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2005
Pyridine derivatives
R 0380
Synthesis and Evaluation of 4-(1-Aminoalkyl)-N-(4-pyridyl)cyclohexanecarboxas Rho Kinase Inhibitors and Neurite Outgrowth Promoters. — The ste03- 135 amides
reochemistry and the length of the amino alkyl chain of the Rho kinase inhibitor
Y-27632, composed of a rigidifying cyclohexane body with a pyridyl amide head and
amino—ethyl tail, are modified to investigate the influence of these alterations on its
kinase inhibitor activity and biology. Two alternative routes are developed for synthesizing derivatives of Y-27632 modified at the alkyl amine. The second method uses a
chiral dioxaborolane derivative, (II), and an olefin metathesis [(VII)→(IX)] to introduce a stereogenic center and to extend the alkyl chain. Compound Y-27632 and its
enantiomer are able to inhibit Rho kinase activity and promote neurite outgrowth. In
contrast, octyl analogue (XII) does not stimulate neurite outgrowth and induces cell
rounding. No clear relationship between Rho kinase inhibition and neurite outgrowth
promotion is observed. — (GINGRAS, K.; AVEDISSIAN, H.; THOUIN, E.;
BOULANGER, V.; ESSAGIAN, C.; MCKERRACHER, L.; LUBELL*, W. D.;
Bioorg. Med. Chem. Lett. 14 (2004) 19, 4931-4934; Dep. Chem., Univ. Montreal,
Montreal, Que. H3C 3J7, Can.; Eng.) — H. Hoennerscheid
2005
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