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Design synthesis and evaluation of novel aldose reductase inhibitors: The case of indolyl-sulfonyl-phenols.
Bioorganic & Medicinal Chemistry ( IF 3.5 ) Pub Date : 2020-06-04 , DOI: 10.1016/j.bmc.2020.115575
Konstantinos Koutsopoulos 1 , Vasiliki Lavrentaki 2 , Ioakeim Antoniou 2 , Antonios Kousaxidis 2 , Matina Lefkopoulou 2 , Anna Tsantili-Kakoulidou 3 , Lucia Kovacikova 4 , Milan Stefek 4 , Ioannis Nicolaou 2
Affiliation  

Therapeutic interventions with aldose reductase inhibitors appear to be a promising approach to major pathological conditions (i.e. neuropathy/angiopathy related to chronic hyperglycemia, chronic inflammation and cancer). Until now, the most potent aldose reductase inhibitors have been carboxylic acid derivatives, which poorly permeate biological membranes. In this work, continuing our previous works, we promote the bioisosteric replacement of the carboxylic acid moiety to make equally potent yet more druggable inhibitors.



中文翻译:

新型醛糖还原酶抑制剂的设计合成和评估:以吲哚基-磺酰基-酚为例。

醛糖还原酶抑制剂的治疗性干预似乎是治疗主要病理状况(即与慢性高血糖症,慢性炎症和癌症有关的神经病变/血管病)的一种有前途的方法。到目前为止,最有效的醛糖还原酶抑制剂是羧酸衍生物,其渗透性差。在这项工作中,继续我们以前的工作,我们促进了羧酸部分的生物等位取代,以制造同样有效但更具药物作用的抑制剂。

更新日期:2020-06-04
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