Acyl, N-protected. alpha.-aminoacyl, and peptidyl derivatives as prodrug forms of the alcohol deterrent agent cyanamide

CH Kwon, HT Nagasawa, EG DeMaster…

Index: Kwon, Chul-Hoon; Nagasawa, Herbert T.; DeMaster, Eugene G.; Shirota, Frances N. Journal of Medicinal Chemistry, 1986 , vol. 29, # 10 p. 1922 - 1929

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Citation Number: 28

Abstract

Cyanamide (H, NC= N), a potent aldehyde dehydrogenase (AlDH) inhibitor that is used therapeutically as an alcohol deterrent agent, is known to be rapidly metabolized and excreted in the urine as acetylcyanamide (1). On the basis of our observation that 1 is deacetylated to cyanamide in vivo, albeit very slightly, thereby serving as a precursor or prodrug form of the latter, several acyl derivatives of cyanamide were synthesized ...