Bioorganic and Medicinal Chemistry Letters p. 1991 - 1996 (1998)
Update date:2022-08-03
Topics:
Augelli-Szafran, Corinne E.
Jaen, Juan C.
Moreland, David W.
Nelson, Carrie B.
Penvose-Yi, Jan R.
Schwarz, Roy D.
Our interest in the area of m4 muscarinic antagonists has led us to study a series of benzoxazine isoquinolines. One of the most potent and selective compounds of this series is example 1 with an IC50 value of 90.7nM at m4 receptors, and 72-fold (m1), 38-fold (m2), 10-fold (m3), and 82- fold (m5) more selective compared to the other receptors. The synthesis and receptor binding affinity of analogs of 1 are reported.
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