Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors.

Caldwell CG; Chen P; He J; Parmee ER; Leiting B; Marsilio F; Patel RA; Wu JK; Eiermann GJ; Petrov A; He H; Lyons KA; Thornberry NA; Weber AE

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Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors.

机译：氟吡咯烷酰胺作为二肽基肽酶IV抑制剂。

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Amides derived from fluorinated pyrrolidines and 4-substituted cyclohexylglycine analogues have been prepared and evaluated as inhibitors of dipeptidyl dipeptidase IV (DP-IV). Analogues which incorporated (S)-3-fluoropyrrolidine showed good selectivity for DP-IV over quiescent cell proline dipeptidase (QPP). Compound 48 had good pharmacokinetic properties and was orally active in an oral glucose tolerance test in lean mice.

机译：已经制备了衍生自氟化吡咯烷和4-取代的环己基甘氨酸类似物的酰胺，并将其评估为二肽基二肽酶IV（DP-IV）的抑制剂。掺入（S）-3-氟吡咯烷的类似物相对于静态细胞脯氨酸二肽酶（QPP）显示出对DP-IV的良好选择性。化合物48具有良好的药代动力学特性，并且在瘦小鼠的口服葡萄糖耐量试验中具有口服活性。

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来源
《Bioorganic and Medicinal Chemistry Letters》 |2004年第5期|共4页
作者
Caldwell CG; Chen P; He J; Parmee ER; Leiting B; Marsilio F; Patel RA; Wu JK; Eiermann GJ; Petrov A; He H; Lyons KA; Thornberry NA; Weber AE;
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正文语种 eng
中图分类基础医学;
关键词
Roman Numeral IV; inhibitors; Amides; DP; Peptide Hydrolases; 酰胺类; 肽水解酶类;

机译：Roman Numeral IV;inhibitors;Amides;DP;Peptide Hydrolases;酰胺类;肽水解酶类;

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专利

1. Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors. [J] . Caldwell CG, Chen P, He J, Bioorganic and Medicinal Chemistry Letters . 2004,第5期

机译：氟吡咯烷酰胺作为二肽基肽酶IV抑制剂。
2. Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors. [J] . Edmondson SD, Wei L, Xu J, Bioorganic and Medicinal Chemistry Letters . 2008,第7期

机译：在二肽基肽酶IV抑制剂中，作为酰胺键的氟烯烃模拟。
3. Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors. [J] . Edmondson SD, Wei L, Xu J, Bioorganic and Medicinal Chemistry Letters . 2008,第7期

机译：在二肽基肽酶IV抑制剂中，作为酰胺键的氟烯烃模拟。
4. Classification analysis using support vector machine, decision tree, and neural network with principal component analysis to determine molecular structure relationship from its biological activity on dipeptidyl peptidase IV inhibitors [C] . Haris Hamzah, Alhadi Bustamam, Arry Yanuar, International Conference on Science and Applied Science . 2020

机译：使用支撑向量机，决策树和神经网络具有主成分分析的分类分析，从而确定二肽基肽酶IV抑制剂的生物活性分子结构关系
5. Screening, Extraction, Isolation and Characterization of a Dipeptidyl Peptidase-IV (DPP-IV) Inhibitor From Ayurvedic and Chinese Herbs [D] . Dai, Fangteng 2018

机译：阿育吠陀和中草药中二肽基肽酶-IV（DPP-IV）抑制剂的筛选，提取，分离和表征
6. Bullous pemphigoid associated with dipeptidyl peptidase IV inhibitors. A case report and review of literature. [O] . Amy Attaway, Tracey L. Mersfelder, Sakshi Vaishnav, 2014

机译：与二肽基肽酶IV抑制剂相关的大疱性类天疱疮。病例报告和文献复习。
7. Glucagon-Like Peptide-1-(7-36)Amide Is Transformed to Glucagon-Like Peptide-1-(9-36)Amide by Dipeptidyl Peptidase IV in the Capillaries Supplying the L Cells of the Porcine Intestine [O] . L. Hansen 1999

机译：胰高血糖素肽-1-（7-36）酰胺通过在供应猪肠的L细胞的毛细管中通过二肽基肽酶IV转化为胰高肽样肽-1-（9-36）酰胺。

Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors.

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