Discovery libraries targeting the major enzyme classes: The serine hydrolases期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

按检索

Discovery libraries targeting the major enzyme classes: The serine hydrolases

Institution:	1. Drugs and Herbal Research Centre, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz, 50300 Kuala Lumpur, Malaysia;2. School of Chemical Sciences and Food Technology, Universiti Kebangsaan Malaysia, 43600 Bangi, Selangor, Malaysia;3. Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia, 43400 Serdang, Selangor, Malaysia;4. Institute of Bioscience, Universiti Putra Malaysia, 43400 Serdang, Selangor, Malaysia;5. Faculty of Science, Universiti Teknologi MARA, 50400 Shah Alam, Selangor, Malaysia;6. Sekolah Tinggi Ilmu Farmasi Riau, Universitas Riau, Kampus Bina Widya Km 12.5, Simpang baru-Pekanbaru, Indonesia;1. Department of Pharmacy, Changzheng Hospital, Second Military Medical University, 415 Fengyang Road, Shanghai 200003, PR China;2. State Key Laboratory of Drug Research, Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, 555 Zuchongzhi Road, Zhangjiang Hi-Tech Park, Shanghai 201203, PR China;3. Department of Pharmacology, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, PR China;1. Departamento de Biofísica e Farmacologia, Universidade Federal do Rio Grande do Norte, 59072-970 Natal-RN, Brazil;2. Instituto de Física, Universidade Federal de Alagoas, 57072-900 Maceió-AL, Brazil;1. Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02115, USA;2. Department of Biological Chemistry & Molecular Pharmacology, Harvard Medical School, 360 Longwood Ave, Boston, MA 02115, USA;3. Vivid BioSciences, 50 Northern Ave, Boston, MA 02210, USA;4. SYNthesis med chem, 425 Changyang Street, Suzhou Industry Park, Suzhou, Jiangsu, China;1. Warren Center for Neuroscience Drug Discovery, Nashville, TN 37232, United States;2. Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232, United States;3. Vanderbilt Kennedy Center, Vanderbilt University School of Medicine, Nashville, TN 37232, United States;4. Department of Chemistry, Vanderbilt University, Nashville, TN 37232, United States;5. Department of Biochemistry, Vanderbilt University, Nashville, TN 37232, United States

Abstract:	Two libraries of modestly reactive ureas containing either electron-deficient acyl anilines or acyl pyrazoles were prepared and are reported as screening libraries for candidate serine hydrolase inhibitors. Within each library is a small but powerful subset of compounds that serve as a chemotype fragment screening library capable of subsequent structural diversification. Elaboration of the pyrazole-based ureas provided remarkably potent irreversible inhibitors of fatty acid amide hydrolase (FAAH, apparent K_i = 100–200 pM) complementary to those previously disclosed enlisting electron-deficient aniline-based ureas.

Keywords:	Serine hydrolase inhibitors Enzyme inhibitors Screening library Fatty acid amide hydrolase
本文献已被 ScienceDirect 等数据库收录！

设为首页 | 免责声明 | 关于勤云 | 加入收藏