Identification of novel and potent isoquinoline aminooxazole-Based IMPDH inhibitors.

Chen P; Norris D; Haslow KD; Murali Dhar TG; Pitts WJ; Watterson SH; Cheney DL; Bassolino DA; Fleener CA; Rouleau KA; Hollenbaugh DL; Townsend RM; Barrish JC; Iwanowicz EJ

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Identification of novel and potent isoquinoline aminooxazole-Based IMPDH inhibitors.

机译：鉴定新型和有效的基于异喹啉氨基恶唑的IMPDH抑制剂。

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Screening of our in-house compound collection led to the discovery of 5-bromo-6-amino-2-isoquinoline 1 as a weak inhibitor of IMPDH. Subsequent optimization of 1 afforded a series of novel 2-isoquinolinoaminooxazole-based inhibitors, represented by 17, with single-digit nanomolar potency against the enzyme.

机译：我们内部化合物收集的筛选导致发现5-溴-6-氨基-2-异喹啉1作为IMPDH的弱抑制剂。随后的优化1提供了一系列新型的以2-异喹啉基氨基恶唑为基的抑制剂，以17表示，具有针对该酶的一位数纳摩尔效能。

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《Bioorganic and Medicinal Chemistry Letters》 |2003年第7期|共4页
作者
Chen P; Norris D; Haslow KD; Murali Dhar TG; Pitts WJ; Watterson SH; Cheney DL; Bassolino DA; Fleener CA; Rouleau KA; Hollenbaugh DL; Townsend RM; Barrish JC; Iwanowicz EJ;
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正文语种 eng
中图分类药学;生物化学;
关键词
novel; isoquinoline; inhibitors; Identification (Psychology); Nanomole/liter; 认同(心理学);

机译：novel;isoquinoline;inhibitors;Identification (Psychology);Nanomole/liter;认同(心理学);

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专利

1. Identification of novel and potent isoquinoline aminooxazole-Based IMPDH inhibitors. [J] . Chen P, Norris D, Haslow KD, Bioorganic and Medicinal Chemistry Letters . 2003,第7期

机译：鉴定新型和有效的基于异喹啉氨基恶唑的IMPDH抑制剂。
2. Development of novel amide–derivatized 2,4-bispyridyl thiophenes as highly potent and selective Dyrk1A inhibitors. Part II: Identification of the cyclopropylamide moiety as a key modification [J] . Sarah S. Darwish, Mohammad Abdel-Halim, Ahmed K. ElHady, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2018,第期

机译：新型酰胺衍生化的2,4-双吡啶基噻吩是高效和选择性的甲孔抑制剂。第二部分：将环丙基酰胺部分的鉴定为关键改性
3. Isolation, structure identification and SAR studies on thiosugar sulfonium salts, neosalaprinol and neoponkoranol, as potent alpha-glucosidase inhibitors. [J] . Xie W, Tanabe G, Akaki J, Bioorganic and medicinal chemistry . 2011,第6期

机译：作为有效的α-葡萄糖苷酶抑制剂的硫糖基sulf盐，新花生米酚和新ponkoranol的分离，结构鉴定和SAR研究。
4. IMPDH Structure and Ligand Binding [C] . Barry M. Goldstein, Dipesh Risal, Michael Strickler Symposium on Inosine Monophosphate Dehydrogenase: A Major Therapeutic Target null null . 2000

机译：IMPDH结构和配体结合
5. Biochemical Characterization of FIKK Kinase from Cryptosporidium parvum and Discovery of Potent Inhibitors. [D] . Osman, Khan Tanjid. 2016

机译：小隐隐孢子虫FIKK激酶的生化特征和有效抑制剂的发现。
6. Structural basis for selectivity of the isoquinoline sulfonamide family of protein kinase inhibitors. [O] . R M Xu, G Carmel, J Kuret, 1996

机译：蛋白激酶抑制剂异喹啉磺酰胺家族选择性的结构基础。
7. Identification of novel piperazinylquinoxaline derivatives as potent phosphoinositide 3-kinase (PI3K) inhibitors. [O] . Peng Wu, Yi Su, Xianghong Guan, 2012

机译：鉴定新的哌嗪基喹喔啉衍生物作为有效的磷酸肌醇3-激酶（pI3K）抑制剂。

Identification of novel and potent isoquinoline aminooxazole-Based IMPDH inhibitors.

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