| Autor: |
Wilde RG; DuPont Merck Pharmaceutical Company, DuPont Experimental Station, Wilmington, DE 19880-0500, USA., Billheimer JT, Germain SJ, Hausner EA, Meunier PC, Munzer DA, Stoltenborg JK, Gillies PJ, Burcham DL, Huang SM, Klaczkiewicz JD, Ko SS, Wexler RR |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry [Bioorg Med Chem] 1996 Sep; Vol. 4 (9), pp. 1493-513. |
| DOI: |
10.1016/0968-0896(96)00143-5 |
| Abstrakt: |
Acyl-CoA:cholesterol acyltransferase (ACAT) is the enzyme largely responsible for intracellular cholesterol esterification. A systemic inhibitor of ACAT is believed to be able to slow or even reverse the atherosclerotic process. Towards that goal, a series of cyclic sulfides, derived from the hetero-Diels-Alder reaction of thioaldehydes with 1,3-dienes, and bearing carboxamide substituents, were prepared and evaluated for in vitro (in several tissues and species) and ex vivo ACAT inhibition. Minor changes in subsequent structure were found to have a significant effect in optimization of the biological activity of this series of compounds. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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