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Easy one-pot synthesis of multifunctionalized indole-pyrrole hybrids as a new class of antileishmanial agents.

作者信息

Ciccone Vittorio, Diotallevi Aurora, Gómez-Benmansour Miriam, Maestrini Sara, Mantellini Fabio, Mari Giacomo, Galluzzi Luca, Lucarini Simone, Favi Gianfranco

机构信息

Department of Biomolecular Sciences, University of Urbino Carlo Bo 61029 Urbino (PU) Italy

出版信息

RSC Adv. 2024 May 14;14(22):15713-15720. doi: 10.1039/d4ra02790f. eCollection 2024 May 10.

DOI:10.1039/d4ra02790f
PMID:38746834
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11092366/
Abstract

A chemoselective one-pot synthesis of pharmaceutically prospective indole-pyrrole hybrids by the formal [3 + 2] cycloaddition of 3-cyanoacetyl indoles (CAIs) with 1,2-diaza-1,3-dienes (DDs) has been developed. The new indole-pyrrole hybrids were phenotypically screened for efficacy against promastigotes. The most active compounds 3c, 3d, and 3j showed IC < 20 μM and moderate cytotoxicity, lower than miltefosine. Compound 3d was the most active with IC = 9.6 μM and a selectivity index of 5. Consequently, 3d could be a new lead compound for the generation of a new class of antileishmanial hybrids.

摘要
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5cea/11092366/20bcbfec9b68/d4ra02790f-s4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5cea/11092366/07647da9c52b/d4ra02790f-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5cea/11092366/e43ae603ee26/d4ra02790f-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5cea/11092366/c0198c034440/d4ra02790f-s2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5cea/11092366/c5fb9714e470/d4ra02790f-s3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5cea/11092366/20bcbfec9b68/d4ra02790f-s4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5cea/11092366/07647da9c52b/d4ra02790f-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5cea/11092366/e43ae603ee26/d4ra02790f-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5cea/11092366/c0198c034440/d4ra02790f-s2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5cea/11092366/c5fb9714e470/d4ra02790f-s3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5cea/11092366/20bcbfec9b68/d4ra02790f-s4.jpg

相似文献

[1]
Easy one-pot synthesis of multifunctionalized indole-pyrrole hybrids as a new class of antileishmanial agents.

RSC Adv. 2024-5-14

[2]
Exploring hydrophilic 2,2-di(indol-3-yl)ethanamine derivatives against Leishmania infantum.

PLoS One. 2024-6-13

[3]
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Molecules. 2022-8-24

[4]
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PLoS One. 2020

[5]
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Bioorg Med Chem. 2016-9-15

[6]
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Eur J Med Chem. 2023-10-5

[7]
Clemastine/tamoxifen hybrids as easily accessible antileishmanial drug leads.

Org Biomol Chem. 2024-2-28

[8]
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[9]
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[10]
Synthesis of Thiocarbohydrazones and Evaluation of their in vitro Antileishmanial Activity.

Med Chem. 2018

本文引用的文献

[1]
Exploring hydrophilic 2,2-di(indol-3-yl)ethanamine derivatives against Leishmania infantum.

PLoS One. 2024-6-13

[2]
Sustainable Synthesis of Indole-Substituted Densely Functionalized Pyrrole.

J Org Chem. 2024-2-2

[3]
Synthetic product-based approach toward potential antileishmanial drug development.

Eur J Med Chem. 2024-1-5

[4]
Is Target-Based Drug Discovery Efficient? Discovery and "Off-Target" Mechanisms of All Drugs.

J Med Chem. 2023-9-28

[5]
A recent update on new synthetic chiral compounds with antileishmanial activity.

Chirality. 2022-10

[6]
Prediction of Antileishmanial Compounds: General Model, Preparation, and Evaluation of 2-Acylpyrrole Derivatives.

J Chem Inf Model. 2022-8-22

[7]
Phenotype Screening of an Azole-bisindole Chemical Library Identifies URB1483 as a New Antileishmanial Agent Devoid of Toxicity on Human Cells.

ACS Omega. 2021-12-15

[8]
Total synthesis of (+)-spiroindimicin A and congeners unveils their antiparasitic activity.

Chem Sci. 2021-6-30

[9]
Recent advancements in anti-leishmanial research: Synthetic strategies and structural activity relationships.

Eur J Med Chem. 2021-11-5

[10]
Metal-Free and Regioselective Synthesis of Substituted and Fused Chromenopyrrole Scaffolds the Divergent Reactivity of α-Azido Ketones in Water.

J Org Chem. 2020-8-7

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