140372-02-7Relevant academic research and scientific papers
Arylaminoethyl carbamates as a novel series of potent and selective cathepsin S inhibitors
Tully, David C.,Liu, Hong,Chatterjee, Arnab K.,Alper, Phil B.,Williams, Jennifer A.,Roberts, Michael J.,Mutnick, Daniel,Woodmansee, David H.,Hollenbeck, Thomas,Gordon, Perry,Chang, Jonathan,Tuntland, Tove,Tumanut, Christine,Li, Jun,Harris, Jennifer L.,Karanewsky, Donald S.
, p. 5107 - 5111 (2007/10/03)
We report a novel series of noncovalent inhibitors of cathepsin S. The synthesis of the peptidomimetic scaffold is described and structure-activity relationships of P3, P1, and P1′ subunits are discussed. Lead optimization to a non-peptidic scaffold has r
ANGIOTENSIN CONVERTING ENZYME INHIBITORS
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, (2008/06/13)
Angiotensin converting enzyme inhibitors have the formula Z(CH. sub.2). sub.n CHR 1 COOCHR 2 COOHin which Z is--SR. sub. 3,--COCHR 4 NHCOR 5, STR1 or--NHCHR 7 COOH, R. sub.4, R. sub.5, R 6, and R 7, which may be the same or different, are each phenyl or alkylphenyl C 7-12,R 4 is hydrogen, alkyl C 1-6, NHR 8 or (CH 2) p R 9, R 2 is (CH 2) m XR 10, alkyl C 1-6 optionally substituted by a saturated 5-or 6-membered carbocyclic or heterocyclic ring, alkylhalo C 1-6, alkylcyano C 1-6, or alkyl phenyl C 7-12, the phenyl being optionally substituted by NO 2 or NH 2,X is O, S(O) q, C=O or NR 11, andR 10 is alkyl C 1-6, alkylhalo C 1-6, alkoxy C 1-6, alkoxy C 1-6 substituted by halogen, alkanoyl C 1-6, S(O) r R. sub.12, NR 13 R 14, phenyl, alkylphenyl C 7-12, naphthalenyl or a 5-membered unsaturated heterocyclic ring, n is an integer from 0 to 6,m and p, which may be the same or different, are each an integer from 1 to 6,R 9 is hydrogen, SR 15 or phenyl optionally substituted by OR 16,R 3 and R 15, which may be the same or different, are each hydrogen or alkanoyl C 1-6,R. sub.8 is hydrogen or COOR 17,q and r, which may be the same or different, are each 0, 1, or 2,R 11, R. sub.13, R. sub.14, R 16, and R 17, which may be the same or different, are each hydrogen or alkyl C 1-6, and R 12 is hydrogen, alkyl C 1-6 or phenyl.The compounds, and salts thereof, are useful as vasodilators.
