Literature DB >> 30064024

Synthesis and biological evaluation of dihydroquinoline carboxamide derivatives as anti-tubercular agents.

Gautam Kumar1, Asawari Sathe1, Vagolu Siva Krishna2, Dharmarajan Sriram2, Sanjay M Jachak3.   

Abstract

Sodium trifluoromethanesulfonate, and glacial acetic acid selectively catalyzed the synthesis of dihydroquinoline via Friedländer annulation. The synthesized dihydroquinoline analogues coupled with different amines by the use of coupling reagent gave dihydroquinoline carboxamide derivatives in moderate to good yields. All the synthesized novel compounds were evaluated for the anti-tubercular activity and cytotoxic activities in vitro. Among tested 30 compounds, two compounds, 8g and 8h showed MIC value of 0.39 and 0.78 μg/mL, respectively against Mycobacterium tuberculosis H37Rv and they were found to be non-toxic. Also these two compounds exhibited good pharmacological properties and oral absorption when studied using in-silico models.
Copyright © 2018 Elsevier Masson SAS. All rights reserved.

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Keywords:  ADME; Anti-tubercular activity; Dihydroquinoline; Friedländer synthesis; Sodium trifluoromethanesulfonate

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Year:  2018        PMID: 30064024     DOI: 10.1016/j.ejmech.2018.07.046

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  2 in total

1.  Application of 2,4-bis(halomethyl)quinoline: synthesis and biological activities of 2,4-bis(benzofuran-2-yl)- and 2,4-bis(aroxymethyl)quinolines.

Authors:  Yang Li; Qiqi Xu; Zhiyuan Li; Wentao Gao; Yu Chen
Journal:  Mol Divers       Date:  2019-03-20       Impact factor: 2.943

Review 2.  Quinoline derivatives volunteering against antimicrobial resistance: rational approaches, design strategies, structure activity relationship and mechanistic insights.

Authors:  Nitish Kumar; Aanchal Khanna; Komalpreet Kaur; Harmandeep Kaur; Anchal Sharma; Preet Mohinder Singh Bedi
Journal:  Mol Divers       Date:  2022-10-05       Impact factor: 3.364

  2 in total

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