close

Вход

Забыли?

вход по аккаунту

?

код для вставки
2004
Peptides
U 0400
52- 172
Identification of a Potent and Rapidly Reversible Inhibitor of the 20S-Proteasome.
— Focused screening of a collection of compounds identifies a potent, lactam based
boronate proteasome inhibitor for the chymotrypsin-like activity. This inhibitor exists
as a 1:1 diastereomeric mixture at the quaternary center at the ring junction. To investigate the stereospecificity of this inhibitor, the required lactam (X) is synthesized. Lactam (X) is resolved into two diastereomers, (XI) and (XII), and separately converted
into the corresponding diastereomers, cf. (XIII). In addition, the effects of replacement
of the sulfonamide and cyclohexylmethyl alanine as well as substitution effects at the
boronate side chain are examined. Compound (XIII) is identified as a potent, selective,
and rapidly reversible inhibitor of the 20S-proteasome (no yields given). —
(PURANDARE*, A. V.; WAN, H.; LAING, N.; BENBATOUL, K.; VACCARO, W.;
POSS, M. A.; Bioorg. Med. Chem. Lett. 14 (2004) 18, 4701-4704; Bristol-Myers
Squibb Pharm. Res. Inst., Princeton, NJ 08543, USA; Eng.) — H. Hoennerscheid
Документ
Категория
Без категории
Просмотров
0
Размер файла
28 Кб
Теги
1/--страниц
Пожаловаться на содержимое документа