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DOI 10.1016/j.bmc.2013.08.025

Медицинская библиотека · Bioorganic & medicinal chemistry · 2013

Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases.

Sandham David A, Arnold Nicola, Aschauer Heinrich, Bala Kamlesh, Barker Lucy, Brown Lyndon, Brown Zarin, Budd David, Cox Brian, Docx Cerys, Dubois Gerald, Duggan Nicholas, England Karen, Everatt Brian, Furegati Marcus, Hall Edward, Kalthoff Frank, King Anna, Leblanc Catherine J, Manini Jodie, Meingassner Josef, Profit Rachael, Schmidt Alfred, Simmons Jennifer, Sohal Bindi, Stringer Rowan, Thomas Matthew, Turner Katharine L, Walker Christoph, Watson Simon J, Westwick John, Willis Jennifer, Williams Gareth, Wilson Caroline

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Аннотация

Optimization of a 7-azaindole-3-acetic acid CRTh2 receptor antagonist chemotype derived from high throughput screening furnished a highly selective compound NVP-QAV680 with low nM functional potency for inhibition of CRTh2 driven human eosinophil and Th2 lymphocyte activation in vitro. The molecule exhibited good oral bioavailability in the rat, combined with efficacy in rodent CRTh2-dependent mechanistic and allergic disease models and was suitable for clinical development.

Для цитирования: Sandham David A, Arnold Nicola, Aschauer Heinrich, Bala Kamlesh, Barker Lucy, Brown Lyndon, Brown Zarin, Budd David, Cox Brian, Docx Cerys, Dubois Gerald, Duggan Nicholas, England Karen, Everatt Brian, Furegati Marcus, Hall Edward, Kalthoff Frank, King Anna, Leblanc Catherine J, Manini Jodie, Meingassner Josef, Profit Rachael, Schmidt Alfred, Simmons Jennifer, Sohal Bindi, Stringer Rowan, Thomas Matthew, Turner Katharine L, Walker Christoph, Watson Simon J, Westwick John, Willis Jennifer, Williams Gareth, Wilson Caroline. Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases.. Bioorganic & medicinal chemistry. 2013. DOI: 10.1016/j.bmc.2013.08.025.

Предметные рубрики MeSH

Administration, OralAnimalsCHO CellsCricetinaeCricetulusDermatitis, ContactDisease Models, AnimalDrug Evaluation, PreclinicalEosinophilsHalf-LifeHumansHypersensitivityIndolizinesMiceMice, Inbred BALB CProtein BindingRatsRats, Sprague-DawleyReceptors, ImmunologicReceptors, ProstaglandinStructure-Activity RelationshipTh2 Cells
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