title: Synthesis and antispasmodic activity of lidocaine derivatives endowed with reduced local anesthetic action.
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.
authors: Laboratório de Síntese Orgânica, Farmanguinhos, FIOCRUZ, Rio de Janeiro, Brazil.
authors: Jorge C S
authors: JC
authors: Costa
authors: Josiane S
authors: JS
authors: Neves
authors: Marcus V N
authors: MV
authors: de Souza
authors: Rodrigo A
authors: RA
authors: Siqueira
authors: Nelilma C
authors: NC
authors: Romeiro
authors: Nubia
authors: N
authors: Boechat
authors: Patrícia M R
authors: PM
authors: e Silva
authors: Marco A
authors: MA
authors: Martins
mesh_terms: D000779:Anesthetics, Local / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D020650:Combinatorial Chemistry Techniques; D004305:Dose-Response Relationship, Drug; D006632:Histamine / Q000494:pharmacology; D008012:Lidocaine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D010276:Parasympatholytics / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D000779:Anesthetics, Local; D010276:Parasympatholytics; D006632:Histamine; D008012:Lidocaine