- Benzimidazolone as potent chymase inhibitor: Modulation of reactive metabolite formation in the hydrophobic (P1) region
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A new class of chymase inhibitor featuring a benzimidazolone core with an acid side chain and a P1 hydrophobic moiety is described. Incubation of the lead compound with GSH resulted in the formation of a GSH conjugate on the benzothiophene P1 moiety. Replacement of the benzothiophene with different heterocyclic systems such as indoles and benzoisothiazole is feasible. Among the P1 replacements, benzoisothiazole prevents the formation of GSH conjugate and an in silico analysis of oxidative potentials agreed with the experimental outcome.
- Lo, Ho Yin,Nemoto, Peter A.,Kim, Jin Mi,Hao, Ming-Hong,Qian, Kevin C.,Farrow, Neil A.,Albaugh, Daniel R.,Fowler, Danielle M.,Schneiderman, Richard D.,Michael August,Martin, Leslie,Hill-Drzewi, Melissa,Pullen, Steven S.,Takahashi, Hidenori,De Lombaert, Stephane
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scheme or table
p. 4533 - 4539
(2011/09/12)
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- Synthesis of acyclo-C-nucleosides in the imidazo[1,2-a]pyridine and pyrimidine series as antiviral agents
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The synthesis and the antiviral activities of C-3 acyclic nucleoside analogues of imidazo[1,2-a]pyridine and pyrimidine are reported. From these compounds, 20, 21, 22, 23, 28, and 34 showed a specific activity against cytomegalovirus and/or varicella-zoster virus.
- Gueiffier, Alain,Lhassani, Mohammed,Elhakmaoui, Ahmed,Snoeck, Robert,Andrei, Graciela,Chavignon, Olivier,Teulade, Jean-Claude,Kerbal, Abdelali,Essassi, El Mokhtar,Debouzy, Jean-Claude,Witvrouw, Myriam,Blache, Yves,Balzarini, Jan,De Clercq, Erik,Chapat, Jean-Pierre
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p. 2856 - 2859
(2007/10/03)
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