Authors: Costa, J.C.S.; Neves, J.S.; De Souza, M.V.N.; Siqueira, R.A.; Romeiro, N.C.; Boechat, N.; Silva, P.M.; Martins, M.A.
Source: Bioorganic & Medicinal Chemistry Letters, v. 18, p. 1162-1166, 2008.Publisher: Elsevier
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) acetamides were selected as the most promising compounds. New insights into the applicability of non-anesthetic lidocaine derivatives as templates in drug discovery for allergic syndromes are provided.Keywords:Lidocaine; Antispasmodic activity; Allergy; Anesthetic activityDocument Type: Research ArticleDOI: http://dx.doi.org/10.1016/j.bmcl.2007.11.122Publication date: 1 de Fevereiro de 2008
