Accession Number : ADB109043
Title : Synthesis of Potential Trypanocides.
Descriptive Note : Final rept. Feb 78-Sep 84,
Corporate Author : VIRGINIA UNIV CHARLOTTESVILLE DEPT OF CHEMISTRY
Personal Author(s) : Sundberg, Richard J.
Report Date : FEB 1986
Pagination or Media Count : 189
Abstract : This report describes research conducted to identify new chemical compounds which could be evaluated as trypanocidal agents. An extensive series of quaternary heteroaromatic salts has been synthesized by chemical methods which are documented in the reports. Many of the compounds exhibit activity in in vivo screens against Trypanosome rhodesiense in mice. The most active compounds are derivatives of the imidazo pyridinium ring system, although several related ring systems exhibit substantial activity. The most potent compounds are guanylhydrazone and N-substituted guanylhydrazones. Several such compounds exceed previously known trypanocidal drugs in level of activity. Three compounds are designed as potential candidates for preclinical and toxicological investigation. Keywords: Trypanosomiasis.
Descriptors : *SYNTHESIS(CHEMISTRY), *TRYPANOCIDES, MICE, POTENCY, DRUGS, TRYPANOSOMIASIS, CHEMICAL COMPOUNDS, RINGS, TRYPANOSOMA, HYDRAZONES, SALTS, AROMATIC COMPOUNDS, PYRIDINES.
Subject Categories : Biochemistry
Medicine and Medical Research
Distribution Statement : APPROVED FOR PUBLIC RELEASE