Coppi G, Falcone A, Manzardo S
Research Centre, Poli Industria Chimica S.p.A., Milan, Italy.
Arzneimittelforschung. 1994 Dec;44(12A):1417-21.
Pidotimod ((R)-3-[(S)-(5-oxo-2-pyrrolidinyl) carbonyl]-thiazolidine-4-carboxylic acid, PGT/1A, CAS 121808-62-6) protected mice against experimental bacterial infections in different experimental models. In all tests the drug's effect was measured as protection from death. The activity of pidotimod was evident and statistically significant after 5 administrations before the bacterial challenges. Pidotimod was active against many bacterial species infections, its active dosages ranging from 0.01 to 100 mg/kg i.p. x 5 times. Pidotimod showed against some bacterial infections a protection similar or better than those of bestatin, N-acetylmuramyl-L-Ala-D-isoGlu-OH and tuftsin. It showed high protection against bacterial infections in cyclophosphamide-immunodepressed mice. Finally, pidotimod showed an additive or synergic activity in combination with beta-lactam antibiotics (cefotaxime, ampicillin) against bacterial infections in mice.
匹多莫德((R)-3-[(S)-(5-氧代-2-吡咯烷基)羰基]-噻唑烷-4-羧酸,PGT/1A,CAS 121808-62-6)在不同实验模型中可保护小鼠免受实验性细菌感染。在所有试验中,药物的效果以防止死亡来衡量。在细菌攻击前给予5次匹多莫德后,其活性明显且具有统计学意义。匹多莫德对多种细菌感染均有活性,其有效剂量为0.01至100 mg/kg腹腔注射×5次。匹多莫德对某些细菌感染的保护作用与贝他定、N-乙酰胞壁酰-L-丙氨酰-D-异谷氨酰胺和促吞噬肽相似或更好。它对环磷酰胺免疫抑制小鼠的细菌感染有高度保护作用。最后,匹多莫德与β-内酰胺类抗生素(头孢噻肟、氨苄西林)联合使用对小鼠细菌感染显示出相加或协同活性。