Literature DB >> 31740250

Synthesis, anti-plasmodial and cytotoxic evaluation of 1H-1,2,3-triazole/acyl hydrazide integrated tetrahydro-β-carboline-4-aminoquinoline conjugates.

Bharvi Sharma1, Simranjeet Kaur1, Jenny Legac2, Philip J Rosenthal2, Vipan Kumar3.   

Abstract

A series of 1H-1,2,3-triazole/acylhydrazide-tethered tetrahydro-β-carboline-4-aminoquinoline conjugates was synthesized with an aim to study their anti-plasmodial structure-activity relationship. The presence of 1H-1,2,3-triazole-core along with a flexible alkyl chain length on aminoquinoline core has favourable influence on the anti-plasmodial activity against Chloroquine-resistant W2 strain of P. falciparum while the introduction of hydrazine core not only diminished the activities but also resulted in increased cytotoxicity against mammalian Vero cells.
Copyright © 2019 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Acyl hydrazide; Antiplasmodial; Quinoline; Tetrahydro-β-carboline; Triazole

Mesh:

Substances:

Year:  2019        PMID: 31740250     DOI: 10.1016/j.bmcl.2019.126810

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


  2 in total

1.  Probing the B- & C-rings of the antimalarial tetrahydro-β-carboline MMV008138 for steric and conformational constraints.

Authors:  Sha Ding; Maryam Ghavami; Joshua H Butler; Emilio F Merino; Carla Slebodnick; Maria B Cassera; Paul R Carlier
Journal:  Bioorg Med Chem Lett       Date:  2020-09-06       Impact factor: 2.823

Review 2.  Phthalimide analogs for antimalarial drug discovery.

Authors:  Meenakshi Bansal; Charu Upadhyay; Sumit Kumar; Brijesh Rathi
Journal:  RSC Med Chem       Date:  2021-08-13
  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.