| 摘要 |
<p>New pharmacologically active dipeptides are of formula NH2-Tyr-Pro-OH (I), in which Tyr represents an opt. substd. tyrosine residue and Pro represents an opt. substd. proline residue. The amine acid residues may be in D-NL-form and the C-terminal may be free from or in the form of the amide, ester or hydrazide. Pref. dipeptides are of formula (Ia) (when R1 is H or 1-4C alkyl; R2 is H or OH; R3 is H, 1-4C alkoxy or -CO-R4; R4 is opt. unsatd. 1-17C alkyl, or phenyl or 7-12C phenylalkyl opt. mono-or disubstd. by halogen, 1-4C alkyl and/or 1-4C alkoxy; W is H, 1-5C alkyl, 3-5C alkenyl, cyclopropylmethyl, cyclobutylmethyl or -CO-R4; and R7 is H, OH, 1-4C alkyl or 1-4C alkoxy; and the pyrrolidine ring can carry one or more keto gps. to be in the form of dehydroproline). The dipeptides exert neuroleptic activity, and can be used in medicine as antipsychotics, tranquilisers and/or neuroleptics. In addn., the dipeptides may be coupled to thyroglobulin or other macromolecular proteins and used as antigens for the prodn. of antibodies which may in turn be used for the determination of the dipeptides in tissues or body fluids.</p> |
