Spirocyclic ureas: orally bioavailable 11beta-HSD1 inhibitors identified by computer-aided drug design.

Tice CM; Zhao W; Xu

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Spirocyclic ureas: orally bioavailable 11beta-HSD1 inhibitors identified by computer-aided drug design.

机译：螺环脲：通过计算机辅助药物设计鉴定的口服可生物利用的11beta-HSD1抑制剂。

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Structure-guided drug design led to the identification of a class of spirocyclic ureas which potently inhibit human 11beta-HSD1 in vitro. Lead compound 10j was shown to be orally bioavailable in three species, distributed into adipose tissue in the mouse, and its (R) isomer 10j2 was efficacious in a primate pharmacodynamic model.

机译：结构导向的药物设计导致了一类螺环脲的鉴定，其在体外有效抑制人11beta-HSD1。铅化合物10j在三种物种中具有口服生物利用度，分布在小鼠的脂肪组织中，其（R）异构体10j2在灵长类动物药效学模型中有效。

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《Bioorganic and Medicinal Chemistry Letters》 |2010年第3期|共6页
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Tice CM; Zhao W; Xu;
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1. Spirocyclic ureas: orally bioavailable 11beta-HSD1 inhibitors identified by computer-aided drug design. [J] . Tice CM, Zhao W, Xu Bioorganic and Medicinal Chemistry Letters . 2010,第3期

机译：螺环脲：通过计算机辅助药物设计鉴定的口服可生物利用的11beta-HSD1抑制剂。
2. Discovery of spirocyclic secondary amine-derived tertiary ureas as highly potent, selective and bioavailable soluble epoxide hydrolase inhibitors. [J] . Shen HC, Ding FX, Wang S Bioorganic and Medicinal Chemistry Letters . 2009,第13期

机译：螺环仲胺衍生的叔脲的发现，作为高效，选择性和可生物利用的可溶性环氧化物水解酶抑制剂。
3. Discovery of novel spirocyclic inhibitors of fatty acid amide hydrolase (FAAH). Part 2. Discovery of 7-azaspiro(3.5)nonane urea PF-04862853, an orally efficacious inhibitor of fatty acid amide hydrolase (FAAH) for pain. [J] . Meyers MJ, Long SA, Pelc MJ, Bioorganic and Medicinal Chemistry Letters . 2011,第21期

机译：发现脂肪酸酰胺水解酶（FAAH）的新型螺环抑制剂。第2部分。7-azaspiro（3.5）壬烷尿素PF-04862853的发现，它是一种用于疼痛的脂肪酸酰胺水解酶（FAAH）的口服有效抑制剂。
4. CNX-774, an Irreversible, Selective and Orally Bioavailable Inhibitor of Bruton's Tyrosine Kinase: In Vitro ADME, Selectivity, and Pharmacokinetic Properties [C] . Prasoon Chaturvedi, Matthew Labenski, Erica Evans, American Society for Mass Spectrometry Conference on Mass Spectrometry and Allied Topics . 2011

机译：CNX-774，Bruton的酪氨酸激酶的不可逆转，选择性和口服生物可利用的抑制剂：体外Adme，选择性和药代动力学性能
5. Bioassay driven drug discovery and computer-aided drug design. [D] . Mohler, Michael L. 2005

机译：生物测定驱动药物发现和计算机辅助药物设计。
6. Computer-Aided Design of Orally Bioavailable Pyrrolidine Carboxamide Inhibitors of Enoyl-Acyl Carrier Protein Reductase of Mycobacterium tuberculosis with Favorable Pharmacokinetic Profiles [O] . Affiba Florance Kouassi, Mawa Kone, Melalie Keita, 2015

机译：具有良好药代动力学特征的结核分枝杆菌的烯丙基酰基载体蛋白还原酶的口服生物利用吡咯烷羧酰胺抑制剂的计算机辅助设计
7. Computer-Aided Design of Orally Bioavailable Pyrrolidine Carboxamide Inhibitors of Enoyl-Acyl Carrier Protein Reductase of Mycobacterium tuberculosis with Favorable Pharmacokinetic Profiles [O] . Affiba Florance Kouassi, Mawa Kone, Melalie Keita, 2015

机译：计算机辅助设计口服生物可利用的吡咯烷羧酰胺抑制剂结核分枝杆菌的酰基 - 酰基载体蛋白还原酶具有良好的药代动力学特征
8. Guidance for Industry: Bioavailability and Bioequivalence Studies for Orally Administered Drug Products - General Considerations. Revision 1 [R] . 2003

机译：工业指南：口服药品的生物利用度和生物等效性研究 - 一般考虑因素。修订版1

Spirocyclic ureas: orally bioavailable 11beta-HSD1 inhibitors identified by computer-aided drug design.

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