申请人:The Regents of the University of California
公开号:US04837305A1
公开(公告)日:1989-06-06
Molecular structures of .beta.-adrenergic antagonists are modified to produce biologically active compounds. The .beta.-antagonists are modified to form molecules of the general structure: ##STR1## wherein R is most generally R"--OCH.sub.2 --, and in some instances is R"--, and R"=an aryl or substituted aryl moiety; R'=--H, --CH.sub.3, or a short chain alkyl moiety; and Y=--OH, or more usually, --OAX or --NHAX, where A=an alkyl, aryl, or aralkyl moiety, and X=a terminal grouping, such as --CH.sub.3, --CF.sub.3 or --(CH.sub.2).sub.n COOH; or AX may be a carrier moiety consisting of a defined peptide or protein.
β-肾上腺素拮抗剂的分子结构被改变以产生生物活性化合物。β-拮抗剂被改变以形成通用结构的分子:##STR1## 其中R通常为R"--OCH.sub.2 --,在某些情况下为R"--,而R"为芳基或取代芳基基团;R'=--H,--CH.sub.3或短链烷基基团;Y=--OH,或更通常的是--OAX或--NHAX,其中A=烷基、芳基或芳基烷基基团,X=末端基团,例如--CH.sub.3、--CF.sub.3或--(CH.sub.2).sub.n COOH;或AX可以是由定义的多肽或蛋白质组成的载体基团。