Heterocyclic sulfones have been shown to have a high level of activity against human immunodeficiency virus type 1. In addition they have expressed a variety of other medicinal properties including activity against tuberculosis, pneumocystis carinii pneumonia, and as tranquilizers. Due to this wide spectrum of medicinal properties, a variety of heterocyclic sulfones were investigated for novel activity using an innovative computational approach. From these studies a new potential molecular target for heterocyclic sulfones, in particular quinoline sulfones, has been discovered: aldose reductase. Inhibitors of aldose reductase have been suggested for the treatment several of disease states including diabetic complications and heart disease. The quinoline sulfones that expressed significant computational activity were synthesized using modified halide displacement and sulfide oxidation reactions.
|Commitee:||Gupta, Pardeep, Neau, Steven, Schaefer, Fred, Zanger, Murray, Zauhar, Randy|
|School:||University of the Sciences in Philadelphia|
|School Location:||United States -- Pennsylvania|
|Source:||DAI-B 77/04(E), Dissertation Abstracts International|
|Keywords:||Aldose reductase, Quinoline, Shape signatures, Similarity ensemble approach, Sulfones|
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