110660-78-1Relevant articles and documents
Design, synthesis, and tripeptidyl peptidase II inhibitory activity of a novel series of (S)-2,3-dihydro-2-(4-alkyl-1H-imidazol-2-yl)-1H-indoles
Breslin, Henry J.,Miskowski, Tamara A.,Kukla, Michael J.,Leister, William H.,De Winter, Hans L.,Gauthier, Diane A.,Somers, Maria V. F.,Peeters, Dani?lle C. G.,Roevens, Peter W. M.
, p. 5303 - 5310 (2007/10/03)
Butabindide, 1, was previously reported as a potent inhibitor (IC50 = 7 nM) of the serine protease enzyme tripeptidyl peptidase II (TPPII), an endogenous protease that degrades cholecystokinin-8 (CCK-8). We found that 1 has some inherent chemical instability, yielding diketopiperazine 2 fairly readily under mimicked physiological conditions. We therefore prepared imidazoles 3, which are void of 1's inherent instability, and have found that our novel analogues maintained comparable TPPII inhibitory activity (e.g., for 3c, IC50 = 4 nM) as 1.
GAMMA-R-GLUTAMOYL DERIVATIVES
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, (2008/06/13)
A compound of the formula STR1 wherein R 1 and R 6 independently represent hydroxy, C 1-C 4-alkoxy, substituted C. sub.1-C 4-alkoxy, amino, or substituted amino, R 2 represents hydrogen, C 1-C 4-alkyl, or C 2-C 4-alkenyl, R 3 represents cyclo-C. sub.3-C 6-alkyl, phenyl, phenyl substituted by C. sub.1-C 4-alkyl, halogen, nitro, or C 1-C 4-alkoxy, or cyclo-C 3-C 6-alkyl fused with benzene, or wherein R 2 and R 3 are connected and together with the adjacent--CH-group and the adjacent N-atom form a saturated or partially saturated, monocyclic, five-or six-membered heterocyclic group or form a saturated or partially saturated, bicyclic heterocyclic group containing five or six atoms per ring, R 4 represents hydrogen or C 1-C 4-alkyl, and R 5 represents an acyl group, are useful as antihypertensive and cardioactive agents. The invention also relates to processes for preparing the compounds of the formula I and to pharmaceutical compositions.
