作为高选择性强效犬类COX-2抑制剂的杂芳基-苯基取代吡唑衍生物的合成及构效关系研究
Synthesis and SAR of heteroaryl-phenyl-substituted pyrazole derivatives as highly selective and potent canine COX-2 inhibitors.
作者信息
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
机构信息
Veterinary Medicine Research and Development Pfizer Inc., Groton, CT 06340, USA.
出版信息
Bioorg Med Chem Lett. 2006 Apr 15;16(8):2076-80. doi: 10.1016/j.bmcl.2006.01.059. Epub 2006 Feb 7.
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 IC50 of 12 nM and selectivity ratio of COX-1/COX-2 greater than 4000-fold.
本文描述了杂芳基-苯基取代的吡唑衍生物作为犬类选择性COX-2抑制剂的发现。对这类化合物的构效关系（SAR）研究导致鉴定出化合物1，其对犬全血COX-2的抑制IC50为12 nM，COX-1/COX-2的选择性比大于4000倍。
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