Synthesis and antispasmodic activity of lidocaine derivatives endowed with reduced local anesthetic action

…, MVN de Souza, RA Siqueira, NC Romeiro…

Index: Costa, Jorge C.S.; Neves, Josiane S.; de Souza, Marcus V.N.; Siqueira, Rodrigo A.; Romeiro, Nelilma C.; Boechat, Nubia; Silva, Patricia M.R.e; Martins, Marco A. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 3 p. 1162 - 1166

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Citation Number: 13

Abstract

The present structure-activity relationship (SAR) study focused on chemical modifications of the structure of the local anesthetic lidocaine, and indicated analogues having reduced anesthetic potency, but with superior potency relative to the prototype in preventing anaphylactic or histamine-evoked ileum contraction. From the SAR analysis, 2- (diethylamino)-N-(trifluoromethyl-phenyl) and 2-(diethylamino)-N-(dimethyl-phenyl) ...