191331-97-2Relevant academic research and scientific papers
Further insights of selenium-containing analogues of WC-9 against Trypanosoma cruzi
Chao, María N.,Lorenzo-Ocampo, María V.,Szajnman, Sergio H.,Docampo, Roberto,Rodriguez, Juan B.
, p. 1350 - 1361 (2019)
As a continuation of our project aimed at searching for new chemotherapeutic agents against American trypanosomiasis (Chagas disease), new selenocyanate derivatives were designed, synthesized and biologically evaluated against the clinically more relevant dividing form of Trypanosoma cruzi, the etiologic agent of this illness. In addition, in order to establish the role of each part of the selenocyanate moiety, different derivatives, in which the selenium atom or the cyano group were absent, were conceived, synthesized and biologically evaluated. In addition, in order to study the optimal position of the terminal phenoxy group, new regioisomers of WC-9 were synthesized and evaluated against T. cruzi. Finally, the resolution of a racemic mixture of a very potent conformationally rigid analogue of WC-9 was accomplished and further tested as growth inhibitors of T. cruzi proliferation. The results provide further insight into the role of the selenocyanate group in its antiparasitic activity.
Design, synthesis, and biological evaluation of new growth inhibitors of Trypanosoma cruzi (epimastigotes)
Schvartzapel, Andrea J.,Zhong, Li,Docampo, Roberto,Rodriguez, Juan B.,Gros, Eduardo G.
, p. 2314 - 2322 (2007/10/03)
As a continuation of our project aimed at the search for new chemotherapeutic agents against Chagas' disease, several drugs structurally related to the insect growth regulator Fenoxycarb and the naturally occurring juvenfie hormone of insects were designed, synthesized, and evaluated as antiproliferative agents against the parasite responsible of this disease. Isoprenoid derivatives (compounds 33, 34, 36, and 37) were potent growth inhibitors of Trypanosoma cruzi epimastigotes. In addition, taking into account the high activity observed for compound 30 and the inhibitory action of related compounds, the allyl ether moiety bonded at the polar extreme of these inhibitors proved to be a promising group for the design of new drugs.
