Abstract: In the present paper a total of 20 derivatives of substituted piperidyl glycolate as anticholinergic agent were synthesized. preliminary pharmacological results showed that some of them possessed potent anticholinergic activity inmice both in central and peripheral nervous systems. Compouod Ⅲ was found to be the most potent anticholinergic agent in this series. Its central anticholinergic ED₅₀ value was 0.173mg/kg (in mice). It was somewhat more potent than or equal to the famous anticholinergic agent QNB.