1.
Org Lett
; 12(15): 3422-5, 2010 Aug 06.
Artigo
em Inglês
| MEDLINE
| ID: mdl-20670007
RESUMO
An efficient enantioselective total synthesis of the potent antibiotic GSK966587 was accomplished. Highlights of the synthesis include two innovative Heck reactions, a highly selective zincate base directed ortho-metalation, Sharpless asymmetric epoxidation, and a fully convergent final step fragment coupling.
Assuntos
Antibacterianos/síntese química , Naftiridinas/síntese química , Antibacterianos/química , Antibacterianos/farmacologia , Estrutura Molecular , Naftiridinas/química , Naftiridinas/farmacologia , Estereoisomerismo
2.
Bioorg Med Chem Lett
; 14(17): 4375-8, 2004 Sep 06.
Artigo
em Inglês
| MEDLINE
| ID: mdl-15357956
RESUMO
A series of 3-substituted N,N'-diarylureas was prepared and the structure-activity relationship relative to CXCR2 receptor affinity as well as their pharmacokinetic properties were examined. In vitro microsomal metabolism studies indicated that the lower clearance rates of the 3-sulfonamido-substituted compounds were most likely due to the suppression of glucuronidation.