Literature DB >> 24287561

Urea/oxalamide tethered β-lactam-7-chloroquinoline conjugates: synthesis and in vitro antimalarial evaluation.

Pardeep Singh1, Raghu Raj1, Parvesh Singh2, Jiri Gut3, Philip J Rosenthal3, Vipan Kumar4.   

Abstract

The manuscript pertains to the synthesis of urea/oxalamide tethered β-lactam-7-chloroquinoline conjugates with well modulated chain lengths and their antimalarial evaluation. The results reveal the dependence of activity profiles on the N-1 substituent of the β-lactam ring, the nature of the linker as well as the length of the alkyl chain. The most potent of the tested compounds showed an IC50 of 34.97 nM against chloroquine resistant W2 strain of Plasmodium falciparum.
Copyright © 2013 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Antimalarial evaluation; Structure–activity relationship; Urea/oxalamide linker; β-Lactam-7-chloroquinoline conjugates

Mesh:

Substances:

Year:  2013        PMID: 24287561     DOI: 10.1016/j.ejmech.2013.10.079

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


  4 in total

1.  Urea Derivatives in Modern Drug Discovery and Medicinal Chemistry.

Authors:  Arun K Ghosh; Margherita Brindisi
Journal:  J Med Chem       Date:  2019-12-02       Impact factor: 7.446

2.  1-[3-(Morpholin-4-yl)prop-yl]-4-(3-nitro-phen-yl)spiro-[azetidine-3,9'-xanthen]-2-one.

Authors:  Ismail Celik; Mehmet Akkurt; Aliasghar Jarrahpour; Roghayeh Heiran; Namık Ozdemir
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2014-02-28

Review 3.  Quinoline-Based Hybrid Compounds with Antimalarial Activity.

Authors:  Xhamla Nqoro; Naki Tobeka; Blessing A Aderibigbe
Journal:  Molecules       Date:  2017-12-19       Impact factor: 4.411

4.  β-amino-alcohol tethered 4-aminoquinoline-isatin conjugates: synthesis and antimalarial evaluation.

Authors:  Jiri Gut; Philip J Rosenthal; Vipan Kumar
Journal:  Eur J Med Chem       Date:  2014-07-21       Impact factor: 6.514

  4 in total

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