Fluorobenzamidrazone thrombin inhibitors: Influence of fluorine on enhancing oral absorption

Bioorganic and Medicinal Chemistry Letters

Volumn 9, Issue 17, 1999, Pages 2483-2486

  Lee, Koo ^a   Jung, Won Hyuk ^a   Sang, Yeul Hwang ^a   Lee, Sung Hack ^a  

^a LG Chemical Ltd   (South Korea)

Author keywords

[No Author keywords available]

Indexed keywords

DRUG ANALOG; FLUORINE; FLUOROBENZAMIDRAZONE; FLUOROBENZAMIDRAZONE DERIVATIVE; IB 30057; THROMBIN; THROMBIN INHIBITOR; TRYPSIN; UNCLASSIFIED DRUG;

ARTICLE; CHEMICAL MODIFICATION; DOG; DRUG ABSORPTION; DRUG POTENCY; DRUG SELECTIVITY; DRUG SYNTHESIS; HUMAN; NONHUMAN; ORAL DRUG ADMINISTRATION; RAT; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; ANTITHROMBINS; BENZAMIDES; DOGS; FLUORINE; RATS;

EID: 0033530115     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(99)00412-6     Document Type: Article

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26. Some substituents investigated other than fluorine were disappointing, including chlorine, bromine, and amino groups. These substituents resulted in at least a 30-fold decrease in thrombin inhibitory potency as compared to the unsubstituted parent.