[3-Benzyl-1,2-benzoisothiazoles: spasmolytic properties of the aminoalkyl derivatives].
The synthesis and chemical and pharmacological properties of 3-benzyl-1,2-benzisothiazoleaminoalkyl derivatives are reported. These compounds were studied because 4-dimethyl-2-phenyl-2-(1,2-benzisotiazol-3-yl)-butyramide and N,N-dimethyl-3-phenyl-3-(1,2-benzisothiazol-3-yl)propylamine were recently found to have antispasmodic properties. Most of the compounds studied aspecifically inhibited the contracturant effects of acetylcholine, histamine and BaCl2. Three of them showed mixed antagonism (competitive and non-competitive) versus acetylcholine and histamine, showing both antimuscarinic and antihistaminic properties. However the antimuscarinic action prevailed over the others, as shown by pA2 and pD'2 calculated values. On the basis of the results obtained, the structure-activity relationships is discussed.
D000109:Acetylcholine / Q000494:pharmacology; D000818:Animals; D001464:Barium / Q000494:pharmacology; D017609:Barium Compounds; D055598:Chemical Phenomena; D002621:Chemistry; D002712:Chlorides; D006168:Guinea Pigs; D006632:Histamine / Q000494:pharmacology; D010276:Parasympatholytics / Q000138:chemical synthesis*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis*
D017609:Barium Compounds; D002712:Chlorides; D010276:Parasympatholytics; D013844:Thiazoles; C024986:barium chloride; D001464:Barium; D006632:Histamine; D000109:Acetylcholine
3-benzil-1,2-benzisotiazoli: proprietà spasmolitiche di aminoalchilderivati.