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Pfizer和英国St Mary’s医学院的研究工作者联合研制了一种新的α-肾上腺素受体拮抗剂(UK-570-46-27)。据称,这种对心肌有选择性的新化合物能有效地减少豚鼠离体心脏心律不齐的发生,并在心肌局部缺血和反复灌注的情况下改变细胞的电参数。以美国为大本营的Upjohn公司研制出一系列3位取代的Steffimyci B的类似物,Steffimyci B是一种使菌类缺糖的蒽环抗生素。这些新开发的化合物比母体化合物抗白血病的作用强得多。在已制备的15种化合物中,有3种衍生物对小鼠P388白血病的抗肿瘤作用与母体化合物比较特别明显。英国Beecham制药公司最近研制出一种抗疱疹病毒药BRI-39123的前体药物BRI-42810,口服有效。在证实该新药有很好的抗病毒活性后便被指定作进一步的评估并在志愿者身上作研究。
Pfizer and researchers at St Mary’s School of Medicine in the UK have co-developed a new α-adrenergic receptor antagonist (UK-570-46-27). Allegedly, this new selective compound of the heart muscle can effectively reduce the incidence of isolated heart arrhythmia in guinea pigs, and change the electrical parameters of cells under myocardial ischemia and repeated perfusion. Upjohn, a U.S.-based company, has developed a series of analogues of the 3-substituted Steffimyci B, an anthracycline antibiotic that causes the yeast to be sugar-deficient. These newly developed compounds are much more potent anti-leukemias than the parent compound. Among the 15 compounds that have been prepared, the antitumor effects of three of the derivatives on mouse P388 leukemia are particularly evident compared to the parent compound. British Beecham Pharmaceutical Company recently developed BRI-3928, a prodrug of anti-herpes virus agent BRI-42810, which is orally effective. After confirming that the new drug has good antiviral activity, it was designated for further evaluation and research on volunteers.