5432-74-6Relevant articles and documents
New 1,4-di-N-oxide-quinoxaline-2-ylmethylene isonicotinic acid hydrazide derivatives as anti-Mycobacterium tuberculosis agents
Torres, Enrique,Moreno, Elsa,Ancizu, Saioa,Barea, Carlos,Galiano, Silvia,Aldana, Ignacio,Monge, Antonio,Perez-Silanes, Silvia
, p. 3699 - 3703 (2011)
The increase in the prevalence of drug-resistant tuberculosis cases demonstrates the need of discovering new and promising compounds with antimycobacterial activity. As a continuation of our research and with the aim of identifying new antitubercular drugs candidates, a new series of quinoxaline 1,4-di-N-oxide derivatives containing isoniazid was synthesized and evaluated for in vitro anti-tuberculosis activity against Mycobacterium tuberculosis H37Rv strain. Moreover, various drug-like properties of new compounds were predicted. Taking into account the biological results and the promising drug-likeness profile of these compounds, make them valid leads for further experimental research.
Preparation method of 2, 3-quinoxaline-1, 4-dioxide
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Paragraph 0008; 0030-0037, (2020/11/09)
The invention discloses a preparation method of 2, 3-quinoxaline-1, 4-dioxide, and belongs to the field of synthesis of medical intermediates. The method comprises the following steps: performing condensation cyclization on 1, 2-phenylenediamine serving as a raw material and 2, 3-butanedione to obtain 2, 3-dimethyl quinoxaline, and oxidizing the 2, 3-dimethyl quinoxaline with hydrogen peroxide under the action of a catalyst to obtain 2, 3-dimethyl quinoxaline-1, 4-dioxide; carrying out rearrangement and hydrolysis on the 2, 3-dimethyl quinoxaline-1, 4-dioxide and acid anhydride to obtain 2, 3-quinoxaline dimethanol; and finally, oxidizing the 2, 3-quinoxaline-1, 4-dioxide with hydrogen peroxide under the action of a catalyst to obtain the 2, 3-quinoxaline-1, 4-dioxide. By adopting the process route, the initial raw materials are easy to obtain, the cost is low, the total yield is as high as 64%, and industrial operation is facilitated.
Synthesis, biological evaluation and structure-activity relationships of new quinoxaline derivatives as anti-Plasmodium falciparum agents
Gil, Ana,Pabon, Adriana,Galiano, Silvia,Burguete, Asuncion,Perez-Silanes, Silvia,Deharo, Eric,Monge, Antonio,Aldana, Ignacio
, p. 2166 - 2180 (2014/03/21)
We report the synthesis and antimalarial activities of eighteen quinoxaline and quinoxaline 1,4-di-N-oxide derivatives, eight of which are completely novel. Compounds 1a and 2a were the most active against Plasmodium falciparum strains. Structure-activity