Accession Number : ADB105446

Title :   Synthesis of Potential Trypanocides.

Descriptive Note : Annual rept. 1 Jul 83-30 Sep 84,

Corporate Author : VIRGINIA UNIV CHARLOTTESVILLE

Personal Author(s) : Sundberg, Richard J.

Report Date : NOV 1984

Pagination or Media Count : 125

Abstract : This project continued work to develop compounds with trypanocidal activity. The early phases of the work identified 1-alkyl-2-arylimidazo1,2-Apyridinium cations as active substances. Subsequent work has identified related ring systems, e.g., 1-alkyl-2-arylimidazo2,1-Bthiazolium, which also possess activity. Principal emphasis has been placed on substituent variation in the imidazo-1,2-Apyridine ring and at the 4'-position on the phenyl ring. Minimal structural requirements for activity include quaternization of the imidazo1,2-Apyridine nitrogen and a polar, preferably strongly basic, substituent at position-4'. During the present contract period ninety-two new compounds were prepared and submitted for evaluation. Principal compound types which were prepared included ring-substituted guanylhydrazones, N-substituted guanylhydrazones, heterocyclic hydrazones and dimeric compounds in which two imidazo1,2-Apyridinium units are linked by a difunctional hydrazide or hydrazine. New biological data received during the contract period indicate an enhanced level of activity in n,N-dialkylated guanylhydrazones.

Descriptors :   *SYNTHESIS(CHEMISTRY), *TRYPANOCIDES, HETEROCYCLIC COMPOUNDS, HYDRAZONES, RINGS, HYDRAZINES, PHENOLS, REQUIREMENTS, MOLECULAR STRUCTURE, PYRIDINES, IMIDAZOLES, CATIONS, DIMERS.

Subject Categories : Pharmacology
      Polymer Chemistry

Distribution Statement : APPROVED FOR PUBLIC RELEASE