Abstract:
:We have already reported unique compounds containing a N,O-spiro acetal structure as an orally active factor Xa (FXa) inhibitor. This time, we described a N,N-spiro acetal structure as an analogue of the N,O-spiro acetal structure for an orally active FXa inhibitor. The synthesis of these analogues could be achieved in a similar fashion to the N,O-spiro acetal synthesis. Consequently, FXa inhibitory activity was increased and more active compounds could be found (M58163: IC50 = 0.61 nM, M58169: IC50 = 0.58 nM). Additionally, the absolute configuration could be determined by X-ray crystallography analysis (M58169: (R)-config.).
journal_name
Chem Pharm Bull (Tokyo)journal_title
Chemical & pharmaceutical bulletinauthors
Saitoh F,Mukaihira T,Nishida H,Satoh T,Okano A,Yumiya Y,Ohkouchi M,Johka R,Matsusue T,Shiromizu I,Hosaka Y,Matsumoto M,Ohnishi Sdoi
10.1248/cpb.54.1535subject
Has Abstractpub_date
2006-11-01 00:00:00pages
1535-44issue
11eissn
0009-2363issn
1347-5223pii
JST.JSTAGE/cpb/54.1535journal_volume
54pub_type
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