Discovery of novel quinolinone adenosine A2B antagonists

Autor:	W. Lynn Rogers, Brian F. Mcguinness, Kurt W. Saionz, Steven G. Kultgen, Vikash Srivastava, Hema Desai, Hao Yan, Tara M. Stauffer, Samiran Saha, Koc-Kan Ho, Shengting Zhang, Neelima Mannava, Yan Jiang, Anthony E. Klon, Tailong Li, Juxing Yin, Weiqing Chen, Konghua Jing, Maria L. Webb, Kanak Kanti Majumdar, Laura L. Rokosz
Rok vydání:	2010
Předmět:	High-throughput screening Clinical Biochemistry Drug Evaluation Preclinical Pharmaceutical Science Quinolones Receptor Adenosine A2B Biochemistry Chemical synthesis Structure-Activity Relationship Drug Discovery medicine Combinatorial Chemistry Techniques Humans Molecular Biology Chemistry Adenosine A2B Receptor Antagonists Organic Chemistry Antagonist Metabolic stability Adenosine In vitro Adenosine A2 Receptor Antagonists Microsomes Liver Molecular Medicine medicine.drug
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 20:7414-7420
ISSN:	0960-894X
Popis:	A novel series of quinolinone-based adenosine A2B receptor antagonists was identified via high throughput screening of an encoded combinatorial compound collection. Synthesis and assay of a series of analogs highlighted essential structural features of the initial hit. Optimization resulted in an A2B antagonist (2i) which exhibited potent activity in a cAMP accumulation assay (5.1 nM) and an IL-8 release assay (0.4 nM).
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3954d9929bb24932679a9f1fdf525fd0 https://doi.org/10.1016/j.bmcl.2010.10.030 Zobrazit plný text záznamu Full Text from ScienceDirect