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戊双脒对鼠实验感染卡氏肺孢子虫肺炎(PCP)有治疗作用,虽有效率低,并且有一些副作用,但它仍是AIDS病人PCP治疗的药物之一。本研究将戊双脒对免疫抑制鼠PCP的治疗作用与7种同类化合物进行比较,对这些化合物的DNA结合活性、对胰蛋白酶和胸苷酸合成酶的抑制作用进行了研究。将小牛胸腺DNA与受试的8种脒衍生物(包括戊双脒)一起孵育,测定DNA熔点
Efficacy of pentamidine in the treatment of experimental Pneumocystis carinii pneumonia (PCP) in mice is ineffective and has some side effects. However, it is still one of the PCP-treated drugs in AIDS patients. In this study, the therapeutic effect of pentamidine on PCP in immunosuppressed mice was compared with that of seven similar compounds. The DNA binding activity of these compounds and the inhibitory effect on trypsin and thymidylate synthase were studied. Calf thymus DNA was incubated with the eight amidine derivatives tested, including pentamidine, and the DNA melting point