Studies toward the structural optimization of novel thiazolylhydrazone-based potent antitrypanosomal agents

In previous studies, we identified promising anti-Trypanosoma cruzi cruzain inhibitors based on thiazolylhydrazones. To optimize this series, a number of medicinal chemistry directions were explored and new thiazolylhydrazones and thiosemicarbazones were thus synthesized. Potent cruzain inhibitors were identified, such as thiazolylhydrazones 3b and 3j, which exhibited IC(50) of 200-400 nM. Furthermore, molecular docking studies showed concordance with experimentally derived structure-activity relationships (SAR) data. In the course of this work, lead compounds exhibiting in vitro activity against both the epimastigote and trypomastigote forms of T. cruzi were identified and in vivo general toxicity analysis was subsequently performed. Novel SAR were documented, including the importance of the thiocarbonyl carbon attached to the thiazolyl ring and the direct comparison between thiosemicarbazones and thiazolylhydrazones. (C) 2010 Elsevier Ltd. All rights reserved.

Center for the Study of Free Reed Instruments Collection, 1947-2011 Finding Aid

The Center for the Study of Free-Reed Instruments Collection is an archival collection at the City University of New York Graduate Center’s Mina Rees Library which contains materials donated by Professor Allan W. Atlas, related to free-reed instruments and the International Concertina Association.

Politian: a critical analysis

Why even look at Politian, an unfinished failure? While it is true that Politian was a failure for its time and surely one of Poe's least successful attempts, it may improve on a stage with a more modern perspective. If not solely for examination of Poe's artistic effort, Politian also warrants a closer read due to its historical relevance by way of Beauchamp and Sharp. Poe, a most fastidious editor of his work, was ultimately required because of financial constraints to lay aside Politian in its unfinished state. As a result, the unedited Politian may provide insight into the writing process of Poe that other polished pieces cannot, and that, if nothing else, warrants a more precise study of his play.