Author
Diego Benítez
Bio: Diego Benítez is an academic researcher from University of the Republic. The author has contributed to research in topics: Trypanosoma cruzi & Cruzipain. The author has an hindex of 13, co-authored 18 publications receiving 480 citations.
Topics: Trypanosoma cruzi, Cruzipain, Nifurtimox, Leishmania, Chagas disease
Papers
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TL;DR: Results demonstrated that the coordination of risedronate to different metal ions improved the antiproliferative effect against T. cruzi, exhibiting growth inhibition values against the intracellular amastigotes ranging the low micromolar levels.
55 citations
TL;DR: Derivatives possessing electron-withdrawing substituents in the 2, 3, 6, and 7-positions were the most active compounds and it was demonstrated that mitochondrial dehydrogenases are involved in the anti-T.
Abstract: For a fourth approach of quinoxaline N,N'-dioxides as anti-trypanosomatid agents against T. cruzi and Leishmania, we found extremely active derivatives. The present study allows us to state the correct requirements for obtaining optimal in vitro anti-T. cruzi activity. Derivatives possessing electron-withdrawing substituents in the 2-, 3-, 6-, and 7-positions were the most active compounds. With regard to these features and taking into account their mammal cytotoxicity, some trifluoromethylquinoxaline N,N'-dioxides have been proposed as candidates for further clinical studies. Consequently, mutagenicity and in vivo analyses were performed with the most promising derivatives. In addition, with regard to the mechanism of action studies, it was demonstrated that mitochondrial dehydrogenases are involved in the anti-T. cruzi activity of the most active derivatives.
51 citations
TL;DR: A series of thiosemicarbazones derived from 1-indanones with good anti-Trypanosoma cruzi activity are synthesized, and all the compounds showed nonspecific cytotoxicity on human erythrocytes.
45 citations
TL;DR: This work identifies new 5-nitrofuranes and the thia-analogues with excellent effects on the viability of T. cruzi and adequate parasite/mammal selectivity indexes and opens potential therapeutic possibilities of them for these infectious diseases.
45 citations
TL;DR: Forty new quinoxaline 1,4-di-N-oxide derivatives have been prepared and tested against M. tuberculosis and T. cruzi, showing great activities against TB and Chagas.
Abstract: Neglected diseases represent a major health problem. It is estimated that one third of the world population is infected with tuberculosis (TB). Besides TB, Chagas disease, affects approximately 20 million people. Quinoxalines display great activities against TB and Chagas. Forty new quinoxaline 1,4-di-N-oxide derivatives have been prepared and tested against M. tuberculosis and T. cruzi. Carboxylic acid quinoxaline 1,4-di-N-oxides (CAQDOs) 5 and 17 showed MIC values on the same order as the reference antituberculosis drug, rifampicin. Meanwhile, CAQDOs 12 and 22 presented IC50 values in the same order as the anti-chagasic drug, nifurtimox.
45 citations
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TL;DR: This work reviews the medicinal applications proposed for vanadium compounds with particular emphasis on the more recent publications and concludes that the potential ofVanadium compounds to treat type 2 diabetes is still an open question and therapies using vanadium compound for e.g. antitumor and anti-parasitic related diseases remain promising.
373 citations
TL;DR: For a review of the state-of-the-art in mechanochemistry, see, e.g., this article, the review presented in this paper. But, there still remains some mystique guarding the "rules" of mechanochemistry.
300 citations
TL;DR: This review describes the arsenal available for treating Leishmania infections, as well as recent advances from research on plants and synthetic compounds as source drugs for treating the disease, and highlights some biopharmaceutical technologies in the design of the delivery strategy.
289 citations
TL;DR: NMR and EPR Spectroscopy papers presented at Varian's Third Annual Workshop on Nuclear Magnetic Resonance and Electron Paramagnetic Resonance, held at Palo Alto, California as mentioned in this paper.
Abstract: NMR and EPR Spectroscopy Papers presented at Varian's Third Annual Workshop on Nuclear Magnetic Resonance and Electron Paramagnetic Resonance, held at Palo Alto, California. By the NMR–EPR Staff of Varian Associates. Pp. viii + 288. (London and New York: Pergamon Press, 1960.) 80s. net.
250 citations
TL;DR: This review aims at highlighting the diverse biological activities of hydrazones, an important class of compounds for new drug development.
Abstract: The development of novel compounds, hydrazones has shown that they possess a wide variety of biological activities viz. antimicrobial, anticonvulsant, antidepressant, anti-inflammatory, analgesic, antiplatelet, antimalarial, anticancer, antifungal, antitubercular, antiviral, cardio protective etc., Hydrazones/azomethines/imines possess-NHN = CH- and constitute an important class of compounds for new drug development. A number of researchers have synthesized and evaluated the biological activities of hydrazones. This review aims at highlighting the diverse biological activities of hydrazones.
248 citations