Literature DB >> 28756265

4-Aminoquinoline-chalcone/-N-acetylpyrazoline conjugates: Synthesis and antiplasmodial evaluation.

Sumit Kumar1, Anu Saini1, Jiri Gut2, Philip J Rosenthal2, Raghu Raj3, Vipan Kumar4.   

Abstract

1H-1,2,3-triazole linked 4-aminoquinoline-chalcone/-N-acetylpyrazoline conjugates were synthesized and evaluated against cultured chloroquine (CQ) resistant strain. Antiplasmodial activities of the synthesized conjugates revealed dependence of activity on the length of the alkyl chain as well as on the presence of methoxy substituents on ring A/ring B of the chalcone. The most potent and non-cytotoxic conjugate showed comparable antiplasmodial activity with that of CQ, with an IC50 value of 53.7 nM.
Copyright © 2017 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  4-Aminoquinoline; Antiplasmodial; Chalcone; Click chemistry; N-acetylpyrazoline

Mesh：

Substances：

Year:  2017        PMID： 28756265     DOI： 10.1016/j.ejmech.2017.07.041

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


  9 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.  1H-1,2,3-Triazole Tethered Nitroimidazole-Isatin Conjugates: Synthesis, Docking, and Anti-Proliferative Evaluation against Breast Cancer.

Authors:  Sumit Kumar; Sourav Taru Saha; Liang Gu; Gabriella Palma; Shanen Perumal; Ashona Singh-Pillay; Parvesh Singh; Amit Anand; Mandeep Kaur; Vipan Kumar
Journal:  ACS Omega       Date:  2018-09-27

3.  Highly Potent 1H-1,2,3-Triazole-Tethered Isatin-Metronidazole Conjugates Against Anaerobic Foodborne, Waterborne, and Sexually-Transmitted Protozoal Parasites.

Authors:  Sumit Kumar; Trpta Bains; Ashley Sae Won Kim; Christina Tam; Jong Kim; Luisa W Cheng; Kirkwood M Land; Anjan Debnath; Vipan Kumar
Journal:  Front Cell Infect Microbiol       Date:  2018-10-30       Impact factor: 5.293

Review 4.  Ferrocene-Based Compounds with Antimalaria/Anticancer Activity.

Authors:  Sijongesonke Peter; Blessing Atim Aderibigbe
Journal:  Molecules       Date:  2019-10-07       Impact factor: 4.411

Review 5.  Recent Advances in Bioactive Flavonoid Hybrids Linked by 1,2,3-Triazole Ring Obtained by Click Chemistry.

Authors:  Daniela Pereira; Madalena Pinto; Marta Correia-da-Silva; Honorina Cidade
Journal:  Molecules       Date:  2021-12-30       Impact factor: 4.411

6.  Synthesis, anti-mycobacterial and cytotoxic evaluation of substituted isoindoline-1,3-dione-4-aminoquinolines coupled via alkyl/amide linkers.

Authors:  Anu Rani; Albertus Viljoen; Matt D Johansen; Laurent Kremer; Vipan Kumar
Journal:  RSC Adv       Date:  2019-03-13       Impact factor: 4.036

7.  Quinoline-triazole hybrids inhibit falcipain-2 and arrest the development of Plasmodium falciparum at the trophozoite stage.

Authors:  Anju Singh; Md Kalamuddin; Asif Mohmmed; Pawan Malhotra; Nasimul Hoda
Journal:  RSC Adv       Date:  2019-11-29       Impact factor: 3.361

Review 8.  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

9.  Design, Synthesis and Preliminary Antimicrobial Evaluation of N-Alkyl Chain Tethered C-5 Functionalized Bis-Isatins.

Authors:  Amandeep Singh; Trpta Bains; Hye Jee Hahn; Nicole Liu; Christina Tam; Luisa W Cheng; Jong Kim; Anjan Debnath; Kirkwood M Land; Vipan Kumar
Journal:  Medchemcomm       Date:  2017-09-19       Impact factor: 3.597
  9 in total

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