Issartel V, Spehner V, Coudert P, Seilles E, Couquelet J
Groupe de Recherche en Pharmacochimie, Faculté de Pharmacie, Clermont-Ferrand, France.
Bioorg Med Chem. 1998 Mar;6(3):349-54. doi: 10.1016/s0968-0896(97)10052-9.
Four pyrrolo[1,2-d][1,2,4]triazines and four thiazolo[3,4-d][1,2,4]triazines were synthesized from trans-4-hydroxy-L-proline and L-thiaproline, respectively. The synthetic route involved formation of hydrazides followed by cyclization with orthoesters. The proliferative response to human lymphocyte mitogen (phytohemagglutinin) revealed significant immunostimulant activity for all test drugs. Furthermore, some triazine derivatives were effective to activate production of free oxygen radical by phagocytes in response to stimulation by opsonized zymosan.
分别由反式-4-羟基-L-脯氨酸和L-硫代脯氨酸合成了4种吡咯并[1,2-d][1,2,4]三嗪和4种噻唑并[3,4-d][1,2,4]三嗪。合成路线包括酰肼的形成，然后与原酸酯环化。对人淋巴细胞有丝分裂原（植物血凝素）的增殖反应显示所有受试药物均具有显著的免疫刺激活性。此外，一些三嗪衍生物在经调理的酵母聚糖刺激后能有效激活吞噬细胞产生游离氧自由基。
