Discovery and synthesis of cyclohexenyl derivatives as modulators of CC chemokine receptor 2 activity.

Brown, Gregory D; Shi, Qing; Delucca, George V; Batt, Douglas G; Galella, Michael A; Cvijic, Mary-Ellen; Liu, Rui-Qin; Qiu, Feng; Zhao, Qihong; Barrish, Joel C; Carter, Percy H

Brown, Gregory D; Shi, Qing; Delucca, George V; Batt, Douglas G; Galella, Michael A; Cvijic, Mary-Ellen; Liu, Rui-Qin; Qiu, Feng; Zhao, Qihong; Barrish, Joel C; Carter, Percy H.

Afiliación

Brown GD; Research and Development, Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, NJ 08543-4000, United States. Electronic address: gregory.brown@bms.com.
Shi Q; Research and Development, Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, NJ 08543-4000, United States.
Delucca GV; Research and Development, Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, NJ 08543-4000, United States.
Batt DG; Research and Development, Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, NJ 08543-4000, United States.
Galella MA; Research and Development, Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, NJ 08543-4000, United States.
Cvijic ME; Research and Development, Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, NJ 08543-4000, United States.
Liu RQ; Research and Development, Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, NJ 08543-4000, United States.
Qiu F; Research and Development, Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, NJ 08543-4000, United States.
Zhao Q; Research and Development, Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, NJ 08543-4000, United States.
Barrish JC; Research and Development, Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, NJ 08543-4000, United States.
Carter PH; Research and Development, Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, NJ 08543-4000, United States.

Bioorg Med Chem Lett ; 26(2): 662-666, 2016 Jan 15.

Article en En | MEDLINE | ID: mdl-26631321

RESUMEN

A novel cyclohexenyl series of CCR2 antagonists has been discovered. This series of small, rigid compounds exhibits submicromolar binding affinity for CCR2. Modification of the substituents on the cyclohexene ring led to the identification of potent CCR2 antagonists. Progress from initial lead 5 (IC50=700nM) to (-)-38 (IC50=9.0nM) is discussed.

Asunto(s)

Ciclohexenos/química; Ciclohexenos/farmacología; Receptores CCR2/antagonistas & inhibidores; Ciclohexenos/síntesis química; Descubrimiento de Drogas; Humanos; Modelos Moleculares; Receptores CCR2/metabolismo; Relación Estructura-Actividad

Palabras clave

CCR2; CCR2 antagonist; Chemokine; GPCR

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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Ciclohexenos / Receptores CCR2 Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2016 Tipo del documento: Article

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