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 substituent.
Laub
J B
JB
Department of Medicinal Chemistry, Merck Research Laboratories, NJ 07065, USA.
Greenlee
M L
ML
DiNinno
F
F
Huber
J L
JL
Sundelof
J G
JG
D000578:Amidines / Q000737:chemistry*; D015780:Carbapenems / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D016106:Methicillin Resistance; D008826:Microbial Sensitivity Tests; D013211:Staphylococcus aureus / Q000187:drug effects*
D000578:Amidines; D015780:Carbapenems