Literature DB >> 24144854

Schiff's base derivatives bearing nitroimidazole moiety: new class of antibacterial, anticancer agents and potential EGFR tyrosine kinase inhibitors.

Jigar A Makawana1, Juan Sun, Hai-Liang Zhu.   

Abstract

New Schiff's base derivatives 5a-5h have been synthesized by reaction between 1-(4-bromophenyl)-2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethanone 3 and various benzohydrazide 4a-4h in presence of nickel (II) nitrate as a catalyst in ethanol at room temperature in good yield (54-88%). All compounds were tested for antibacterial as well as anticancer and inhibition of EGFR. Of the compounds studied, compounds 5d, 5f and 5g in the case of antiproliferation and inhibition of EGFR as well as compounds 5b, 5c, 5e and 5h in the case of antibacterial activity were found to be most effective compounds in the series. Compound 5f shows effective inhibition (IC50=0.21±0.02 μM) by binding in to the active pocket of EGFR receptor with minimum binding energy (ΔGb=-49.4869 kcal/mol).
Copyright © 2013 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Antibacterial activity; Anticancer activity; EGFR inhibition; Nitroimidazole; Schiff’s base

Mesh:

Substances:

Year:  2013        PMID: 24144854     DOI: 10.1016/j.bmcl.2013.09.086

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

Review 1.  Functionalized Nitroimidazole Scaffold Construction and Their Pharmaceutical Applications: A 1950-2021 Comprehensive Overview.

Authors:  Ria Gupta; Sumit Sharma; Rohit Singh; Ram A Vishwakarma; Serge Mignani; Parvinder Pal Singh
Journal:  Pharmaceuticals (Basel)       Date:  2022-04-30

Review 2.  An Updated Review on the Synthesis and Antibacterial Activity of Molecular Hybrids and Conjugates Bearing Imidazole Moiety.

Authors:  Renzo Rossi; Maurizio Ciofalo
Journal:  Molecules       Date:  2020-11-04       Impact factor: 4.411

3.  Synthesis and Anticancer and Antimicrobial Evaluation of Novel Ether-linked Derivatives of Ornidazole.

Authors:  Sevil Şenkardeş; Necla Kulabaş; Özlem Bingöl Özakpinar; Sadık Kalayci; Fikrettin Şahin; İlkay Küçükgüzel; Ş Güniz Küçükgüzel
Journal:  Turk J Pharm Sci       Date:  2020-02-19
  3 in total

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