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Medicinally Privileged Sultams: Synthesis and Mechanism of Action.
Mini-Reviews in Medicinal Chemistry ( IF 3.3 ) Pub Date : 2020-01-01 , DOI: 10.2174/1389557520666200719015234
Precious M Okwuchukwu 1 , Debasish Bandyopadhyay 1
Affiliation  

To date, more than a thousand research articles have been published detailing various regio-, stereo-, chemo-, and enantioselective specific synthesis of the cyclic sulfonamides (sultams). Although enormous synthetic efforts were made, but bioactivities of sultams have not been widely investigated. Sultams are the sulfur analogs of lactams (cyclic amides) which demonstrate a broad range of medicinal activities and several lactam drugs are commercially available. In contrast, only a few sultam drugs are commercially available, while the presence of two oxygens on sulfur in sultam motifs can serve as a better H-bond acceptor than lactam scaffolds. One of the major objectives of this minireview is to draw appropriate attention from the medicinal/pharmaceutical chemists to conduct indepth research on sultam derivatives targeted to the development of new drugs. This article gives a brief account of the synthesis, potential bioactivity, and mechanisms of therapeutic action of four to seven-membered sultam derivatives. Based on the available literature, this is the first effort to consolidate only the medicinally privileged sultam molecules and drugs under the same umbrella. While every effort was taken to comprise all the relevant reports related to bioactive sultams, any oversight is truly unintentional.

中文翻译:

药用特权 Sultams:合成和作用机制。

迄今为止,已经发表了超过 1000 篇研究文章,详细介绍了环状磺酰胺(sultams)的各种区域选择性、立体选择性、化学选择性和对映选择性特异性合成。尽管进行了巨大的合成努力,但尚未对 sultams 的生物活性进行广泛研究。Sultams 是内酰胺(环酰胺)的硫类似物,具有广泛的药用活性,并且有几种内酰胺药物可商购。相比之下,只有少数 sultam 药物可商购,而 sultam 基序中硫上的两个氧的存在可以作为比内酰胺支架更好的 H 键受体。本次小综述的主要目标之一是引起药物/药物化学家的适当关注,以对针对新药开发的舒坦衍生物进行深入研究。本文简要介绍了四至七元舒坦衍生物的合成、潜在生物活性和治疗作用机制。根据现有文献,这是第一次将具有医学特权的 sultam 分子和药物整合到同一保护伞下。尽管已尽一切努力包含与生物活性 sultam 相关的所有相关报告,但任何疏忽都确实是无意的。根据现有文献,这是第一次将具有医学特权的 sultam 分子和药物整合到同一保护伞下。尽管已尽一切努力包含与生物活性 sultam 相关的所有相关报告,但任何疏忽都确实是无意的。根据现有文献,这是第一次将具有医学特权的 sultam 分子和药物整合到同一保护伞下。尽管已尽一切努力包含与生物活性 sultam 相关的所有相关报告,但任何疏忽都确实是无意的。
更新日期:2020-07-18
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