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Bioorg Med Chem Lett. 2003 Mar 24;13(6):1115-8.

Structure-based de novo design of non-nucleoside adenosine deaminase inhibitors.

Author information

1
Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., 2-1-6 Kashima, Yodogawa-ku, Osaka 532-8514, Japan. isao_nakanishi@po.fujisawa.co.jp

Erratum in

  • Bioorg Med Chem Lett. 2003 Nov 17;13(22):4147.

Abstract

We searched for non-nucleoside inhibitors of adenosine deaminase by rational structure-based de novo design and succeeded in the discovery of 1-(1-hydroxy-4-phenyl-2-butyl)imidazole-4-carboxamide (FR221647: K(i)=5.9 microM to human ADA) as a novel inhibitor with moderate activity and good pharmacokinetics compared with the known inhibitors pentostatin and EHNA.

PMID:
12643924
DOI:
10.1016/s0960-894x(03)00026-x
[Indexed for MEDLINE]

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