Hypoxia-Selective Agents Derived from 2-Quinoxalinecarbonitrile 1,4-Di-N-oxides. 2

Design of novel iron compounds as potential therapeutic agents against tuberculosis

“…The ligands L1-L4 were synthesized by reaction of the corresponding benzofuroxan and malonitrile and characterized as previously described [18]. L2 and L4 were obtained as mixtures of 6-and 7-substituted isomers [18].…”

Antimicrobial Activity of Quinoxaline Derivatives

“…Quinoxaline derivatives exhibit a broad spectrum of biological activity such as antibacterial [2][3][4] , antifungal 5,6 , antiviral 7 , anticancer 8 , anti-tubercular 9 , antimalarial 10 and anti-inflammatory 11 . Quinoxaline is well known for its broad coverage in the field of medicine as well as for its application in the pharmaceuticals.…”

Comparative use of solvent-free KF-A12O3and K2CO3in acetone in the synthesis of quinoxaline 1,4-dioxide derivatives designed as antimalarial drug candidates

“…Our research group has recently described the preparation and pharmacological evaluation of various quinoxaline 1,4-dioxides derivatives with antichagas, antimalarial, anticancer and antituberculosis activities [4][5][6][7][8][9][10]. For example, we reported that compound, 3-amino-2-quinoxalinecarbonitrile 1,4-dioxide (1), displays a hypoxia-selective cytotoxicity in cell culture which is similar to that observed for tirapazamine (TZP, 2), a clinically promising anticancer agent that selectively kills the hypoxic cells [4][5].…”

“…In an attempt to optimize the pharmacological activity of compound (3), a prototype of an antimalarial drug candidate [11], the synthesis of 2-(carboethoxy)-3-phenylquinoxaline 1,4-dioxide funcionalized derivatives (4)(5)(6)(7)(8)(9)(10)(11) was carried out in order to evaluate their antimalarial profile (Chart 1). This paper describes the systematic study of base and acid catalyst condensation of benzofurazan oxide (12) with ethyl benzoylacetate, as well as the comparative use of solvent free KF-Al 2 O 3 and K 2 CO 3 in acetone in the synthesis of the target esters (4-11) (Tables 1 and 2).…”