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Medicinally Privileged Sultams: Synthesis and Mechanism of Action
Mini-Reviews in Medicinal Chemistry ( IF 3.3 ) Pub Date : 2020-11-30 , 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:

药用特权阿片:合成及其作用机理

迄今为止,已经发表了超过一千篇研究文章,详细介绍了环磺酰胺(sultams)的各种区域,立体,化学和对映选择性合成。尽管已经做出了巨大的合成努力,但是尚未广泛研究阿ult的生物活性。苏丹乳是内酰胺的硫类似物(环酰胺),具有广泛的医学活性,几种内酰胺药物可商购。相比之下,只有少量的舒马坦药物是可商购的,而与内酰胺支架相比,舒马赫基序中硫上存在的两个氧可以作为更好的氢键受体。这项小型审查的主要目标之一是引起药物/药物化学家的适当关注,以针对针对新药开发的舒马坦衍生物进行深入研究。本文简要介绍了四至七元磺胺衍生物的合成,潜在的生物活性和治疗作用的机制。根据现有文献,这是在同一保护伞下仅合并具有医学优势的sultam分子和药物的首次尝试。尽管已尽一切努力将所有与生物活性苏丹酸有关的报告都包括在内,但任何监督实际上都是无意的。根据现有文献,这是在同一保护伞下仅合并具有医学优势的sultam分子和药物的首次尝试。尽管已尽一切努力将所有与生物活性苏丹酸有关的报告都包括在内,但任何监督实际上都是无意的。根据现有文献,这是在同一保护伞下仅合并具有医学优势的sultam分子和药物的首次尝试。尽管已尽一切努力将所有与生物活性苏丹酸有关的报告都包括在内,但任何监督实际上都是无意的。

更新日期:2021-01-15
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