30134-76-0Relevant articles and documents
Resolution, Absolute Configuration, and Cholinergic Enantioselectivity of (+)- and (-)-cis-2-Methyl-5--1,3-oxathiolane Methiodide
Teodori, Elisabetta,Gualtieri, Fulvio,Angeli, Piero,Brasili, Livio,Giannella, Mario,Pigini, Maria
, p. 1610 - 1615 (1986)
The potent cholinergic agonist (+/-)-cis-2-methyl-5--1,3-oxathiolane methiodide was resolved into enantiomeric forms.Their absolute configurations were established by a synthetic pathway that also allowed the synthesis of the corresponding diastereomeric (+)- and (-)-trans-2-methyl-5--1,3-oxathiolane methiodide .Compound (+)-1, which is the most potent of the four isomers, showed the same absolute configuration as L-(+)-muscarine and (+)-cis-dioxolane.The four isomers were tested on guinea pig ileum and frog rectus abdominis, and their muscarinic and nicotinic potency (EPMR) and selectivity were determined.The relationships between stereoisomerism and potency are discussed.
COMPOUNDS AND COMPOSITIONS AS CATHEPSIN S INHIBITORS
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Page/Page column 28, (2010/02/14)
The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cathepsin S.
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.