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Bioorg Med Chem Lett. 2014 Sep 1;24(17):4336-40. doi: 10.1016/j.bmcl.2014.06.008. Epub 2014 Jun 21.

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

Author information

1
Medicinal Chemistry Research Laboratories II, Research Division, Mitsubishi Tanabe Pharma Corporation, 2-2-50, Kawagishi, Toda-shi, Saitama 335-8505, Japan. Electronic address: Nakao.Akira@mc.mt-pharma.co.jp.
2
Pharmacology Research Laboratories I, Research Division, Mitsubishi Tanabe Pharma Corporation, 1000, Kamoshida-cho, Aoba-ku, Yokohama 227-0033, Japan.
3
Medicinal Chemistry Research Laboratories II, Research Division, Mitsubishi Tanabe Pharma Corporation, 2-2-50, Kawagishi, Toda-shi, Saitama 335-8505, Japan.

Abstract

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 Ki value of 1.5 nM. Compound 39 could be a promising lead compound for research to reduce elevated homocysteine levels.

KEYWORDS:

Competitive; Homocysteine; S-Adenosyl-l-homocysteine hydrolase inhibitors

PMID:
25022879
DOI:
10.1016/j.bmcl.2014.06.008
[Indexed for MEDLINE]

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