benzofurans and dicyandiamido

benzofurans has been researched along with dicyandiamido* in 1 studies

Other Studies

1 other study(ies) available for benzofurans and dicyandiamido

Article	Year
Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors. Bioorganic & medicinal chemistry letters, 2009, Aug-01, Volume: 19, Issue:15 The N,N'-disubstituted cyanoguanidine is an excellent bioisostere of the thiourea and ketene aminal functional groups. We report the design and synthesis of a novel class of cyanoguanidine-based lactam derivatives as potent and orally active FXa inhibitors. The SAR studies led to the discovery of compound 4 (BMS-269223, K(i)=6.5nM, EC(2xPT)=32muM) as a selective, orally bioavailable FXa inhibitor with an excellent in vitro liability profile, favorable pharmacokinetics and pharmacodynamics in animal models. The X-ray crystal structure of 4 bound in FXa is presented and key ligand-protein interactions are discussed. Topics: Administration, Oral; Animals; Antithrombin III; Benzofurans; Chemistry, Pharmaceutical; Crystallography, X-Ray; Dogs; Guanidines; Haplorhini; Humans; Inhibitory Concentration 50; Kinetics; Lactams; Ligands; Models, Chemical; Rats; Structure-Activity Relationship; Thiourea	2009

Article

Year

Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors.

Bioorganic & medicinal chemistry letters, 2009, Aug-01, Volume: 19, Issue:15

The N,N'-disubstituted cyanoguanidine is an excellent bioisostere of the thiourea and ketene aminal functional groups. We report the design and synthesis of a novel class of cyanoguanidine-based lactam derivatives as potent and orally active FXa inhibitors. The SAR studies led to the discovery of compound 4 (BMS-269223, K(i)=6.5nM, EC(2xPT)=32muM) as a selective, orally bioavailable FXa inhibitor with an excellent in vitro liability profile, favorable pharmacokinetics and pharmacodynamics in animal models. The X-ray crystal structure of 4 bound in FXa is presented and key ligand-protein interactions are discussed.

Topics: Administration, Oral; Animals; Antithrombin III; Benzofurans; Chemistry, Pharmaceutical; Crystallography, X-Ray; Dogs; Guanidines; Haplorhini; Humans; Inhibitory Concentration 50; Kinetics; Lactams; Ligands; Models, Chemical; Rats; Structure-Activity Relationship; Thiourea

2009