SSR182289A, a selective and potent orally active thrombin inhibitor

Design, synthesis and evaluation of graftable thrombin inhibitors for the preparation of blood-compatible polymer materials

“…13, 14 Historically, two research lines have been developed in parallel: (i) the steric inhibitors (non-covalently bound) based on two simple lead compounds, namely N-tosyl-L-arginine methyl ester (TAME, Fig. 1), 15 and benzamidine;…”

“…Native polyester membranes (14) were cut into disks of 13 mm of diameter. The polymer samples (10 disks) were stirred at 20…”

Synthesis of ethynylated biaryls and asymmetric diethynylated benzene via sequential Sonogashira and Suzuki couplings in water

“…Using NaOH/TBAB/water as catalytic system in the presence of 1 mol% Pd-cat I at reflux temperature for 8 hr gave only 50% yield and the starting material did not completely consume (Table 1, run 1). Repeating the same conditions using 2 mol% of the Pd-cat I resulted in full conversion into the cross-coupled product 1-phenyl-2-(4-biphenylyl)acetylene (7) in 85% isolated yield (Table 1, run 2). Under the typical conditions above, when water was replaced with toluene at reflux for 4 hr, the product 6 was obtained in 73% yield ( Pd-Cat II When Suzuki coupling of the 1-bromo-4-(2-phenylethynyl)benzene (4) with 3-chlorophenylboronic acid (6b) was similarly carried out in H 2 O/K 2 CO 3 /TBAB reaction system under thermal heating at 100 °C using 1 mol% Pd-cat.…”

“…[3][4][5][6][7][8] In addition, Suzuki-Miyaura cross-coupling reaction is one of the most versatile and utilized reactions for carbon-carbon bond formation in the synthesis of natural products and pharmaceuticals. [9][10][11][12][13] Water as an available, cheap, renewable, safe and green solvent and allows easy work up and separation, has been exploited in several catalytic C-C bond formation reactions and was reported as an important partner in improving the catalyst activity.…”

Tripeptides with non-code amino acids as potential serine proteases inhibitors

“…At the P2 thrombin has strict preference to proline, it has not strong correlation at the P3 and has a preference for aliphatic amino acids in the P4. Thrombin inhibitors are classified as indirect inhibitors (heparin) and direct inhibitors (hirudin, bivalirudin, argatroban, dabigatran 9,10 ). Argatroban and dabigatran mimic D-Phe-Pro-Arg thrombin peptide substrate.…”