Discovery of 2,3-dihydro-1-pyrrolo[3,4-]quinolin-1-one Derivatives As Possible Antileishmanial Agents

Overview

Journal RSC Med Chem

Publisher Royal Society of Chemistry

Specialty Chemistry

Date 2022 Jul 11

PMID 35814931

Authors

Anuradha Seth

Anirban Ghoshal

Varun Dewaker

Ankita Rani

Sangh Priya Singh

Mukul Dutta

Shivani Katiyar

Sandeep Kumar Singh

Mamunur Rashid

Muhammad Wahajuddin

Susanta Kar

Ajay Kumar Srivastava

Affiliations

Soon will be listed here.

Abstract

A series of uniquely functionalized 2,3,-dihydro-1-pyyrolo[3,4-]quinolin-1-one derivatives were synthesized in one to two steps by utilizing a post-Ugi modification strategy and were evaluated for antileishmanial efficacy against visceral leishmaniasis (VL). Among the library compounds, compound 5m exhibited potential antileishmanial activity (CC = 65.11 μM, SI = 7.79, anti-amastigote IC = 8.36 μM). antileishmanial evaluation of 5m demonstrated 56.2% inhibition in liver and 61.1% inhibition in spleen parasite burden in infected Balb/c mice (12.5 mg kg, i.p.). pharmacokinetic study ascertained the stability of 5m in both simulated gastric fluid and simulated intestinal fluid. All the active compounds passed the PAINS filter and showed no toxicity in predictions.

Citing Articles

Synthesis, antimalarial, antileishmanial evaluation, and molecular docking study of some 3-aryl-2-styryl substituted-4(3H)-quinazolinone derivatives.

Seifu G, Birhan Y, Beshay B, Hymete A, Bekhit A BMC Chem. 2022; 16(1):107.

PMID: 36461074 PMC: 9716151. DOI: 10.1186/s13065-022-00903-0.

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