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2005
Medicinal chemistry
V 1100
CVT-4325: A Potent Fatty Acid Oxidation Inhibitor with Favorable Oral Bio— The "left hand" side of a lead palmCoA oxidation inhibitor is investi15- 236 availability.
gated to optimize the potency and metabolic stability. Suitable bioisosteric replacements for the amide group are achieved by preparing various nitrogen heterocycles. Introduction of an oxadiazole derivative as an amide surrogate results in both good palmCoA inhibition and a favorable pharmacokinetic profile. Compound (I) causes a metabolic shift from fatty acids to glucose. — (ZABLOCKI*, J. A.; et al.; Bioorg. Med.
Chem. Lett. 14 (2004) 24, 6017-6021; Dep. Bioorg. Chem., CV Therapeutics Inc.,
Palo Alto, CA 94304, USA; Eng.) — H. Hoennerscheid
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