Preparations of N-[3-(hetero)aryl-aminocarbonyl]propanoyl-L-proline derivatives 12, 13, 22 and 23 are described. A novel approach consists of fusing (80-100 °C) N-(hetero)aryl-succinimides (7, 8, 20, 21) with unprotected L-proline and imidazole in the presence of dimethylformamide. In vitro tests for angiotensin converting enzyme (ACE) inhibition showed that all N-(arylaminocarbonyl)-propanoyl-...

In this study, the effects of solvents and molecular structure upon acidity, five 3-alkyl(aryl)-4-phthalimido-4,5-dihydro-1H-1,2,4-triazol-5-ones (3-7) were potentiometrically titrated with tetrabutylammonium hydroxide (TBAH) in four different anhydrous (isopropyl alcohol, acetonitrile, tert-butyl alcohol N,N-dimethylformamide) HNP corresponding pKa values determined by half-neutralization meth...

A series of novel 4-substituted-N-(phenylcarbamoyl)-3-pyridinesulfonamides 11-27 have been synthesized by the reaction of 4-substituted pyridine-3-sulfonamides 2-10 with the appropriate aryl isocyanates in presence of potassium carbonate. The in vitro anticancer activity of compounds 11, 12, 14-21 and 24-26 was evaluated at the U.S. National Cancer Institute and in light of the results, some st...

Title Page 1 2 Activation of aryl hydrocarbon receptor mediates suppression of hypoxia inducible 3 factor-dependent erythropoietin expression by indoxyl sulfate 4 5 Hirobumi Asai, Junya Hirata, Ayumi Hirano, Kazuya Hirai, Sayaka Seki and Mie 6 Watanabe-Akanuma 7 8 Safety Research Center, Kureha Corporation, 3-26-2 Hyakunin-cho, Shinjuku-ku, 9 Tokyo 169-8503, Japan 10 11 12 Running Head: Indoxyl...