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Objectives In this work analgesic activity of more than 80 derivatives of cage-like amines is investigated. Carbox-, sulfon- and phosphonamides, ureas, sulfonylureas and aminoalcohols. They were got on the basis of stereochemically homogeneous amines (exo- and endo-2-aminomethylbicyclo[2.2.1]hept-5-enes and their saturated analogues, exo-5-aminomethyl-exo-2,3- epoxybicyclo[2.2.1]heptanes, and also sulfolan, deitiforin and amines of adamantane family by comparison to base amines are plugged into the investigated group. Download : Download full-size image [Figure] Rigid molecules with «fixed» in space substituents used as models for the study of structure-activity relationship of analgesic activity compounds with their chemical structure. Methods The investigation of compounds has been carried out on white mise. The acute toxicity (LD50) and analgesic activity («hot plate» method, 55°C) were determined. Explored compounds were entered in a dose equal 1/10 LD50 for 30 minutes prior to testing. Activity of preparations was estimated in % in relation to the control group of animals. Results Dependence of analgesic activity on the orientation of substituents in norbornene frame is marked: higher activity for endo-stereoisomers than for exo-form. Analgesic action decreases with disappearance of double bond and increase of number of cycles in carbon frame. The deitiforin derivatives are considerably more active than adamantane analogues. Conclusions More than 15 patents of Ukraine are got. |
