Author/Authors :
Zhihua Sui، نويسنده , , Jihua Guan، نويسنده , , Michael P. Ferro، نويسنده , , Kathy McCoy، نويسنده , , Michael P. Wachter، نويسنده , , William V. Murray، نويسنده , , Monica Singer، نويسنده , , Michele Steber، نويسنده , , Dave M. Ritchie، نويسنده , , Dennis C. Argentieri، نويسنده ,
Abstract :
Novel 1,3-diarylcycloalkanopyrazoles Scheme 1 and Scheme 2, and diphenyl hydrazides Scheme 1 and Scheme 2 were identified as selective inhibitors of cyclooxygenase-2. The 1,3-diaryl substitution pattern of the pyrazole ring in Scheme 1 and Scheme 2 differentiates these compounds from most of the known selective COX-2 inhibitors that contain two aryl rings at the adjacent positions on a heterocyclic or a phenyl ring. Similarly, the two phenyl rings in Scheme 1 and Scheme 2 are also separated by three atoms. SAR of both phenyl rings in Scheme 1 and Scheme 2, and the aliphatic ring in Scheme 1 and Scheme 2 will be discussed.
Scheme 1.
Scheme 2.