Structure-guided discovery of thiazolidine-2,4-dione derivatives as a novel class of Leishmania major pteridine reductase 1 inhibitors
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- 作者：Franco Henrique A. Leitea ; Priscila Brandã ; o Gomes da Silva Santiagob ; Thamires Quadros Froesd ; Joã ; o da Silva Filhob ; Suellen Gonç ; alves da Silvad ; Rafael M. Ximenesb ; Antô ; nio Rodolfo de Fariac ; Dalci José ; Brondanic ; Julianna F.C. de Albuquerqueb ; Marcelo Santos Castilhoa ; d ; castilho@ufba.br" class="auth_mail" title="E-mail the corresponding author
- 关键词：Leishmania ; Thiazolidine-2 ; 4-dione derivatives ; Pteridine reductase 1 ; Thermal shift assay ; Kinetic assay ; Molecular modeling
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：10 November 2016
- 年：2016
- 卷：123
- 期：Complete
- 页码：639-648
- 全文大小：989 K
文摘
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Thiazolidine-2,4-dione derivatives are promising leads for antileishmanial drug design.
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Thiazolidinone ring mimics NADPH binding, thus acting as a noncompetitive inhibitor.
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Molecular dynamics support thiazolidine-2,4-dione one binding profile to LmPTR1.