Walzer P D, Kim C K, Foy J, Zhang J L
Cincinnati Veterans Affairs Medical Center, Ohio.
Antimicrob Agents Chemother. 1991 Jan;35(1):158-63. doi: 10.1128/AAC.35.1.158.
Furazolidone and nitrofurantoin, oral nitrofuran derivatives with broad-spectrum antimicrobial properties already in clinical use, were compared for activity against Pneumocystis carinii in an immunosuppressed rat model of P. carinii pneumonia. Furazolidone exhibited only slight activity as a prophylactic agent but was moderately effective in the therapy of pneumocystosis. The median histologic score and organism count fell from 4+ and 10(8) to 10(9) cysts per lung, respectively, in the controls to 1+ to 2+ and 10(7) to 10(8) cysts per lung, respectively, in the furazolidone-treated groups. However, these results were not as good as those obtained with the standard drug, trimethoprim-sulfamethoxazole (0+, 10(6) to 10(7) cysts per lung). Nitrofurantoin showed little anti-P. carinii activity despite different doses or drug preparations. The high doses of furazolidone used here and their toxic effects on the rats will probably discourage investigation of this drug in the treatment of pneumocystosis in humans. Nevertheless, since many nitrofurans have been synthesized, further exploration of this class of compounds might be helpful in developing new anti-P. carinii agents or in studying structure-activity relationships.
呋喃唑酮和呋喃妥因是已在临床使用的具有广谱抗菌特性的口服硝基呋喃衍生物，在卡氏肺孢子虫肺炎的免疫抑制大鼠模型中，对它们抗卡氏肺孢子虫的活性进行了比较。呋喃唑酮作为预防药物仅表现出轻微活性，但在治疗肺孢子虫病方面有一定效果。在对照组中，组织学评分中位数和每肺的虫体计数分别从4+和10⁸至10⁹个囊肿降至呋喃唑酮治疗组的1+至2+和10⁷至10⁸个囊肿。然而，这些结果不如使用标准药物甲氧苄啶-磺胺甲恶唑所获得的结果（每肺0+、10⁶至10⁷个囊肿）。尽管使用了不同剂量或药物制剂，呋喃妥因显示出几乎没有抗卡氏肺孢子虫活性。这里使用的高剂量呋喃唑酮及其对大鼠的毒性作用可能会阻碍对该药物在人类肺孢子虫病治疗中的研究。尽管如此，由于已经合成了许多硝基呋喃，进一步探索这类化合物可能有助于开发新的抗卡氏肺孢子虫药物或研究构效关系。
