cas 84102-77-2, Methyl 5-cyanobenzofuran-2-carboxylate | Articles data ｜lookchem

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84102-77-2

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Use of conformationally restricted benzamidines as arginine surrogates in the design of platelet GPIIb-IIIa receptor antagonists
The use of 5,6-bicyclic amidines as arginine surrogates in the design of a novel class of potent platelet glycoprotein IIb-IIIa receptor (GPIIb-IIIa) antagonists is described. The additional conformational restriction offered by the bicyclic nucleus results in 20-400-fold increases in potency compared to the freely flexible, acyclic benzamidine counterpart. The design, synthesis, structure-activity relationships (SAR), and in vitro activity of this novel class of GPIIb-IIIa antagonists are presented.
Sall, Daniel J.,Arfsten, Ann E.,Bastian, Jolie A.,Denney, Michael L.,Harms, Cathy S.,McCowan, Jefferson R.,Morin Jr., John M.,Rose, Jack W.,Scarborough, Robert M.,Smyth, Mark S.,Um, Suzane L.,Utterback, Barbara G.,Vasileff, Robert T.,Wikel, James H.,Wyss, Virginia L.,Jakubowski, Joseph A.
p. 2843 - 2857
(2007/10/03)

5,6-Bicyclic glycoprotein IIb IIIa antagonists useful in inhibition of platelet aggregation
This invention relates to 5,6 fused ring bicyclic compounds inclusive of indoles, benzofurans, and benzothiophenes, and corresponding to the formula (I) substituted with both basic (B) and acidic (A) functionality, which are useful in inhibition of platelet aggregation.
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(2008/06/13)

Syntheses of Biscationic, Trypanocidal 1-Benzofuran Compounds
2-Phenyl-1-benzofurans with the substituents Br, NO2, CN, and -NH2, -NH-C(=NH)-NH2, -C(=NH)-NH2, in 4',5-position were synthesized. - For arylated formamidine derivatives a simple new preparation was found by reacting amine hydrochlorides with dimethylformamide in the presence of cyanamide. - Based on 5- or 6-cyano-1-benzofuran-2-carboxylates a series of α,ω-bis(1-benzofuran-2-yl) derivatives with cyano-, amidino-, or imidazolinyl groups in 5- or 6-position was prepared.
Dann, Otto,Char, Helmut,Griessmeier, Helmut
p. 1836 - 1869
(2007/10/02)

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Chemical Properties

Storage Temp.:2-8°C
PSA: 63.23000
LogP: 2.09108

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