Literature DB >> 31518758

Variedly connected 1,8-naphthalimide-7-chloroquinoline conjugates: Synthesis, anti-mycobacterial and cytotoxic evaluation.

Matt D Johansen1, Laurent Kremer2, Vipan Kumar3.   

Abstract

Recent disclosures about anti-bacterial and anti-tubercular potential of naphthalimide and quinoline core respectively propelled us to synthesize a library of 1,8-naphthalimide-7-chloroquinoline hybrids. Different modes of linkage between two pharmacophoric units viz. simple alkyl chains and induction of amide bond were used and the substituents on the naphthalimide core were varied in order to determine Structure-Activity-Relationship (SAR). Our findings demonstrated that simple alkyl chain linked conjugates showed better activity profiles without any cytotoxicity, while the inclusion of amide bond enhanced the cytotoxic tendency. An interesting behaviour of conjugates in terms of activity and cytotoxicity was observed via switching over the nature of linker between two pharmacophores.
Copyright © 2019 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  1,8-Naphthalic anhydride; 7-Chloroquinoline; Anti-mycobacterial; Cytotoxicity; Structure-activity relationship

Year:  2019        PMID: 31518758     DOI: 10.1016/j.bioorg.2019.103241

Source DB:  PubMed          Journal:  Bioorg Chem        ISSN: 0045-2068            Impact factor:   5.275


  2 in total

1.  Functionalized Naphthalimide-4-aminoquinoline Conjugates as Promising Antiplasmodials, with Mechanistic Insights.

Authors:  Jenny Legac; Adebayo A Adeniyi; Prishani Kisten; Philip J Rosenthal; Parvesh Singh; Vipan Kumar
Journal:  ACS Med Chem Lett       Date:  2020-01-08       Impact factor: 4.345

2.  A Multifunctional and Fast-Response Lysosome-Targetable Fluorescent Probe for Monitoring pH and Isoxaflutole.

Authors:  Liu Yang; Yan Liu; Mingli Yue; Ping Li; Yulong Liu; Fei Ye; Ying Fu
Journal:  Int J Mol Sci       Date:  2022-06-02       Impact factor: 6.208

  2 in total

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