67139-38-2Relevant academic research and scientific papers
Aurones and Analogues: Promising Heterocyclic Scaffolds for Development of Antioxidant and Antimicrobial Agents
Irshad,Ali,Iram,Ahamad,Saleem,Saadia,Batool,Kanwal,Tabassum
, p. 1519 - 1527 (2019/08/21)
Synthesis of some new multi-functional analogues of 2′-hydroxy chalcone containing isoxazole and pyrazole functions were synthesized, and their pharmacological activity was tested. Chalcone derivatives were synthesized by the reaction of 2′-hydroxy acetophenone with various substituted benzaldehydes in a basic medium. Aurones were isolated upon treatment with mercuric acetate. Synthesized chalcones and aurones were converted into the corresponding isoxazole and pyrazole derivatives upon their reaction with hydroxylamine hydrochloride or hydrazine hydrate, respectively. Structures of the compounds were confirmed by spectroscopic methods. All synthesized compounds were tested for antioxidant and antibacterial potential. Some of those demonstrated excellent antioxidant activity, and one product was identified as a promising antimicrobial candidate.
Synthesis of 3,5-diarylisoxazole derivatives and evaluation of in vitro trypanocidal activity
De Souza, Aline A. N.,Xavier, Viviane F.,Coelho, Gleicekelly S.,Sales Junior, Policarpo A.,Romanha, Alvaro J.,Murta, Silvane M. F.,Carneiro, Claudia M.,Taylor, Jason G.
, p. 269 - 277 (2017/12/08)
Chagas disease is included in the neglected tropical diseases list and is endemic to 21 Latin American countries. The two drugs currently available for treating Chagas disease are nifurtimox and benznidazole and both result in many significant side effects. The study describes the synthesis and biological evaluation of 3,5-disubstituted isoxazoles. Isoxazoles were obtained by reaction of flavones and hydroxylamine and either alkylated at the free hydroxyl group and/or nitrated at the isoxazole ring. These compounds were evaluated for their in vitro anti-Trypanosoma cruzi activity against trypomastigote and amastigote forms of the parasite in T. cruzi-infected cell lineages. Benznidazole was used as a reference compound for the in vitro assay and mammalian L929 cells were employed to evaluate cytotoxicity. A majority of the compounds tested were very active and the most active isoxazole against amastigote and trypomastigotes of T. cruzi was slightly more potent than the current medicine benznidazole.
β-cyclodextrin (β-CD) as a supramolecular catalyst for the synthesis of isoxazoles and thiopyrimidines and their antimicrobial screening
Chate, Asha V.,Gill, Charansingh H.
, p. 93 - 102 (2017/03/30)
Background: Isoxazole and pyrimidines are interesting heterocyclic molecules, which are present as structural motif in numerous natural products synthetic drugs. Isoxazole and thiopyrimidines exhibit antidiabetic, cytotoxic tuberculostatic, and anticonvul
The Preparation of 5-Phenacylisoxazoles and 5-Hydroxyphenylisoxazoles and -pyrazoles by the Condensation of C(α)-Dianions with Ethyl Benzoylacetate and Methyl Salicylate
Livingston, Melanie J.,Chick, MarLisa F.,Shealy, Ernest O.,Beam, Charles F.
, p. 215 - 217 (2007/10/02)
C(α),O-Dilithiooximes and C(α),N-Dilithiophenylhydrazones were prepared in an excess of lithium diisopropylamide (LDA).The former was condensed with ethyl benzoylacetate and methyl salicylate, and the latter condensed with methyl salicylate.The resulting precyclization intermediates were than treated with aqueous acid, which was followed by cyclodehydration to give phenacylisoxazoles and hydroxyphenylisoxazoles and -pyrazoles.
