143619-73-2Relevant academic research and scientific papers
N-(arylacetyl)-biphenylalanines as potent VLA-4 antagonists.
Li, Bing,de Laszlo, Stephen E,Kamenecka, Theodore M,Kopka, Ihor E,Durette, Philippe L,Lanza Jr., Thomas,MacCoss, Malcolm,Tong, Sharon,Mumford, Richard A,McCauley, Ermengilda D,Van Riper, Gail,Schmidt, John A,Hagmann, William K
, p. 2141 - 2144 (2007/10/03)
A series of potent N-(aralkyl-, arylcycloalkyl-, and heteroaryl-acyl)-4-biphenylalanine VLA-4 antagonists was prepared by rapid analogue methods using solid-phase chemistry. Further optimization led to several highly potent compounds (IC(50) 1 nM). Evalu
Synthesis and Biological Activity of trans-(+/-)-N-Methyl-2-(3-pirydyl)-2-tetrahydrothiopyrancarbothioamide 1-Oxide (RP 49356) and Analogues: A New Class of Potassium Channel Opener
Brown, Thomas J.,Chapman, Robert F.,Cook, David C.,Hart, Terance W.,McLay, Iain M.,et al.
, p. 3613 - 3624 (2007/10/02)
The synthesis and biological activity of trans-(+/-)-N-methyl-2-(3-pyridyl)-2-tetrahydrothiopyrancarbothioamide 1-oxide (8a, RP 49356) and analoques is reported.These compounds constitute a new structural class of K+-channel opener.The effects of changes in the pyridyl group, thioamide, and thiane ring on in vitro K+-channel opening activity are discussed.A 3-pyridyl or 3-quinolyl group, a small N-alkyl thioamide function, and a thiane oxide ring, in which the sulfoxide is in a trans relationship to thioamide, are preferred for activity.Selected compounds were tested intravenously in the normotensive anaesthetized rat for hypotensive effects, and the activities reflect their in vitro K+-channel opening activity.This led to further evaluation of compound 8a and the selection of the (-)-enantiomer 8b (RP 52891) for development as an antihypertensive and antianginal agent.
