RESUMEN
Berkeleylactone A is a potent 16-membered macrolactone antibiotic, recently isolated from a coculture of Berkeley Pit Lake fungi. Although its antimicrobial activity has already been investigated, little is known about the structure-activity relationship. Based on our previous synthetic studies, a series of berkeleylactone A derivatives were synthesized and evaluated for their in vitro antimicrobial activities against methicillin-sensitive and methicillin-resistant Staphylococcus aureus (MRSA) strains. Our data confirmed the essential role of the embedded conjugated system and suggest a reversible sulfa-protection of the Michael acceptor as a viable option. Structurally simplified achiral macrolactam 8 showed the best inhibitory activity against S. aureus L12 (MRSA) with MIC50 values of 0.39 µg mL-1, 8-fold lower than those of berkeleylactone A. These studies may be of value in the development of more advanced candidates for antibiotic applications.
Asunto(s)
Staphylococcus aureus Resistente a Meticilina , Antibacterianos/farmacología , Macrólidos , Meticilina , Pruebas de Sensibilidad Microbiana , Staphylococcus aureus , Relación Estructura-ActividadRESUMEN
The structure and magnetic properties of a complex containing a {Dy2Cu5} core are presented. In 1, the Dy(III) are 9- and the Cu(II) are 4-, 5- and 6-coordinated. Antiferromagnetic interactions cause an irregular energy spectrum with the ground state J = 25/2. The complex is a single molecule magnet exhibiting slow magnetic relaxation in zero magnetic field.