Mata E G
Instituto de Química Orgánica de Síntesis. CONICET - Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas, Argentina.
Curr Pharm Des. 1999 Nov;5(11):955-64.
Combinatorial chemistry has became a core technology for the rapid development of novel lead compounds in the pharmaceutical industry and for the optimization of therapeutic efficacy. The effort to prepare libraries of compounds by combinatorial chemistry has led to an unprecedented growth in solid phase organic synthesis (SPOS), particularly for the preparation of non-oligomeric small molecules. In this context, the clinically valuable b-lactam compounds are very attractive targets for research using these new techniques. In recent years, b-lactam compounds have been recognized not only as unique antibacterial agents but also as potent enzyme inhibitors, drug delivery agents, and versatile synthetic intermediates. This review gives a comprehensive up-date for the application of solid-phase and combinatorial synthesis to b-lactam compounds.
组合化学已成为制药行业快速开发新型先导化合物以及优化治疗效果的核心技术。通过组合化学制备化合物库的努力推动了固相有机合成（SPOS）的空前发展，特别是在制备非寡聚小分子方面。在这种背景下，具有临床价值的β-内酰胺化合物是使用这些新技术进行研究的极具吸引力的目标。近年来，β-内酰胺化合物不仅被认为是独特的抗菌剂，而且还是有效的酶抑制剂、药物递送剂和通用的合成中间体。本综述全面更新了固相和组合合成在β-内酰胺化合物中的应用。
