The synthesis and anti-MRSA activity of amidinium-substituted 2-dibenzofuranylcarbapenems

A series of amidinium-substituted 2-dibenzofuranylcarbapenems with potent activity against MRSA has been synthesized via a Stille cross-coupling reaction. These new carbapenems show reduced serum protein binding and improved in vivo efficacy as a consequence of the positively charged amidinium subst...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1999-10, Vol.9 (20), p.2973-2976
Hauptverfasser:	Laub, Joanne B., Greenlee, Mark L., DiNinno, Frank, Huber, Joann L., Sundelof, Jon G.
Format:	Artikel
Sprache:	eng
Schlagworte:	Amidines - chemistry Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Biological and medical sciences Carbapenems - chemical synthesis Carbapenems - chemistry Carbapenems - pharmacology Medical sciences Methicillin Resistance Microbial Sensitivity Tests Pharmacology. Drug treatments Staphylococcus aureus - drug effects
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Zusammenfassung:	A series of amidinium-substituted 2-dibenzofuranylcarbapenems with potent activity against MRSA has been synthesized via a Stille cross-coupling reaction. These new carbapenems show reduced serum protein binding and improved in vivo efficacy as a consequence of the positively charged amidinium substituent. A series of amidinium-substituted 2-dibenzofuranylcarbapenems with potent activity against MRSA has been synthesized via a Stille cross-coupling reaction. These new carbapenems show reduced serum protein binding and improved in vivo efficacy as a consequence of the positively charged amidinium substituent. [Display omitted]
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(99)00526-0