Literature DB >> 26114811

Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids.

Hardeep Kaur1, Jan Balzarini2, Carmen de Kock3, Peter J Smith3, Kelly Chibale4, Kamaljit Singh5.   

Abstract

A series of hybrids comprising of 5-cyanopyrimidine and quinoline moiety were synthesized and tested for in vitro antiplasmodial activity against NF54 and Dd2 strains of Plasmodium falciparum. Hybrid bearing m-nitrophenyl substituent at C-4 of pyrimidine displayed the highest antiplasmodial activity [IC50 = 56 nM] against the CQ(R) (Dd2) strain, which is four-fold greater than CQ.
Copyright © 2015 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  4-Aminoquinoline; Antiplasmodial agents; Cytotoxic activity; Heme binding; Hybrid antimalarials; Pyrimidine

Mesh:

Substances:

Year:  2015        PMID: 26114811     DOI: 10.1016/j.ejmech.2015.06.024

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


  5 in total

1.  Synthesis and molecular docking of new N4-piperazinyl ciprofloxacin hybrids as antimicrobial DNA gyrase inhibitors.

Authors:  Hamada H H Mohammed; Doaa Mohamed Elroby Ali; Mohamed Badr; Ahmed G K Habib; Abobakr Mohamed Mahmoud; Sarah M Farhan; Shimaa Salah Hassan Abd El Gany; Soad A Mohamad; Alaa M Hayallah; Samar H Abbas; Gamal El-Din A Abuo-Rahma
Journal:  Mol Divers       Date:  2022-09-24       Impact factor: 3.364

Review 2.  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

Review 3.  Combination Therapy Strategies for the Treatment of Malaria.

Authors:  Sibusiso Alven; Blessing Aderibigbe
Journal:  Molecules       Date:  2019-10-07       Impact factor: 4.411

4.  Novel camphor-based pyrimidine derivatives induced cancer cell death through a ROS-mediated mitochondrial apoptosis pathway.

Authors:  Yan Zhang; Yunyun Wang; Yuxun Zhao; Wen Gu; Yongqiang Zhu; Shifa Wang
Journal:  RSC Adv       Date:  2019-09-19       Impact factor: 4.036

5.  Design and Synthesis of New Pyrimidine-Quinolone Hybrids as Novel hLDHA Inhibitors.

Authors:  Iván Díaz; Sofia Salido; Manuel Nogueras; Justo Cobo
Journal:  Pharmaceuticals (Basel)       Date:  2022-06-24
  5 in total

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