A SARS-coronovirus 3CL protease inhibitor isolated from the marine sponge Axinella cf. corrugata: structure elucidation and synthesis

Autor(es)

Simone P. de Lira ^[1] ; Mirna H. R. Seleghim ^[2] ; David E. Williams ^[3] ; Frederic Marion ; Pamela Hamill ^[5] ; François Jean ^[6] ; Raymond J. Andersen ; Eduardo Hajdu ^[8] ; Roberto G. S. Berlinck ^[9]

Afiliação do(s) autor(es)

^[1] Universidade de São Paulo. Instituto de Química de São Carlos - Brasil

^[2] Universidade de São Paulo. Instituto de Química de São Carlos - Brasil

^[3] University of British Columbia. Department of Chemistry

^[5] University of British Columbia. Life Sciences Centre. Department of Microbiology and Immunology - Canadá

^[6] University of British Columbia. Life Sciences Centre. Department of Microbiology and Immunology - Canadá

^[8] Universidade Federal do Rio de Janeiro. Museu Nacional - Brasil

^[9] Universidade de São Paulo. Instituto de Química de São Carlos - Brasil

• Tipo de documento: Artigo Científico
• Fonte: Journal of the Brazilian Chemical Society; v. 18, n. 2, p. 440-443, 2007-04-00.

Resumo

Two coumarin derivatives, esculetin-4-carboxylic acid methyl ester (1) and esculetin-4-carboxylic acid ethyl ester (2), have been isolated from the marine sponge Axinella cf. corrugata. Structure determination included analysis of spectroscopic data and total synthesis of compound 2. These are the first coumarin derivatives isolated from a marine sponge. The ethyl ester 2 was found to be an in vitro inhibitor of SARS 3CL-protease and an effective inhibitor of SARS-CoV replication in Vero cells at non-cytotoxic concentrations. (AU)

• Processo FAPESP: 01/03095-5 - Produtos de invertebrados marinhos: agentes quimioterápicos anti-proliferativos, antibióticos, e contra doenças tropicais
• Beneficiário: Roberto Gomes de Souza Berlinck
• Modalidade de apoio: Auxílio à Pesquisa - Temático