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
      Pharmacology

Distribution Statement : APPROVED FOR PUBLIC RELEASE