4-Substituted-7-N-alkyl-N-acetyl 2-aminobenzothiazole amides: drug-like and non-xanthine based A2B adenosine receptor antagonists.
Bioorg Med Chem Lett
; 20(14): 4140-6, 2010 Jul 15.
Article
in En
| MEDLINE
| ID: mdl-20541935
ABSTRACT
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 A(2B) receptor antagonists because of its slight selectivity against A(1) and A(2A) receptors and modest A(2B) 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 A(2B) potency, modest selectivity versus A(2A) and A(1) receptors, and good rodent PK properties.
Full text:
1
Database:
MEDLINE
Main subject:
Xanthine
/
Receptor, Adenosine A2B
/
Benzothiazoles
/
Adenosine A2 Receptor Antagonists
Language:
En
Year:
2010
Type:
Article