[Synthesis of N-(4-carbomethoxy-4-phthalimidobutanoyl)-N-substituted glycines, proline and pyroglutamic acid].
This paper reports the synthesis of eleven N-(4-carbomethoxy-4-phthalimidobutanoyl)-N-substituted glycines (VII1-9), proline (VII10) and pyroglutamic acid (VII11) expected to have inhibitory activity on angiotensin converting enzyme. All of the compounds mentioned above and the corresponding t-butyl esters of VII1-9 were not reported in the literature previously. The structures were confirmed through their IR, 1HNMR, MS spectra and elemental analysis. In preliminary test in rats, compounds VII8, VII9 and VII10 showed marked hypotensive activity.
Lin
W Q
WQ
School of Pharmacy, West China University of Medical Sciences, Chengdu.
Cai
C Y
CY
Gong
K S
KS
Wu
Y
Y
Long
Z
Z
Luo
X X
XX
Yang
L
L
Li
J F
JF
Yao
X J
XJ
D000806:Angiotensin-Converting Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D051381:Rats; D017207:Rats, Sprague-Dawley
D000806:Angiotensin-Converting Enzyme Inhibitors