Design, synthesis and evaluation of novel pyrrole-hydroxybutenolide hybrids as promising antiplasmodial and anti-inflammatory agents.

Animals Mice Antimalarials / pharmacology Chloroquine / pharmacology Plasmodium falciparum Monocytes Anti-Inflammatory Agents / pharmacology
Antiinflammatory activity Antimalarial activity CQ-Resistant CQ-Sensitive Carrageenan Hu-TNFα Luciferase assay Plasmodium falciparum Plasmodium yoelli Pyrrole-hydroxybutenolides

Journal

European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510

Informations de publication

Date de publication:
05 Jun 2023
Historique:
received: 27 01 2023
revised: 27 03 2023
accepted: 02 04 2023
medline: 8 5 2023
pubmed: 14 4 2023
entrez: 13 4 2023
Statut: ppublish

Résumé

In the pursuance of novel scaffolds with promising antiplasmodial and anti-inflammatory activity, a series of twenty-one compounds embraced with most promising penta-substituted pyrrole and biodynamic hydroxybutenolide in single skeleton was designed and synthesized. These pyrrole-hydroxybutenolide hybrids were evaluated against Plasmodium falciparum parasite. Four hybrids 5b, 5d, 5t and 5u exhibited good activity with IC

Identifiants

DOI: 10.1016/j.ejmech.2023.115340 PMID: 37054559
pubmed: 37054559
pii: S0223-5234(23)00306-9
doi: 10.1016/j.ejmech.2023.115340
pii:
doi:

Substances chimiques

Antimalarials 0
Chloroquine 886U3H6UFF
Anti-Inflammatory Agents 0

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

115340

Informations de copyright

Copyright © 2023 Elsevier Masson SAS. All rights reserved.

Déclaration de conflit d'intérêts

Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Auteurs

Alka Raj Pandey (AR)

Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, 226031, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, U.P, India.

Suriya Pratap Singh (SP)

Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, 226031, India.

Prince Joshi (P)

Division of Molecular Microbiology and Immunology, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, 226031, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, U.P, India.

Kunwar Satyadeep Srivastav (KS)

Division of Pharmacology, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, 226031, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, U.P, India.

Smriti Srivastava (S)

Division of Pharmacology, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, 226031, India.

Kanchan Yadav (K)

Division of Molecular Microbiology and Immunology, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, 226031, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, U.P, India.

Ramesh Chandra (R)

Division of Pharmacology, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, 226031, India.

Amol Chhatrapati Bisen (AC)

Pharmaceutics and Pharmacokinetics Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, 226031, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, U.P, India.

Sristi Agrawal (S)

Pharmaceutics and Pharmacokinetics Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, 226031, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, U.P, India.

Sachin Nashik Sanap (SN)

Pharmaceutics and Pharmacokinetics Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, 226031, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, U.P, India.

Rabi Sankar Bhatta (RS)

Pharmaceutics and Pharmacokinetics Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, 226031, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, U.P, India.

Renu Tripathi (R)

Division of Molecular Microbiology and Immunology, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, 226031, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, U.P, India.

Manoj Kumar Barthwal (MK)

Division of Pharmacology, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, 226031, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, U.P, India.

Koneni V Sashidhara (KV)

Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, 226031, India; Sophisticated Analytical Instrument Facility & Research, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, 226031, U.P, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, U.P, India. Electronic address: kv_sashidhara@cdri.res.in.

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Classifications MeSH

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questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Anti-infectieux › Antiparasitaires › Antiprotozoaires › Antipaludiques › Design, synthesis and evaluation of novel...
questionsmedicales.fr › Composés hétérocycliques › Composés hétérocycliques à cycles fusionnés › Composés hétérobicycliques › Quinoléines › Aminoquinoléines › Chloroquine › Design, synthesis and evaluation of novel...
questionsmedicales.fr › Eucaryotes › Alveolata › Apicomplexa › Haemosporida › Plasmodium › Plasmodium falciparum › Design, synthesis and evaluation of novel...
questionsmedicales.fr › Systèmes sanguin et immunitaire › Système immunitaire › Phagocytes › Monocytes › Design, synthesis and evaluation of novel...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Anti-inflammatoires › Design, synthesis and evaluation of novel...