Synthesis and anti-HCMV activity of 1-acyl-β-lactams and 1-acylazetidines derived from phenylalanine
2004; Elsevier BV; Volume: 14; Issue: 9 Linguagem: Inglês
10.1016/j.bmcl.2004.02.010
ISSN1464-3405
AutoresGuillermo Gerona‐Navarro, M. Jesús Pérez de Vega, Ma̱ Teresa Garcı́a-López, Graciela Andreï, Robert Snoeck, Jan Balzarini, Erik De Clercq, Rosario González‐Muñiz,
Tópico(s)Synthesis and Catalytic Reactions
ResumoDifferent Phe-derived 1-acyl-β-lactams, analogous to a series of 2-azetidinones acting as HCMV serine protease inhibitors, were synthesized. Some of these compounds were modest inhibitors of the HCMV replication. Interestingly, removal of the carbonyl group of the β-lactam ring, most likely acting as the serine trap, resulted in an azetidine derivative with anti-HCMV activity comparable to that of the reference compound ganciclovir.
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