Synthesis of bicyclic 1,4-thiazepines as novel anti-<i>Trypanosoma brucei brucei</i> agents

Vairoletti, Franco; Medeiros, Andrea; Fontán, Pablo; Meléndrez, Jennifer; Tabarez, Carlos; Salinas, Gustavo; Franco, J.; Comini, Marcelo A.; Saldaña, Jenny; Jancik, Vojtech; Mahler, Graciela; Saiz, Cecilia

doi:10.1039/c9md00064j

Cited by 4 publications

(1 citation statement)

References 33 publications

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“…The novel compounds were tested for anthelmintic action against Nippostrongylus brasiliensis , Caenorhabditis elegans , and T. brucei brucei . When compared to the positive control (nifurtimox, IC 50 15.0 μM), two compounds ( 30 and 31) were found to be phenomenally effective, with IC 50 values of 2.5 μM and 2.8 μM against T. b. brucei (Vairoletti et al., 2019). Synthesis of some anti‐ T. cruzi agents of 5,7‐diaryl‐2,3‐dihydro‐1,4‐diazepines has been reported by Menezes et al.…”

Section: Synthetic Antichagas Agentsmentioning

confidence: 99%

A comprehensive review on potential candidates for the treatment of chagas disease

et al. 2023

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Twenty different infectious disorders induced by bacteria, viruses, and parasites are categorized as neglected tropical diseases (NTDs) by WHO. The severity of chagas disease remains a major concern in endemic areas and an emerging public health hazard in nonendemic countries. Trypanosoma cruzi, the etiological agent of this NTD, is mostly transmitted by triatomine vectors and comprises a range of epidemiologically significant variants. Current chemotherapeutics are obsolete, and one of the primary reasons for treatment cessation is their poor safety and effectiveness. Due to the aforementioned challenges, researchers are now focusing on discovering alternative novel safe, and economically reachable therapies for the treatment of trypanosomiasis. Certain target‐based drugs that target specific biochemical processes of the causative parasites have been described as potential antichagasic agents that possesses various types of heterocyclic scaffolds. These flexible molecules have a wide range of biological actions, and various synthesized compounds with strong activity have been documented. This review aims to discuss the available literature on synthetic anti‐T. cruzi drugs that will give a food for thought to medicinal chemists thriving to design and develop such drugs. Furthermore, some of the studies discussed herein are concerned with the potential of novel drugs to block new viable sites in T. cruzi.

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Section: Synthetic Antichagas Agentsmentioning

confidence: 99%