ABSTRACT
In the reactions of 3-hydroxy-1,2-benzisoxazole (BIO) and its 5-Cl and 6-Cl derivatives with ethyl bromoacetate were obtained the mixtures of O- and N- substituted esters but 7-NO2-BIO formed only O-ester. The products of N-aminomethylation of 5-NO2-BIO were active against Trichomonas vaginalis. The structures of pure compounds have been confirmed by elementary analysis and IR spectrometry. Determinations of dissociation constants (pKa) of BIO, 5-Cl-BIO, 6-Cl-BIO, 7-Cl-BIO, 5-F-BIO, 5-NO2-BIO, 7-NO2-BIO by potentiometric titration method were described. Investigated compounds have two values of ionisation constants except the nitro derivatives, this is the confirmation of equilibrium 3-hydroxy-1,2-benzisoxazole <==> 1,2-benzisoxazolinone-3.
Subject(s)
Antiprotozoal Agents/chemistry , Isoxazoles/chemistry , Alkylation , Animals , Spectrometry, Fluorescence , Trichomonas vaginalis/drug effectsABSTRACT
New ester, acetamide and aminomethylacetamide derivatives of 3-benzoxazolin-2-one and its 5- and 6-chloro derivatives, 2-methyl-l-benzimidazole, and of 1- and 2-benzotriazole were obtained. Pharmacological screening has shown that amides VII, VIII, XI and XII exert slight deppressory effects on the central nervous system.
Subject(s)
Acetates/pharmacology , Benzimidazoles/pharmacology , Benzoxazoles/pharmacology , Motor Activity/drug effects , Triazoles/pharmacology , Acetates/chemical synthesis , Animals , Benzimidazoles/chemical synthesis , Benzoxazoles/chemical synthesis , Chemical Phenomena , Chemistry , Depression, Chemical , Drug Evaluation, Preclinical , Mice , Motor Activity/physiology , Triazoles/chemical synthesisSubject(s)
Isoxazoles/chemical synthesis , Oxazoles/chemical synthesis , Animals , Antinematodal Agents , Antitrichomonal Agents , Chemical Phenomena , Chemistry , Depression/chemically induced , Drug Evaluation, Preclinical , Humans , Isoxazoles/pharmacology , Mice , Morpholines/chemical synthesis , Morpholines/pharmacology , Nematoda/drug effects , Piperazines/chemical synthesis , Piperazines/pharmacology , Piperidines/chemical synthesis , Piperidines/pharmacology , Trichomonas vaginalis/drug effectsABSTRACT
Occurrence of ganglion on the wrist in the scaphoid region in connection with protuberance of the scaphoid bone is statistically of high significance. As ganglions result from mucoid degeneration of connective tissue following microtraumata, the scaphoid protuberance may cause ganglion to appear most frequently at a localization above the scaphoid bone on the wrist. We suggest that this localization be called 'loco typico'.
