Abstract:
:Structure-activity relationship (SAR) studies of novel 5-alkyl and 5-aryl/heteroaryl substituted 1,2,4-triazoles are described. The in vitro activity is compared to the pyrazole class of compounds with analogous side chains to delineate the contribution of the triazole ring nitrogen in binding to the active site. Both series are quite potent and selective in the canine whole blood (CWB) COX-2 assay, suggesting the increased binding contribution of the hydrophobic side chains.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Sakya SM,Shavnya A,Cheng H,Li C,Rast B,Li J,Koss DA,Jaynes BH,Mann DW,Petras CF,Seibel SB,Haven ML,Lynch MPdoi
10.1016/j.bmcl.2007.12.025subject
Has Abstractpub_date
2008-02-01 00:00:00pages
1042-5issue
3eissn
0960-894Xissn
1464-3405pii
S0960-894X(07)01471-0journal_volume
18pub_type
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