Bioorganic & Medicinal Chemistry 2008-06-01

Benzanilides with spasmolytic activity: chemistry, pharmacology, and SAR.

Gerda Brunhofer, Norbert Handler, Klaus Leisser, Christian R Studenik, Thomas Erker

Index: Bioorg. Med. Chem. 16 , 5974-81, (2008)

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Abstract

The following study describes the synthesis of new benzanilide derivatives and their pharmacological investigation on smooth muscle preparations of guinea pigs. All compounds were synthesized in good yields and showed a spasmolytic activity without significant effect on vascular smooth muscles and heart muscle preparations. Moreover, further pharmacological investigations as well as in silico studies were performed to elucidate the mechanism of action. Compound 3 showed the most potent spasmolytic activity with an IC(50) of 3.25microM.