Core exploration in optimization of chemokine receptor CCR4 antagonists

Authors :: Purandare, Ashok V.
Wan, Honghe
Somerville, John E.
Burke, Christine
Vaccaro, Wayne
Yang, XiaoXia
McIntyre, Kim W.
Poss, Michael A.
Source :: Bioorganic & Medicinal Chemistry Letters. Feb2007, Vol. 17 Issue 3, p679-682. 4p.
Publication Year :: 2007
Abstract: Abstract: The design, synthesis, and SAR studies of ‘core’ variations led to identification of novel, selective, and potent small molecule antagonist (22) of the CC chemokine receptor-4 (CCR4) with improved in vitro activity and liability profile. Compound 22 was efficacious in a murine allergic inflammation model (ED50 ∼10mg/kg). [Copyright &y& Elsevier]