Type of Document Master's Thesis Author Shareef, Abdur-Rafay Author's Email Address Raf3232@hotmail.com URN etd-12052005-150536 Title Synthesis Of Potential Anti-Leishmania Dicationic Diaryldiamidines Degree Master of Science Department Chemistry Advisory Committee
Advisor Name Title David Boykin Committee Chair Alfons Baumstark Committee Member David Wilson Committee Member Keywords
- Dications
- Diamidines
- Trichomoniasis
- Leishmania
- Thiophene
- Anti-Microbials
- Efficacy
- Pharmacodynamic
Date of Defense 2005-11-29 Availability restricted Abstract Dicationic diamidines synthesized in the Boykin group a have shownbroad range of activity against a wide variety of microbial pathogens such as
Cryptosporidium parvum, Leishmania donovani, Plasmodium falciparum,
Trypanosoma burcei, and Trichomonas vaginalis. Thiophene based dicationic
diamidines have been especially impressive versus Trichomoniasis, and several
species of the leishmania parasite. The best compound in vitro against leishmania
was 2,5-bis-(4-amidophenyl)thiophene [DB 351].
In an attempt to improve upon antileishmanial activity, several analogs of
DB 351 have been synthesized. Previously the central heterocyclic ring has been
changed (furan, pyrrole, etc.), and the phenyl has been substituted with a pyridine
ring, however, in the thiophene series, the 3 and 4 position of the central
thiophene ring has remained unmodified. By modifying the 3 and 4 position of
the thiophene ring, and taking advantage of the substituent effect, the
pharmacodynamic and distribution properties of DB 351 will altered; hopefully
leading to more potent antileishmanial compounds.
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