PHARMACOLOGICAL STUDIES OF 1-(P-CHLOROPHENYL)PROPANOL AND 2-(1-HYDROXY-3-BUTENYL)PHENOL - 2 NEW NONNARCOTIC ANALGESICS DESIGNED BY MOLECULAR CONNECTIVITY

Molecular topology has been applied to the design of new analgesic dru gs. Linear discriminant analysis and connectivity functions were used to design two potentially suitable drugs which were synthesized and te sted for analgesic properties by the acetic acid-induced abdominal con striction test in mice and the tail-flick test in rats. In mice, the c ompound 1-(p-chlorophenyl)propanol showed higher analgesic activity, b oth intraperitoneally and orally, than acetylsalicylic acid. 2-(1-Hydr oxy-3-butenyl)phenol exhibited a lesser protective effect (70% of that shown by acetylsalicylic acid). In rats, acetylsalicylic acid gave th e greatest protection against pain when administered intraperitoneally , while 1-(p-chlorophenyl)propanol was the most active orally. The 2-( 1-hydroxy-3-butenyl)phenol, both intraperitoneally and orally, showed the least protective effect. These results demonstrated the peripheral analgesic properties of the selected compounds, thus confirming the v alidity of the molecular design method.