Discovery of S-adenosyl-L-homocysteine hydrolase inhibitors based on non-adenosine analogs

作者：Nakao Akira^*; Suzuki Hiroko; Ueno Hiroaki; Iwasaki Hiroshi; Setsuta Tomofumi

来源：Bioorganic & Medicinal Chemistry Letters, 2014, 24(17): 4336-4340.

DOI：10.1016/j.bmcl.2014.06.008

• Homocysteine
• S-Adenosyl-L-homocysteine hydrolase inhibitors
• Competitive

High throughput screening using Automated Ligand Identification System (ALIS) resulted in the discovery of a new series of S-adenosyl-L-homocysteine hydrolase inhibitors based on non-adenosine analogs. The optimization campaign led to very potent and competitive compound 39 with a K-i value of 1.5 nM. Compound 39 could be a promising lead compound for research to reduce elevated homocysteine levels.

• 出版日期2014-9-1