Details

Autor(en) / Beteiligte

• Cheng, Hengmiao
• Lundy DeMello, Kristin M.
• Li, Jin
• Sakya, Subas M.
• Ando, Kazuo
• Kawamura, K.
• Kato, Tomoki
• Rafka, Robert J.
• Jaynes, Burton H.
• Ziegler, Carl B.
• Stevens, Rod
• Lund, Lisa A.
• Mann, Donald W.
• Kilroy, Carolyn
• Haven, Michelle L.
• Nimz, Erik L.
• Dutra, Jason K.
• Li, Chao
• Minich, Martha L.
• Kolosko, Nicole L.
• Petras, Carol
• Silvia, Annette M.
• Seibel, Scott B.

Titel

Synthesis and SAR of heteroaryl-phenyl-substituted pyrazole derivatives as highly selective and potent canine COX-2 inhibitors

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2006-04, Vol.16 (8), p.2076-2080

Ort / Verlag

Oxford: Elsevier Ltd

Erscheinungsjahr

2006

Link zum Volltext

Quelle

MEDLINE

Beschreibungen/Notizen

• The discovery of heteroaryl-phenyl-substituted pyrazole derivatives as canine selective COX-2 inhibitors is described. Structure–activity relationship (SAR) studies of this class of compounds led to the identification of compound 1 which demonstrated a canine whole blood COX-2 inhibitory IC 50 of 12 nM and selectivity ratio of COX-1/COX-2 greater than 4000-fold. The discovery of heteroaryl-phenyl-substituted pyrazole derivatives as canine selective COX-2 inhibitors is described. Structure–activity relationship (SAR) studies of this class of compounds led to the identification of compound 1 which demonstrated a canine whole blood COX-2 inhibitory IC 50 of 12 nM and selectivity ratio of COX-1/COX-2 greater than 4000-fold.