固相有机合成小分子化学库

本文综述了1, 4-苯并二氮杂　、哌嗪二酮、异喹啉酮、二氢和四氢异喹啉、1, 4-二氢吡啶、Biginelli 型二氢嘧啶、乙内酰脲、吡咯烷、噻唑烷-4-羧酸、4-噻唑烷酮及42间噻嗪酮衍生物、咪唑衍生物、β-内酰胺及氮杂环丁酮衍生物等杂环化合物库与β-折叠模拟物、天门冬氨酸蛋白酶抑制剂、C₂ 对称HIV-1 蛋白酶抑制剂、碳酸酐酶抑制剂、含锌蛋白酶抑制剂、酪氨酸激酶抑制剂、雌激素受体配体化合物等靶向组合库固相有机合成研究方面的最新进展。

Small Molecular Chemical Libraries Generated Through Solid Phase Organic Synthesis

Recent progress in solid phase supported organic synthesis of heterocyclic libraries with important physiological activity, such as 1, 4- benzodiazpines, diketopiperazines, isoquinolinones, dihydro and tetrahydroisoquinolines, 1, 4-dihydropyridines, dihydropyrimidines, hydantoins, pyrrolidines, thiazolidine-4-carboxylic acids, 4-thiazolidnones and related 4-metathiazanones, imidazoles, β-lactams and related azetidinones; important targeted libraries including β-turn mimetics library, protease and kinase inhibitor libraries such as aspartic acid protease, HIV-1 protease, zinic protease, carbonic anhydrase、tyrosine kinase, as well as estrogen receptor ligand library are reviewed.