Lian-Yong Chen

Trans diastereoselective synthesis of 3-alkyl substituted β-lactams via the acid chloride-imine reaction of nonactivated acid chlorides

Abstract New conditions for the acid chloride-imine reaction of nonactivated alkyl acid chlorides provide 3-alkyl substituted β-lactams in good yields with high trans selectivity.

Benzylidene ketal derivatives as M2 muscarinic receptor antagonists

Benzylidene ketal derivatives were investigated as selective M2 receptor antagonists for the treatment of Alzheimers disease. Compound 10 was discovered to have subnanomolar M2 receptor affinity and 100-fold selectivity against other muscarinic receptors. Also, 10 demonstrated in vivo efficacy in rodent models of muscarinic activity and cognition.

Diphenylsulfone muscarinic antagonists: piperidine derivatives with high m2 selectivity and improved potency

Piperidine analogues of our previously described piperazine muscarinic antagonists are described. Piperidine analogues show a distinct structure-activity relationship (SAR) that differs from comparable piperazines. Compounds with high selectivity and improved potency for the M2 receptor have been identified. The lead compound, 12b, increases acetylcholine release in vivo. Compounds of this class may be useful for the treatment of cognitive disorders such as Alzheimers disease (AD).