Laborde María A, Mata Ernesto G
Instituto de Química Orgánica de Síntesis, CONICET - Universidad Nacional de Rosario, Facultad de Ciencias Bioquímicas y Farmacéuticas, Suipacha 531, 2000 Rosario, Argentina.
Mini Rev Med Chem. 2006 Jan;6(1):109-20. doi: 10.2174/138955706775197794.
Solid-phase organic synthesis (SPOS) has become an effective synthetic tool for the preparation of combinatorial libraries of non-oligomeric small molecules. Owing to their high efficacy and extremely safe toxicological profile, beta-lactam antibiotics are the first choice for bacterial infectious diseases. Moreover, beta-lactam compounds have also showed other biological activities that include inhibition of prostate specific antigen, thrombin, human cytomegalovirus protein, human leukocyte elastase and cholesterol absorption. Thus, the application of combinatorial and related methodologies to the chemistry of the beta-lactam ring has been recognized as a very attractive challenge by different research groups around the world. This review covers the solid-phase and combinatorial chemistry related to mono-and multicyclic beta-lactam compounds that has been reported in the literature from 1999 to 2004.
固相有机合成（SPOS）已成为制备非寡聚小分子组合文库的有效合成工具。由于其高效性和极低的毒理学风险，β-内酰胺类抗生素是细菌性传染病的首选药物。此外，β-内酰胺化合物还表现出其他生物活性，包括抑制前列腺特异性抗原、凝血酶、人巨细胞病毒蛋白、人白细胞弹性蛋白酶以及胆固醇吸收。因此，组合化学及相关方法在β-内酰胺环化学中的应用已被全球不同研究团队视为极具吸引力的挑战。本综述涵盖了1999年至2004年文献中报道的与单环和多环β-内酰胺化合物相关的固相化学和组合化学。
