4-Substituted-7-N-alkyl-N-acetyl 2-aminobenzothiazole amides: drug-like and non-xanthine based A2B adenosine receptor antagonists.

@article{Cheung20104Substituted7NalkylNacetyl2A,
  title={4-Substituted-7-N-alkyl-N-acetyl 2-aminobenzothiazole amides: drug-like and non-xanthine based A2B adenosine receptor antagonists.},
  author={Adrian Wai-Hing Cheung and John Brinkman and Fariborz Firooznia and Alexander Flohr and Joseph S. Grimsby and Mary Lou Gubler and Kevin R Guertin and Rachid Hamid and Nicholas Marcopulos and Roger D. Norcross and Lida Qi and Gwendolyn Ramsey and Jenny Tan and Yang Wen and Ramakanth Sarabu},
  journal={Bioorganic & medicinal chemistry letters},
  year={2010},
  volume={20 14},
  pages={4140-6}
}
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… CONTINUE READING