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作为p38丝裂原活化蛋白激酶抑制剂的2,3,4-三芳基-1,2,4-恶二唑-5-酮的合成与生物学评价

Synthesis and Biological Evaluation of 2,3,4-Triaryl-1,2,4-oxadiazol-5-ones as p38 MAPK Inhibitors.

作者信息

Romeo Roberto, Giofrè Salvatore V, Chiacchio Maria A, Veltri Lucia, Celesti Consuelo, Iannazzo Daniela

机构信息

Dipartimento di ScienzeChimiche, Biologiche, Farmaceutiche ed Ambientali, Università di Messina, Via S.S. Annunziata, 98168 Messina, Italy.

DipartimentoScienze del Farmaco, Università di Catania, Viale A. Doria 6, 95125 Catania, Italy.

出版信息

Molecules. 2021 Mar 20;26(6):1745. doi: 10.3390/molecules26061745.

DOI:10.3390/molecules26061745
PMID:33804659
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8003627/
Abstract

A series of azastilbene derivatives, characterized by the presence of the 1,2,4-oxadiazole-5-one system as a linker of the two aromatic rings of stilbenes, have been prepared as novel potential inhibitors of p38 MAPK. Biological assays indicated that some of the synthesized compounds are endowed with good inhibitory activity towards the kinase. Molecular modeling data support the biological results showing that the designed compounds possess a reasonable binding mode in the ATP binding pocket of p38α kinase with a good binding affinity.

摘要

一系列氮杂芪衍生物已被制备为新型潜在的p38丝裂原活化蛋白激酶（p38 MAPK）抑制剂，其特征是存在1,2,4-恶二唑-5-酮体系作为芪类两个芳香环的连接基团。生物学试验表明，一些合成化合物对该激酶具有良好的抑制活性。分子模拟数据支持生物学结果，表明所设计的化合物在p38α激酶的ATP结合口袋中具有合理的结合模式和良好的结合亲和力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7e9d/8003627/89671405685d/molecules-26-01745-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7e9d/8003627/3bf5a422fb4e/molecules-26-01745-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7e9d/8003627/607ab69a3341/molecules-26-01745-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7e9d/8003627/70578d4d164d/molecules-26-01745-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7e9d/8003627/59f53db3e5de/molecules-26-01745-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7e9d/8003627/615f8425b7f5/molecules-26-01745-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7e9d/8003627/89671405685d/molecules-26-01745-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7e9d/8003627/3bf5a422fb4e/molecules-26-01745-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7e9d/8003627/607ab69a3341/molecules-26-01745-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7e9d/8003627/70578d4d164d/molecules-26-01745-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7e9d/8003627/59f53db3e5de/molecules-26-01745-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7e9d/8003627/615f8425b7f5/molecules-26-01745-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7e9d/8003627/89671405685d/molecules-26-01745-g006.jpg

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