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Synthesis and structure-activity-relationships of indan acid derivatives as analgesic and anti-inflammatory agents
Reviews and Advances in Chemistry Pub Date : 2016-05-19 , DOI: 10.1134/s2079978016020011
S. C. Bachar , L. Nahar , S. D. Sarker

Indan ring system, also known as indane or benzocyclopentane, is an important chemical feature associated with various biological activities. Among the drugs possessing an indan ring system, 1H-indene-3-acetic acid-5-fluoro-2-methyl-1-[4-(methylsulfinyl)-phenyl]methylene (Sulindac) and 6-chloro-5-cyclohexyl indan-1-carboxylic acid (Clidanac) are well known anti-inflammatory agents, whilst indan-1,3-dione is an anticoagulant. Over the years, several indan derivatives, particularly indan acid derivatives, have been synthesized and their potential analgesic and anti-inflammatory properties have been studied. This review critically appraises various synthetic protocols and structure-activity-relationships of indan acids as analgesic and anti-inflammatory agents with low ulcerogenicity.

中文翻译:

茚满酸衍生物作为镇痛和消炎药的合成及其构效关系

茚满环系统,也称为茚满或苯并环戊烷,是与各种生物活性有关的重要化学特征。在具有茚满环系统的药物中,1 H-茚三-3-乙酸-5-氟-2-甲基-1- [4-(甲基亚磺酰基)-苯基]亚甲基(舒林酸)和6-氯-5-环己基茚满-1-羧酸(Clidanac)是众所周知的抗炎药,而茚满-1,3-二酮是抗凝剂。多年来,已经合成了几种茚满衍生物,特别是茚满酸衍生物,并且已经研究了其潜在的止痛和抗炎特性。这篇综述严格评估了茚满酸作为镇痛药和消炎药的低溃疡性的各种合成方案和构效关系。
更新日期:2016-05-19
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