Bioisosteric modification of PETT-HIV-1 RT-inhibitors: synthesis and biological evaluation
摘要:
Bioisosteric substitution of the thiourea (3, 5, 7, 9) and urea (10) moiety of PETT compounds with sulfamide (1), cyanoguanidine (2, 4) and guanidine (6, 8) functionalities, and replacement of the phenethyl group with benzoylethyl group (compounds 11-20) have been studied. Synthesis and antiviral activities are described. (C) 2000 Elsevier Science Ltd. All rights reserved.
The present invention relates to pyrrolidine derivatives useful as inhibitors of metalloproteases, e.g. zinc proteases, and which are effective in treating disease states associated with vasoconstriction.
The present invention relates to compounds of formula (I)
1
wherein U, Y, V, W, L, X, A
1
, A
2
, A
3
, A
4
, A
5
and A
6
are as defined in the description and claims and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, parasite infections, gallstones, tumors and/or hyperproliferative disorders, and/or treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
The present invention relates to aminocyclohexanol derivatives useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
Synthesis and antiviral activity of new benzothiadiazine dioxide derivatives
作者:Annalisa Tait、Amedeo Luppi、Claudio Cermelli
DOI:10.1002/jhet.5570410516
日期:2004.9
A series of 2,1,3- and 1,2,4-benzothiadiazine derivatives were synthesized by alkylation via Mitsunobu reaction and evaluated for their antiviralactivity against ADV, HHV-6, Cox-B5 and H-CMV. Most of them were active at micromolar level against one or more viral strains. All the molecules studied are poorly cytotoxic (maximum non toxic concentrations were >25μM), except one compound that presents
[EN] PYRROLIDINE DERIVATIVES AS METALLOPROTEASE INHIBITORS<br/>[FR] DERIVES DE PYRROLIDINE UTILISES EN TANT QU'INHIBITEURS DE METALLOPROTEASE
申请人:HOFFMANN LA ROCHE
公开号:WO2002008185A1
公开(公告)日:2002-01-31
The present invention relates to compounds of formula (I) wherein R?1, R2, R3, R4, R5, R6¿, Y, n, m, o. p and q are as defined in the description and the claims and dimeric forms and/or pharmaceutically acceptable esters, and/or salts thereof. The compounds are useful as inhibitors of metalloproteases, e.g. zinc proteases, particularly zinc hydrolases, and which are effective in treating disease states are associated with vasoconstriction of increasing occurrences.