- A Facile and Versatile Synthesis of Energetic Furazan-Functionalized 5-Nitroimino-1,2,4-Triazoles
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An analogue-oriented synthetic route for the formulation of furazan-functionalized 5-nitroimino-1,2,4-triazoles has been explored. The process was found to be straightforward, high yielding, and highly efficient, and scalable. Nine compounds were synthesized and the physicochemical and energetic properties, including density, thermal stability, and sensitivity, were investigated, as well as the energetic performance (e.g., detonation velocities and detonation pressures) as evaluated by using EXPLO5 code. Among the new materials, compounds 4–6 and 11 possess high densities, acceptable sensitivities, and good detonation performances, and thereby demonstrate the potential applications as new secondary explosives.
- Xu, Zhen,Cheng, Guangbin,Yang, Hongwei,Ju, Xuehai,Yin, Ping,Zhang, Jiaheng,Shreeve, Jean'ne M.
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- Hybrid furoxanyl N-acylhydrazone derivatives as hits for the development of neglected diseases drug candidates
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Neglected diseases represent a major health problem. It is estimated that one third of the world population is infected with tuberculosis and additionally Leishmaniosis and Chagas disease affect approximately 30 million people. N-Acylhydrazone moiety is a
- Hernandez, Paola,Rojas, Rosario,Gilman, Robert H.,Sauvain, Michel,Lima, Lidia M.,Barreiro, Eliezer J.,Gonzalez, Mercedes,Cerecetto, Hugo
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- The first synthesis of furoxan and 1,3,4-oxadiazole ring ensembles
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Previously unknown furoxan and 1,3,4-oxadiazole ring ensembles incorporating two, three, and five furoxan and 1,3,4-oxadiazole rings in different combinations were for the first time synthesized from accessible azides and hydrazides of furoxancarboxylic acids. An interdependence of furoxan and 1,3,4-oxadiazole rings on their geometric parameters was revealed by the X-ray diffraction method.
- Finogenov, Aleksey O.,Kulikov, Alexander S.,Epishina, Margarita A.,Ovchinnikov, Igor V.,Nelyubina, Yu. V.,Makhova, Nina N.
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p. 135 - 140
(2013/03/13)
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- Discovery of new orally effective analgesic and anti-inflammatory hybrid furoxanyl N-acylhydrazone derivatives
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We report the design, the synthesis and the biological evaluation of the analgesic and anti-inflammatory activities of furoxanyl N-acylhydrazones (furoxanyl-NAH) by applying molecular hybridization approach. Hybrid compounds with IL-8-release inhibition capabilities were identified. Among them, furoxanyl-NAH, 17, and benzofuroxanyl-derivative, 24, together with furoxanyl-NAH derivative, 31, without IL-8 inhibition displayed both orally analgesic and anti-inflammatory activities. These hybrid derivatives do not have additional LOX- or COX-inhibition activities. For instance, LOX-inhibition by furoxanyl-NAH derivative, 42, emerged as a structural lead to develop new inhibitors. The lack of mutagenicity of the active derivatives 17, 31, and 42, allow us to propose them as candidates for further clinical studies. These results confirmed the success in the exploitation of hybridization strategy for identification of novel N-acylhydrazones (NAH) with optimized activities.
- Hernández, Paola,Cabrera, Mauricio,Lavaggi, María Laura,Celano, Laura,Tiscornia, Inés,Rodrigues Da Costa, Thiago,Thomson, Leonor,Bollati-Fogolín, Mariela,Miranda, Ana Luisa P.,Lima, Lidia M.,Barreiro, Eliezer J.,González, Mercedes,Cerecetto, Hugo
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experimental part
p. 2158 - 2171
(2012/05/04)
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