145902-49-4Relevant academic research and scientific papers
Rapid discovery and structure-activity profiling of novel inhibitors of human immunodeficiency virus type 1 protease enabled by the copper(I)-catalyzed synthesis of 1,2,3-triazoles and their further functionalization
Whiting, Matthew,Tripp, Jonathan C.,Lin, Ying-Chuan,Lindstrom, William,Olson, Arthur J.,Elder, John H.,Sharpless, K. Barry,Fokin, Valery V.
, p. 7697 - 7710 (2007/10/03)
Building from the results of a computational screen of a range of triazole-containing compounds for binding efficiency to human immunodeficiency virus type 1 protease (HIV-1-Pr), a novel series of potent inhibitors has been developed. The copper(I)-cataly
TIGHT-BINDING INHIBITORS OF LEUKOTRIENE A4 HYDROLASE
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, (2008/06/13)
Inhibitors of leukotriene A 4 hydrolase are disclosed, corresponding to Formula I, below: STR1 wherein the depicted--NH 2 group is in the (S) configuration;--W is--CH 2 SH,--CH 2 NH. sub.2 or C(=Z)--Y, wherein =Z is =O, or--H and--OH; and--Y is selected from the group consisting of (a) phenyl, (b) trifluoromethylphenyl, (c) carboxyphenyl, (d) benzyl, (e) C 1-C 6 alkylenecarboxyl, (f) C. sub.1-C 6 alkyl, (g) C 2-C 6 alkenyl, (h) C 1-C 6 alkylenephenyl and (i)--C(=O)--X--R. sup.1 wherein X is O or NH and, R 1 is selected from the group consisting of C 1-C 6 alkyl, C 1-C 6 alkylenecarboxyl, and benzyl; R 2 is hydrogen, benzyloxy or 2-naphthylmethyloxy, and a pharmaceutically acceptable acid addition salt thereof. Inhibitors wherein--W is--CH 2 SH,--CH 2 NH 2 or C(=Z)--Y wherein =Z is =O and--Y is--C(=O)--X--R. sup.1 are particularly preferred, as are those compounds wherein =Z is = O and--Y is selected from the group consisting of (a) phenyl, (b) trifluoromethylphenyl, (c) carboxyphenyl, (d) benzyl, (e) C 1-C 6 alkylenecarboxyl, (f) C 1-C 6 alkyl, (g) C 2-C 6 alkenyl, (h) C 1-C 6 alkylenephenyl. An inhibitor where--W is--CH 2 SH,--CH 2 NH 2 or C(=Z)--Y wherein =Z is =O and--Y is--C(=O)--X--R 1 is particularly preferred, as are those inhibitor compounds where =Z is =O and--Y is (a)--(h) .
Development of selective tight-binding inhibitors of leukotriene A4 hydrolase
Yuan,Munoz,Wong,Haeggstrom,Wetterholm,Samuelsson
, p. 211 - 220 (2007/10/02)
Leukotriene A4 hydrolase is a zinc-containing enzyme which exhibits both epoxide hydrolase and aminopeptidase activities. Since the enzyme product leukotriene B4 is an inflammatory mediator, it is of interest to develop selective inh
