Wood, JM, Satam, NS, Almeida, RG, Cristani, VS, de Lima, DP, Dantas-Pereira, L, Salomão, K, Menna-Barreto, RFS, Namboothiri, INN, Bower, JF ORCID: 0000-0002-7551-8221 et al (show 1 more authors)
(2020)
Strategies towards potent trypanocidal drugs: Application of Rh-catalyzed [2 + 2 + 2] cycloadditions, sulfonyl phthalide annulation and nitroalkene reactions for the synthesis of substituted quinones and their evaluation against Trypanosoma cruzi.
Bioorganic and Medicinal Chemistry, 28 (15).
115565-.
Text
2. Manuscript - Rishi John and Eufrânio - accepted.docx - Author Accepted Manuscript Download (928kB) |
Abstract
Rhodium-catalyzed [2 + 2 + 2] cycloadditions, sulfonyl phthalide annulations and nitroalkene reactions have been employed for the synthesis of 56 quinone-based compounds. These were evaluated against Trypanosoma cruzi, the parasite that causes Chagas disease. The reactions described here are part of a program that aims to utilize modern, versatile and efficient synthetic methods for the one or two step preparation of trypanocidal compounds. We have identified 9 compounds with potent activity against the parasite; 3 of these were 30-fold more potent than benznidazole (Bz), a drug used for the treatment of Chagas disease. This article provides a comprehensive outline of reactions involving over 120 compounds aimed at the discovery of new quinone-based frameworks with activity against T. cruzi.
Item Type: | Article |
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Uncontrolled Keywords: | Quinones, Chagas disease |
Depositing User: | Symplectic Admin |
Date Deposited: | 26 Jun 2020 08:10 |
Last Modified: | 18 Jan 2023 23:48 |
DOI: | 10.1016/j.bmc.2020.115565 |
Related URLs: | |
URI: | https://livrepository.liverpool.ac.uk/id/eprint/3091688 |