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. 1998 Apr 21;8(8):919-24.
doi: 10.1016/s0960-894x(98)00132-2.

Peptidyl human heart chymase inhibitors. 2. Discovery of highly selective difluoromethylene ketone derivatives with Glu at P3 site

M Eda  1 , A Ashimori, F Akahoshi, T Yoshimura, Y Inoue, C Fukaya, M Nakajima, H Fukuyama, T Imada, S Takai, N Shiota, M Miyazaki, N Nakamura
Affiliations

Peptidyl human heart chymase inhibitors. 2. Discovery of highly selective difluoromethylene ketone derivatives with Glu at P3 site

M Eda et al. Bioorg Med Chem Lett. .

Erratum in

  • Bioorg Med Chem Lett 1998 Jul 7;8(13):1779

Abstract

Appropriate structural modification of the difluoromethylene ketone derivatives at both P3 and P' positions led us to the discovery of peptidyl human heart chymase inhibitor 12h which shows potent activity with Ki = 6 nM and high selectivity against closely related serine protease bovine alpha-chymotrypsin (chymotrypsin Ki = > 100 microM). Using the compound 12b, a docking study with human heart chymase was carried out to presume probable interactions.

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