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Stereoselective Synthesis of Novel anti-MRSA Tricyclic Carbapenems (Trinems)

✍ Scribed by Osamu Kanno; Isao Kawamoto


Publisher
Elsevier Science
Year
2000
Tongue
French
Weight
191 KB
Volume
56
Category
Article
ISSN
0040-4020

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✦ Synopsis


AbstractÐ(4S)-Hydroxymethyltrinem 3 was prepared via stereoselective aldol-type reaction with optically pure (R)-2-t-butyldimethylsilyloxymethylcyclohexanone ((R)-16). (4S)-Hydroxymethyltrinem 3 was converted into various kinds of trinem derivatives with anti-MRSA activity by using the Mitsunobu reaction.


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A series of sulphur-linked and carbon-linked lipophLlic carhapenems has been prepared and evaluated for antibacterial activity in vitro and in vivo and for affinity for PBP2' of Staphylococcus aureus. Potent activity in vitro against methicillin-resistant S. aureus and methicillin-resistant coagulas