close

Вход

Забыли?

вход по аккаунту

?

код для вставки
2004
Ring closure reactions
O 0130
Synthesis and Evaluation of Substrate-Mimicking Cytosolic Phospholipase A2 In— Reducing the Lipophilicity of the Arachidonyl Chain Isostere. — The
45- 039 hibitors
long alkyl chain of recently described potent cPLA2 inhibitors, mimicking the arachidonyl group of the natural substrate and responsible for the high lipophilicity of these
compounds, is modified to obtain more "drug-like" inhibitors. The modified alkyl chain
is attached first to a suitably functionalized phenol like (I) or (VI) by alkylation or condensation with electrophiles or nucleophiles. Reaction products (III) and (VIII) are subsequently combined with epoxide (IV) to give the inhibitors (V) and (IX), respectively,
after oxidation and ester hydrolysis. Oxadiazoles (V) display pleasing activities in the
monomeric assay while phthalimide derivative (IX) shows improved whole cell potencies against cPLA2 together with lower c log P's. — (WALTERS* IAIN; et al.;
Bioorg. Med. Chem. Lett. 14 (2004) 14, 3645-3649; Dep. Med. Chem., Astra
Charnwood, Loughborough, Leicestershire LE11 5RH, UK; Eng.) —
H. Hoennerscheid
Документ
Категория
Без категории
Просмотров
0
Размер файла
23 Кб
Теги
1/--страниц
Пожаловаться на содержимое документа