161620-93-5Relevant articles and documents
Amidino derivatives and their use as thrombin inhibitors
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, (2008/06/13)
There is provided compounds of formula I, wherein R1, R2, R3, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
Diarylsulfonamides as selective, non-peptidic thrombin inhibitors
Weber, Ingo R.,Neidlein, Richard,Von Der Saal, Wolfgang,Grams, Frank,Leinert, Herbert,Strein, Klaus,Engh, Richard A.,Kucznierz, Ralf
, p. 1613 - 1618 (2007/10/03)
Based on the structures of aminopyridine thrombin inhibitors (1), a series of aminoalkyl- and guanidinoalkyl-substituted diarylsulfonamides were prepared. The most potent derivative, N-[3-(4-guanidinobutoxy)-5-methyl- phenyl]-benzenesulfonamide (6c) had Ki = 0.18 μM for thrombin and did not inhibit trypsin, plasmin, or factor Xa. Comparison of the X-ray structures of the thrombin / 1b and the thrombin / 6e complexes revealed important aspects which govern the binding of such diarylsulfonamides to thrombin.
Synthesis of the benzo[b] carbazoloquinone with the structure proposed for prekinamycin
Echavarren, Antonio M.,Tamayo, Nuria,Carmen Paredes
, p. 4713 - 4716 (2007/10/02)
The synthesis of the N-cyano benzo[b]carbazolequinone with the structure proposed for prekinamycin has been achieved by palladium and copper catalyzed coupling of a 2-bromonaphthoquinone with an arylstannane followed by ring closure, N-cyanation, and demethylation. Unexpectedly, the ring closure reaction gave also a regioisomer by an unprecedented rearrangement reaction.