Antibacterial agent discovery using thymidylate synthase biolibrary screening

…, A Gelain, D Barlocco, S Ghelli, F Soragni…

文献索引：Costi, M. Paola; Gelain, Arianna; Barlocco, Daniela; Ghelli, Stefano; Soragni, Fabrizia; Reniero, Fabiano; Rossi, Tiziana; Ruberto, Antonio; Guillou, Claude; Cavazzuti, Antonio; Casolari, Chiara; Ferrari, Stefania Journal of Medicinal Chemistry, 2006 , vol. 49, # 20 p. 5958 - 5968

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被引用次数: 17

摘要

Thymidylate synthase (TS, ThyA) catalyzes the reductive methylation of 2'-deoxyuridine 5'- monophosphate to 2'-deoxythymidine 5'-monophosphate, an essential precursor for DNA synthesis. A specific inhibition of this enzyme induces bacterial cell death. As a second round lead optimization design, new 1, 2-naphthalein derivatives have been synthesized and tested against a TS-based biolibrary, including human thymidylate synthase (hTS). ...