722550-78-9Relevant articles and documents
4-Substituted-7-N-alkyl-N-acetyl 2-aminobenzothiazole amides: Drug-like and non-xanthine based A2B adenosine receptor antagonists
Cheung, Adrian Wai-Hing,Brinkman, John,Firooznia, Fariborz,Flohr, Alexander,Grimsby, Joseph,Gubler, Mary Lou,Guertin, Kevin,Hamid, Rachid,Marcopulos, Nicholas,Norcross, Roger D.,Qi, Lida,Ramsey, Gwendolyn,Tan, Jenny,Wen, Yang,Sarabu, Ramakanth
scheme or table, p. 4140 - 4146 (2010/08/20)
7-N-Acetamide-4-methoxy-2-aminobenzothiazole 4-fluorobenzamide (compound 1) was chosen as a drug-like and non-xanthine based starting point for the discovery of A2B receptor antagonists because of its slight selectivity against A1 and A2A receptors and modest A2B potency. SAR exploration of compound 1 described herein included modifications to the 7-N-acetamide group, substitution of the 4-methoxy group by halogens as well as replacement of the p-flouro-benzamide side chain. This work culminated in the identification of compound 37 with excellent A2B potency, modest selectivity versus A2A and A1 receptors, and good rodent PK properties.
