| 摘要 |
<p>N-Substd.-L-alanyl-L-proline derivs. and analogues of formula (I) and their salts are new. R1-A1-X-A2-CR2(Q2-R2O)-NR3-CHR4-CO -NR5-CR6R16-Q1-R10 (I) In (I) either (1) R1 is aryl or heterocyclyl, and A1 is a direct link or (2) R1 is aryl, heterocyclyl, H, halogen, OH, NH2, guanidino, SH, COOH, CONH2, R11-O, R11R21N, R11R21NCO, R11CONH, R11S or R11OCO, and A1 is 1-15C alkylene, (cyclo)alkylene or cycloalkenylene; R11 is alkyl or Ph; R21 is H or alkyl; X is CO, CH(OH), CH(OR11), CH(O-COR11), C:N(OR12), C:N(O-COR11), CH-NH(OR12), CH-NH(O-COR11), C:N-NH-CONH2, C(OR13)(OR14) or C(SR13)(SR14); R12 is H or alkyl opt. substd. by aryl; R13 and R14 are alkyl; or R13+R14 is alkylene; A2 is alkylene, alkenylene or alkylidene; or X-A2 is C(OR11):CR15-A3 or C(O-COR11):CR15-A3; R15 is H or alkyl; A3 is absent or is alkylene; R2 is H, alkyl, opt. substd. by aryl, or Q2-R2O; R3 is H, alkyl, CH2-O-COR11, COR21 or COOR11; R4 is H, alkyl (opt. substd.), alkoxy, (di)alkylamino, 1-5C alkylthio or cyclic amino; or alkanoylamino, alkoxycarbonylamino or alkoxycarbonyl; arylalkoxy-carbonyl; or aryl or heterocyclyl; R5 is H or alkyl opt. substd. by aryl; R6 is H, aryl, heterocyclyl, or alkyl (opt. substd.); or R5+R6 form alkylene or alkenylene, or their oxa, thia or aza derivs., or they are opt. substd. by a OH or oxo; R16 is H, alkyl or Q1-R10; or R6+R16 is alkylene; or R16 together with the first C atom of R6 form a double bond where R6 is otherwise alkyl (opt. substd.) or where R6+R5 are otherwise joined together as above (i.e. R5, R6 and R16 together form alkylidene); Q1 and Q2 are CO or CH2; either R10 and R20 are eg. OH, NH2, hydroxyamino, aryloxy, arylthio, alkenyloxy, (cyclo)alkoxy, (di)alkylamino, cyclic amino, hydroxyalkoxy, acyloxyalkoxy, (di)(alkyl)aminoalkoxy, cyclic aminoalkoxy, alkanoylaminoalkoxy, etc. or R10 and R6 are joined together such that R10 is O joined to the terminal C of R6 when it is alkyl.</p> |
