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Chemical Compound Review:

Fragment 17 isoquinolin-1-amine

Synonyms: PubChem18941, CHEMBL62083, SureCN49220, SureCN392338, AG-D-79209, ...

Lam, P.Y. et al., Pauls, H.W. et al.

Lam, Clark, Li, Pinto, Orwat, Galemmo, Fevig, Teleha, Alexander, Smallwood, Rossi, Wright, Bai, He, Luettgen, Wong, Knabb, Wexler, Pauls, Ewing,

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High impact information on isoquinolin-1-amine

SQ311, which utilizes a 1-aminoisoquinoline as the P1 ligand, inhibits factor Xa with a K(i) of 0.33 nM and demonstrates both good in vivo antithrombotic efficacy and oral bioavailability [1].
The first active and bioavailable benzamidine isostere i.e. the 1-aminoisoquinoline (RPR208815, Ki = 22 nM) was discovered on the pyrrolidinone scaffold (Part 2.3) [2].

References

Structure-based design of novel guanidine/benzamidine mimics: potent and orally bioavailable factor Xa inhibitors as novel anticoagulants. Lam, P.Y., Clark, C.G., Li, R., Pinto, D.J., Orwat, M.J., Galemmo, R.A., Fevig, J.M., Teleha, C.A., Alexander, R.S., Smallwood, A.M., Rossi, K.A., Wright, M.R., Bai, S.A., He, K., Luettgen, J.M., Wong, P.C., Knabb, R.M., Wexler, R.R. J. Med. Chem. (2003) [Pubmed]
The design of competitive, small-molecule inhibitors of coagulation factor Xa. Pauls, H.W., Ewing, W.R. Current topics in medicinal chemistry. (2001) [Pubmed]

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