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Titolo:
Design and synthesis of carboxylate inhibitors for matrix metalloproteinases
Autore:
Fujisawa, T; Katakura, S; Odake, S; Morita, Y; Yasuda, J; Yasumatsu, I; Morikawa, T;
Indirizzi:
Fuji Chem Ind Co Ltd, Inst Res, Takaoka, Toyama 9338511, Japan Fuji Chem Ind Co Ltd Takaoka Toyama Japan 9338511 , Toyama 9338511, Japan Daiichi Pharmaceut Co Ltd, Tokyo R&D Ctr, Discovery Res Lab, Edogawa Ku, Tokyo 1348630, Japan Daiichi Pharmaceut Co Ltd Tokyo Japan 1348630 a Ku, Tokyo 1348630, Japan
Titolo Testata:
CHEMICAL & PHARMACEUTICAL BULLETIN
fascicolo: 10, volume: 49, anno: 2001,
pagine: 1272 - 1279
SICI:
0009-2363(200110)49:10<1272:DASOCI>2.0.ZU;2-0
Fonte:
ISI
Lingua:
ENG
Soggetto:
CATALYTIC DOMAIN; HYDROXAMIC ACIDS; COLLAGENASE; DERIVATIVES; CANCER;
Keywords:
human fibroblast collagenase; computerized drug design; inhibitor; carboxylate; stromelysin-1;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
27
Recensione:
Indirizzi per estratti:
Indirizzo: Morikawa, T Fuji Chem Ind Co Ltd, Inst Res, 530 Chikeiji, Takaoka, Toyama 9338511, Japan Fuji Chem Ind Co Ltd 530 Chikeiji Takaoka Toyama Japan 9338511
Citazione:
T. Fujisawa et al., "Design and synthesis of carboxylate inhibitors for matrix metalloproteinases", CHEM PHARM, 49(10), 2001, pp. 1272-1279

Abstract

A series of carboxylate compounds were prepared from N-alpha-substituted 2,3-diaminopropionic acid and were tested for efficacy as matrix metalloproteinase (MMP) inhibitors. During modeling of the initial compound 10a, we utilized three-dimensional structure modeling software (InsightII/Discover Ver. 2.98). Some of the prepared carboxylate derivatives, such as carbamate compounds (12c, d, 22) and sulfonamide compounds (14b, c), proved to be effective MMP-1 inhibitors (with ICS, values of a 10(-6) M order), depending onthe substituent at the N-alpha-position of 2,3-diaminopropionic acid. Someof them were also evaluated for inhibition of stromelysin-1 (MMP-3), and the sulfonamide compound 14c exceeded the lead compound 5b in its MMP-3 inhibitory potency. For the carbamate compounds, we investigated the minimum molecular size at which the MMP-1 inhibitory potency was maintained, and found that this was P-3-P-1' compound 10b.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 27/09/20 alle ore 19:56:54