close

Вход

Забыли?

вход по аккаунту

?

код для вставки
2005
Pyrrole derivatives
R 0120
Synthesis and Evaluation of Novel Peripherally Restricted κ-Opioid Receptor
— To further improve the peripheral restriction of a highly potent κ-agonist,
25- 113 Agonists.
analogues with modifications on the central phenyl ring are synthesized and evaluated
for in vitro binding affinity and in vivo antinociceptive activity. The oxygenated analogues of the central phenyl ring of the lead, cf. (VII)—(X), are prepared as racemates.
The corresponding amino analogues, e.g. (XII), are prepared as optically pure compounds following a literature procedure. Almost all compounds potently bind to the
κ-receptor in vitro and they are selected for κ- or µ- and δ-opioid receptors. The degree
of peripheral restriction of these κ-agonists is improved approximately 2- to 7-fold.
— (KUMAR*, V.; et al.; Bioorg. Med. Chem. Lett. 15 (2005) 4, 1091-1095; Dep.
Chem., Adolor Corp., Exton, PA 19341, USA; Eng.) — H. Hoennerscheid
Документ
Категория
Без категории
Просмотров
0
Размер файла
24 Кб
Теги
1/--страниц
Пожаловаться на содержимое документа