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含1,3,4-恶二唑骨架的非甾体抗炎药的抗炎、镇痛及致溃疡潜力的合成与评估

Synthesis and evaluation of antiinflammatory, analgesic and ulcerogenic potential of NSAIDs bearing 1,3,4-oxadiazole scaffold.

作者信息

Somani R R, Bhanushali U V

机构信息

Department of Pharmaceutical Chemistry, VES's College of Pharmacy, Collector Colony, Chembur, Mumbai, India.

出版信息

Indian J Pharm Sci. 2011 Nov;73(6):634-40. doi: 10.4103/0250-474X.100237.

DOI:10.4103/0250-474X.100237
PMID:23112397
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3480748/
Abstract

Synthesis of 1,3,4-oxadiazole derivatives of diclofenac and mefenamic acid are described. The target compounds 5-[2-(2,6-dichloroanilino)benzyl]-2-aryl-1,3,4-oxadiazole (3a-3e) and 5-[2-(2,3-dimethylanilino)phenyl]-2-(aryl)-1,3,4-oxadiazole (6a-6e) were obtained by treating 2 and 5 with various aromatic acids using POCl(3) as dehydrating agent. They were purified and characterized by IR, (1)H-NMR and elemental analysis. These compounds were further subjected to antiinflammatory, analgesic and acute ulcerogenic activity. Compound 3c and 6d exhibited good antiinflammatory activity and compounds 3c, 3e, 6c, 6d, 6e were found to be non ulcerogenic.

摘要

描述了双氯芬酸和甲芬那酸的1,3,4-恶二唑衍生物的合成。通过使用POCl₃作为脱水剂，将2和5与各种芳香酸处理，得到目标化合物5-[2-(2,6-二氯苯胺基)苄基]-2-芳基-1,3,4-恶二唑(3a - 3e)和5-[2-(2,3-二甲基苯胺基)苯基]-2-(芳基)-1,3,4-恶二唑(6a - 6e)。它们通过红外光谱、¹H-NMR和元素分析进行纯化和表征。这些化合物进一步进行抗炎、镇痛和急性致溃疡活性研究。化合物3c和6d表现出良好的抗炎活性，并且发现化合物3c、3e、6c、6d、6e无致溃疡作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/46d9/3480748/171504ab924d/IJPhS-73-634-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/46d9/3480748/90b4d18ef5ba/IJPhS-73-634-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/46d9/3480748/5ddfa4ba814b/IJPhS-73-634-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/46d9/3480748/4d55e2963e2c/IJPhS-73-634-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/46d9/3480748/171504ab924d/IJPhS-73-634-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/46d9/3480748/90b4d18ef5ba/IJPhS-73-634-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/46d9/3480748/5ddfa4ba814b/IJPhS-73-634-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/46d9/3480748/4d55e2963e2c/IJPhS-73-634-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/46d9/3480748/171504ab924d/IJPhS-73-634-g007.jpg

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