Chemistry and Chemical Biology ETDs

Publication Date

6-15-1971

Abstract

The need for new antimicrobial and antifungal agents as well as medicinals possessing antiprotozoal activity against special strains of malaria resistant to most synthetic antimalarials prompted the synthesis of new compounds that may have the desired antimetabolite properties. The structural similarities of the 1,2,5-thiadiazolo[3,4-d] pyridazines and the v-triazolo[4,5-d]pyridazines with the biologically important purines prompted the synthesis of members of these ring systems. The 1,2,5-thiadiazoles synthesized as intermediates ware also screened as potential chemotherapeutic agents. Similarly, the pyridazine N-oxides and the 5-nitro substituted pyrimidines are structurally similar to the pyrazine N-oxides and the pyridine N-oxides, which are known to possess a broad spectrum inhibition against bacteria and fungi in a very low concentration.77,112 A series of 4,7-disubstituted and 4-monosubstituted 1,2,5-thiadiazolo [3,4-d]pyridazines, 4-substituted 7-methyl-v-triazolo[4,5-d] pyridazines, some 6-aminopyridazine 1-oxides substituted in the 3 position and several 5-nitropyrimidines substituted in the 4,6 positions were prepared. Ultra­violet and infrared spectra were reported for all compounds, while nuclear magnetic resonance spectra were measured only for certain select compounds. A number of these compounds were screened for their inhibitory action against several bacterial and fungal species.

Document Type

Dissertation

Degree Name

Chemistry

Level of Degree

Doctoral

Department Name

Department of Chemistry and Chemical Biology

First Committee Member (Chair)

Raymond N. Castle

Second Committee Member

Terence Joseph Scallen

Third Committee Member

Roy Dudley Caton Jr

Fourth Committee Member

Milton Kahn

Fifth Committee Member

Eleftherios Paul Papadopoulos

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