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核心技术专利：CN118964589B侵权必究
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新型 3-乙酰基-1,3,4-恶二唑啉与嘧啶类化合物的联合合成及其抗利什曼原虫和抗病毒活性。

Synthesis of new 3-acetyl-1,3,4-oxadiazolines combined with pyrimidines as antileishmanial and antiviral agents.

机构信息

Laboratory of Biomolecular and Medicinal Chemistry, Faculty of Science Semlalia, University Cadi Ayyad, Marrakech, Morocco.

Department of Chemistry, University of the Free State, P.O. Box 339, Bloemfontein, 9300, South Africa.

出版信息

Mol Divers. 2023 Oct;27(5):2147-2159. doi: 10.1007/s11030-022-10548-9. Epub 2022 Oct 17.

DOI:10.1007/s11030-022-10548-9
PMID:36251201
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9573813/
Abstract

A new series of 3-acetyl-1,3,4-oxadiazoline hybrid molecules was designed and synthesized using a condensation between acyclonucleosides and substituted phenylhydrazone. All intermediates and final products were screened against Leishmania donovani, a Protozoan parasite and against three viruses SARS-CoV-2, HCMV and VZV. While no significant activity was observed against the viruses, the intermediate with 6-azatymine as thymine and 5-azathymine-3-acetyl-1,3,4-oxadiazoline hybrid exhibited a significant antileishmanial activity. The later compound was the most promising, exhibiting an IC value at 8.98 µM on L. donovani intramacrophage amastigotes and a moderate selectivity index value at 2.4.

摘要

设计并合成了一系列新的 3-乙酰基-1,3,4-噁二唑啉杂合分子，方法是通过acyclonucleosides 和取代苯基腙之间的缩合反应。所有中间体和最终产物都针对利什曼原虫（一种原生动物寄生虫）和三种病毒 SARS-CoV-2、HCMV 和 VZV 进行了筛选。虽然对病毒没有明显的活性，但具有 6-氮杂胸腺嘧啶和 5-氮杂胸腺嘧啶-3-乙酰基-1,3,4-噁二唑啉杂合的中间体表现出显著的抗利什曼原虫活性。后期化合物最有前途，对 L. donovani 巨噬细胞内变形体的 IC 值为 8.98µM，选择性指数值为 2.4。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/94d6/9573813/dcf674f46712/11030_2022_10548_Sch3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/94d6/9573813/796e4eed87fc/11030_2022_10548_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/94d6/9573813/ec14733ee384/11030_2022_10548_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/94d6/9573813/9ac40772e065/11030_2022_10548_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/94d6/9573813/04daf4f1c754/11030_2022_10548_Sch1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/94d6/9573813/ff9d448c9363/11030_2022_10548_Sch2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/94d6/9573813/dcf674f46712/11030_2022_10548_Sch3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/94d6/9573813/796e4eed87fc/11030_2022_10548_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/94d6/9573813/ec14733ee384/11030_2022_10548_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/94d6/9573813/9ac40772e065/11030_2022_10548_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/94d6/9573813/04daf4f1c754/11030_2022_10548_Sch1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/94d6/9573813/ff9d448c9363/11030_2022_10548_Sch2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/94d6/9573813/dcf674f46712/11030_2022_10548_Sch3_HTML.jpg

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引用本文的文献

[1]
Hydrazides as Powerful Tools in Medicinal Chemistry: Synthesis, Reactivity, and Biological Applications.

Molecules. 2025-7-3

[2]
Synthesis and Antioxidant Activities of Novel Pyrimidine Acrylamides as Inhibitors of Lipoxygenase: Molecular Modeling and In Silico Physicochemical Studies.

Molecules. 2024-3-7

[3]
Novel 2-Thiouracil-5-Sulfonamide Derivatives: Design, Synthesis, Molecular Docking, and Biological Evaluation as Antioxidants with 15-LOX Inhibition.

Molecules. 2023-2-17

本文引用的文献

[1]
5-Iodotubercidin inhibits SARS-CoV-2 RNA synthesis.

Antiviral Res. 2022-2

[2]
Visceral leishmaniasis and COVID-19 coinfection - A case report.

IDCases. 2022

[3]
Sandfly Fever Sicilian Virus-Leishmania major co-infection modulates innate inflammatory response favoring myeloid cell infections and skin hyperinflammation.

PLoS Negl Trop Dis. 2021-7

[4]
An adamantamine derivative as a drug candidate for the treatment of visceral leishmaniasis.

J Antimicrob Chemother. 2021-9-15

[5]
A robust SARS-CoV-2 replication model in primary human epithelial cells at the air liquid interface to assess antiviral agents.

Antiviral Res. 2021-8

[6]
STAT2 signaling restricts viral dissemination but drives severe pneumonia in SARS-CoV-2 infected hamsters.

Nat Commun. 2020-11-17

[7]
Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19.

J Med Chem. 2020-10-15

[8]
Design, synthesis, chemical characterization, biological evaluation, and docking study of new 1,3,4-oxadiazole homonucleoside analogs.

Nucleosides Nucleotides Nucleic Acids. 2020

[9]
Ribavirin, Remdesivir, Sofosbuvir, Galidesivir, and Tenofovir against SARS-CoV-2 RNA dependent RNA polymerase (RdRp): A molecular docking study.

Life Sci. 2020-3-25

[10]
Nucleoside Analogues as Antibacterial Agents.

Front Microbiol. 2019-5-22

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