa) and Supt1. Additionally, structure and antibacterial activity relationship were also further supported by in silico molecular docking studies of the active compounds against DNA topoisomerase.
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http://dx.doi.org/10.1186/s13065-017-0364-3DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5760494PMC
January 2018

Synthesis of -butyl (substituted benzamido)phenylcarbamate derivatives: anti-inflammatory activity and docking studies.

J Chem Biol 2017 Jul 5;10(3):105-115. Epub 2017 Apr 5.

Department of Biochemistry, University College of Science, Osmania University, Hyderabad, Telangana 500007 India.

A series of new -butyl 2-(substituted benzamido) phenylcarbamate - were synthesized by the condensation of -butyl 2-amino phenylcarbamate () with various substituted carboxylic acid in the presence of EDCI and HOBt as coupling reagent, obtain in excellent yields. The structures of all newly synthesized compounds were characterized spectroscopically and evaluated for in vivo anti-inflammatory activity compared to the standard drug, indomethacin, by using the carrageenan-induced rat paw edema protocol. Most of the compounds exhibited a promising anti-inflammatory activity within 9 to 12 h, the percentage of inhibition values ranging from 54.239 to 39.021%. The results revealed that the compounds and exhibited better or equivalent anti-inflammatory activity with the percentage of inhibition of 54.239 and 54.130%, respectively, which was comparable to standard drug. In addition to experimental results, in silico docking studies was used as a tool to verify and expand the experimental outcomes.
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http://dx.doi.org/10.1007/s12154-017-0168-xDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5480262PMC
July 2017
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