- Inhibitors of acyl-CoA:cholesterol O-acyltransferase (ACAT) as hypocholesterolemic agents: Synthesis and structure-activity relationships of novel series of sulfonamides, acylphosphonamides and acylphosphoramidates
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Sulfoacetic acid, phosphoramidate, and phosphonamide analogs of the ACAT inhibitors, CI-999 and CI-1011 were synthesized. The structure-activity relationships of these compounds as ACAT inhibitors are described.
- Lee,Roark,Picard,Sliskovic,Roth,Stanfield,Hamelehle,Bousley,Krause
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p. 289 - 294
(2007/10/03)
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- β-carboxy sulfonamide ACAT inhibitors
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β-Carboxy sulfonyl compounds of the formula STR1 wherein R1 is aryl, R3 is hydrogen or alkyl, R3 and R4 are hydrogen or alkyl, Y is --O--, --S--, or --NR2 --, and R5 is alkyl or aryl are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia and atherosclerosis.
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- Sulfonamide tetrazole ACAT inhibitors
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Pharmaceutically useful compounds having ACAT inhibitory activity of the formula STR1 wherein R1 is phenyl, substituted phenyl, naphthyl, substituted naphthyl, a heteroaromatic group or a hydrocarbon group having from 1 to 18 carbon atoms; Rsu
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