1, 3, 4-Thiadiazole: synthesis, reactions, and applications in medicinal, agricultural, and materials chemistry

Y Hu, CY Li, XM Wang, YH Yang, HL Zhu - Chemical reviews, 2014 - ACS Publications
Over the past decades, the bulk of chemists' interests have been on heterocyclic compounds
and their various derivatives as well as their applications in the pharmaceutical and …

Trypanocidal activity of nitroaromatic prodrugs: current treatments and future perspectives

SR Wilkinson, C Bot, JM Kelly… - Current topics in …, 2011 - ingentaconnect.com
Chagas disease and African sleeping sickness are trypanosomal infections that represent
important public health problems in Latin America and Africa, respectively. The restriction of …

[HTML][HTML] Screening of potential anti-Trypanosoma cruzi candidates: in vitro and in vivo studies

CS Maria de Nazaré, SL de Castro - The Open Medicinal …, 2011 - ncbi.nlm.nih.gov
Chagas disease (CD), caused by the intracellular protozoan Trypanosoma cruzi, is a
parasitic illness endemic in Latin America. In the centennial after CD discovery by Carlos …

[HTML][HTML] Studies of genotoxicity and mutagenicity of nitroimidazoles: demystifying this critical relationship with the nitro group

N Boechat, AS Carvalho, K Salomão… - Memórias do Instituto …, 2015 - SciELO Brasil
Nitroimidazoles exhibit high microbicidal activity, but mutagenic, genotoxic and cytotoxic
properties have been attributed to the presence of the nitro group. However, we synthesised …

Stairway to heaven or hell? Perspectives and limitations of Chagas disease chemotherapy

K Salomao… - Current Topics in …, 2016 - ingentaconnect.com
In this review, we intend to provide a general view of the evolution of experimental studies in
the area of chemotherapy for Chagas disease. We can follow the process of drug …

In Vitro and In Vivo Activities of 1,3,4-Thiadiazole-2-Arylhydrazone Derivatives of Megazol against Trypanosoma cruzi

K Salomão, EM De Souza, SA Carvalho… - Antimicrobial agents …, 2010 - Am Soc Microbiol
ABSTRACT From a series of 1, 3, 4-thiadiazole-2-arylhydrazone derivatives of megazol
screened in vitro against Trypanosoma cruzi, eight (S1 to S8) were selected for in vivo …

Studies toward the structural optimization of new brazilizone-related trypanocidal 1, 3, 4-thiadiazole-2-arylhydrazone derivatives

SA Carvalho, FAS Lopes, K Salomão… - Bioorganic & medicinal …, 2008 - Elsevier
Megazol is a highly active compound against Trypanosoma cruzi, and has become a core
structure for the design of new trypanocidal agents. Recently, we have identified the new …

Preparation of 1,3,4-oxadiazoles and 1,3,4-thiadiazoles via chemoselective сyclocondensation of electrophilically activated nitroalkanes to (thio)semicarbazides or …

NA Aksenov, NA Arutiunov, NK Kirillov… - Chemistry of …, 2020 - Springer
Unusual reaction proceeding via the electrophilic activation of nitroalkanes in the presence
of polyphosphoric acid has been discovered. Subsequent nucleophilic attack with …

Synthesis and Trypanocidal Activity of Novel 2,4,5-Triaryl-N-Hydroxylimidazole Derivatives

RB Da Silva, VB Loback, K Salomão, SL De Castro… - Molecules, 2013 - mdpi.com
Herein, we report the design, synthesis and trypanocidal activity of some novel trisubstituted
imidazole derivatives. These heterocyclic derivatives were structurally planned by exploring …

Novel nitroimidazole derivatives evaluated for their trypanocidal, cytotoxic, and genotoxic activities

FVC e Mello, BMCS Quaresma, MCR Pitombeira… - European Journal of …, 2020 - Elsevier
The current treatment of Chagas disease is based on the use of two drugs, nifurtimox (Nfx)
and benznidazole (Bnz), both of which present limited efficacy in the chronic stage of the …