Bioorganic & Medicinal Chemistry Letters 2000-09-04

Synthesis and biological effects of a new series of 2-amino-3-benzoylthiophenes as allosteric enhancers of A1-adenosine receptor.

P G Baraldi, A N Zaid, I Lampronti, F Fruttarolo, M G Pavani, M A Tabrizi, J C Shryock, E Leung, R Romagnoli

Index: Bioorg. Med. Chem. Lett. 10(17) , 1953-7, (2000)

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Abstract

New derivatives of PD 81,723, an allosteric enhancer of agonist binding to the A1-adenosine receptor, have been synthesized and evaluated in an intact cell assay. Compounds 3a, 3o and 3p appeared to be more potent than PD 81,723 and at a concentration of 0.1 microM caused significant reductions of cAMP content of CHO cells expressing the human A1-adenosine receptor. Compounds 4e and 4o appeared to be allosteric enhancers at a low concentration and antagonists at a higher concentration, whereas compounds 3c, 3g, 3s and 4l appeared to be weak antagonists that are also allosteric enhancers at the higher concentration of 10 microM.