Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: A novel, potent and orally active direct inhibitor of factor Xa

Add time:07/25/2019    Source:sciencedirect.com

In the early 1990’s, we reported on the low-molecular selective fXa inhibitor DX-9065a having two amidino groups. However, it had poor oral bioavailability due to its strong basic amidino groups. To obtain fXa inhibitors with improved oral bioavailability, we investigated various non-amidino fXa inhibitors and finally discovered cis-1,2-diaminocyclohexane derivative 4c to have potent fXa inhibition, promising anticoagulant activity, and good oral bioavailability, compared with amidino compound DX-9065a. In addition, we will discuss the influence of the third substituent on the cyclohexane ring on anti-fXa activity, anticoagulant activity, PK profile, and lipophilicity.

We also recommend Trading Suppliers and Manufacturers of 4-IODO-BENZAMIDINE HYDROCHLORIDE (cas 134322-01-3). Pls Click Website Link as below: cas 134322-01-3 suppliers

Prev:Synthesis of 11β-(4-dimethylaminophenyl)-17β-hydroxy-17α- (3-methyl-1-butynyl)-4, 9-estradien-3-one and 11β-(4-acetophenyl)- 17β-hydroxy-17α-(3-methyl-1-butynyl)-4, 9-estradien-3-one: two new analogs of mifepristone (RU-486)☆,☆☆2,☆☆☆2
Next:SERRATE, a miRNA biogenesis factor, affects viroid infection in Nicotiana benthamiana and Nicotiana tabacum)