Literature DB >> 21376586

Design, synthesis and antimycobacterial activity of cinnamide derivatives: a molecular hybridization approach.

Manoj D Kakwani1, Prashant Suryavanshi, Muktikant Ray, M G R Rajan, Sharmila Majee, Abdul Samad, Padma Devarajan, Mariam S Degani.   

Abstract

A series of cinnamide derivatives was designed as potential antimycobacterial agents using molecular hybridization approach. The diamine moiety, a key feature of ethambutol and its other analogs, and certain structural features of cerulenin and cinnamic acid were hybridized to obtain cinnamide derivatives. The minimum inhibitory concentration (MIC) of all synthesized compounds was determined against M. tuberculosis H(37)R(v) using Resazurin Microtitre plate Assay (REMA) method. The synthesized molecules showed good to moderate activity with MIC in the range of 5-150 μM and good safety profile. Additionally, the most potent compound 1a, having MIC 5.1 μM exhibited synergy with rifampicin.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21376586     DOI: 10.1016/j.bmcl.2011.02.022

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


  8 in total

1.  An orally antitumor chalcone hybrid inhibited HepG2 cells growth and migration as the tubulin binding agent.

Authors:  Wang Yan; Chen Xiangyu; Li Ya; Wang Yu; Xu Feng
Journal:  Invest New Drugs       Date:  2019-02-11       Impact factor: 3.850

2.  Discovery and anticancer evaluation of a formononetin derivative against gastric cancer SGC7901 cells.

Authors:  Jian-Ning Yao; Xue-Xiu Zhang; Yan-Zhen Zhang; Jia-Heng Li; Dong-Yao Zhao; Bing Gao; Hai-Ning Zhou; Shi-Lin Gao; Lian-Feng Zhang
Journal:  Invest New Drugs       Date:  2019-03-30       Impact factor: 3.850

3.  Design, Synthesis and Biological Evaluation of Novel Primaquine-Cinnamic Acid Conjugates of the Amide and Acylsemicarbazide Type.

Authors:  Kristina Pavić; Ivana Perković; Petra Gilja; Filip Kozlina; Katja Ester; Marijeta Kralj; Dominique Schols; Dimitra Hadjipavlou-Litina; Eleni Pontiki; Branka Zorc
Journal:  Molecules       Date:  2016-11-28       Impact factor: 4.411

4.  Cinnamoyl-Oxaborole Amides: Synthesis and Their in Vitro Biological Activity.

Authors:  Maureen Gumbo; Richard M Beteck; Tawanda Mandizvo; Ronnett Seldon; Digby F Warner; Heinrich C Hoppe; Michelle Isaacs; Dustin Laming; Christina C Tam; Luisa W Cheng; Nicole Liu; Kirkwood M Land; Setshaba D Khanye
Journal:  Molecules       Date:  2018-08-15       Impact factor: 4.411

Review 5.  Primaquine derivatives: Modifications of the terminal amino group.

Authors:  Branka Zorc; Ivana Perković; Kristina Pavić; Zrinka Rajić; Maja Beus
Journal:  Eur J Med Chem       Date:  2019-08-23       Impact factor: 6.514

6.  Synthesis and characterization of piperazine-substituted dihydrofuran derivatives viaMn(OAc) 3 mediated radical cyclizations.

Authors:  Sait Sari; Mehmet Yilmaz
Journal:  Turk J Chem       Date:  2020-10-26       Impact factor: 1.239

7.  Asymmetric Primaquine and Halogenaniline Fumardiamides as Novel Biologically Active Michael Acceptors.

Authors:  Zrinka Rajić; Maja Beus; Hana Michnová; Josipa Vlainić; Leentje Persoons; Ivan Kosalec; Josef Jampílek; Dominique Schols; Toma Keser; Branka Zorc
Journal:  Molecules       Date:  2018-07-14       Impact factor: 4.411

8.  Cinnamic Derivatives as Antitubercular Agents: Characterization by Quantitative Structure-Activity Relationship Studies.

Authors:  Cátia Teixeira; Cristina Ventura; José R B Gomes; Paula Gomes; Filomena Martins
Journal:  Molecules       Date:  2020-01-21       Impact factor: 4.411

  8 in total

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