Synthesis and Antimalarial Activity of New 3-Arylquinoxaline-2-carbonitrile Derivatives

doi:10.1055/s-0031-1296926

Paper

Synthesis and Antimalarial Activity of New 3-Arylquinoxaline-2-carbonitrile Derivatives

Published Dec 1, 2005 · Belén Zarranz, Andrés Jaso, I. Aldana

Arzneimittelforschung

UNKNOWN SJR score

41

Citations

2

Influential Citations

Full textSemantic Scholar

Abstract

Summary New series of 3-arylquinoxaline-carbonitrile derivatives have been synthesized from various 5-substituted or 5,6-disubstituted benzofuroxanes and tested for their in vitro and in vivo activity against the erythrocytic development of Plasmodium falciparum strain with different chloroquine-resistance status. Quinoxaline 1,4-dioxide derivatives showed superior antimalarial activity in respect to reduced quinoxaline analogues. The best activity was observed with nonsubstituted quinoxaline 1,4-dioxides in positions 6 and 7 of the aromatic ring and with a hydrogen or chloro substituent in para position of the phenyl group.

In Vitro Study

Study Snapshot

New 3-arylquinoxaline-2-carbonitrile derivatives show superior antimalarial activity, particularly with quinoxaline 1,4-dioxide derivatives in positions 6 and 7.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Sign up to use Study Snapshot

Consensus is limited without an account. Create an account or sign in to get more searches and use the Study Snapshot.

Create an account

Paper

Synthesis and Antimalarial Activity of New 3-Arylquinoxaline-2-carbonitrile Derivatives

Sign up to use Study Snapshot

References

Synthesis of new quinoxaline-2-carboxylate 1,4-dioxide derivatives as anti-Mycobacterium tuberculosis agents.

New quinoxaline-2-carboxylate 1,4-dioxide derivatives show potency, selectivity, and low cytotoxicity against Mycobacterium tuberculosis, making them valid leads for synthesizing new compounds with better activity.

Quinoxaline N,N'-dioxide derivatives and related compounds as growth inhibitors of Trypanosoma cruzi. Structure-activity relationships.

Quinoxaline derivatives show good inhibitory activity against Trypanosoma cruzi growth, with derivative 13 and reduced derivatives 19 and 20 showing the most cytotoxic effects.

Synthesis, antimalarial activity, and molecular modeling of new pyrrolo[1,2-a]quinoxalines, bispyrrolo[1,2-a]quinoxalines, bispyrido[3,2-e]pyrrolo[1,2-a]pyrazines, and bispyrrolo[1,2-a]thieno[3,2-e]pyrazines.

Bispyrrolo[1,2-a]quinoxalines show superior antimalarial activity, with the best activity observed with bispyrrolo[1,2-a]quinoxalines linked by a bis(3-aminopropyl)piperazine.

Anti-malarial activity of some 7-chloro-2-quinoxalinecarbonitrile-1,4-di-N-oxide derivatives.

The presence of a piperazine ring is essential for antimalarial activity, with compounds 4a and 5 showing the highest activity.

Water stability and cytotoxic activity relationship of a series of ferrocenium derivatives. ESR insights on the radical production during the degradation process.

DEMFc(+) is the most stable ferrocenium derivative, with the highest cytotoxic activity against MCF-7 cells, and its degradation in water produces oxygen radicals, which can cause DNA damage and synergize with bleomycin.

Citations

One-Pot Synthesis and In Vitro Studies of Calix[4]-2-methylresorcinarene Derivatives as Antimalarial Agents Against Plasmodium falciparum Chloroquine-Resistant Strain FCR-3

Calix[4]-2-methylresorcinarene derivatives show potent antimalarial activity against Plasmodium falciparum FCR-3, with the most potent activity observed in the C-4-chlorophenylcalix[4]-2-methylresorcinerene compound

Design and Synthesis of Novel Quinoxaline-Piperazine Linked Isoxazole Conjugates: Anti-cancer Assessment, tyrosine kinase EGFR inhibitory activity, Molecular Docking and DFT Studies

Novel quinoxaline-piperazine-isoxazole conjugates show promising anti-cancer activity and tyrosine kinase EGFR inhibitory potency, with compounds 7f, 7e, and 7 g showing higher EGFR binding interactions than Erlotinib.

Synthesis and evaluation of sulfonamide derivatives of quinoxaline 1,4-dioxides as carbonic anhydrase inhibitors

Sulfonamide-derived quinoxaline 1,4-dioxides show promising inhibitory activity against carbonic anhydrases, with potential for developing chemotherapeutic agents targeting carbonic anhydrases.

Quinoxaline 1,4-Dioxides: Advances in Chemistry and Chemotherapeutic Drug Development

Quinoxaline 1,4-dioxides show promise for developing new drugs targeting bacterial infections, oncological diseases, and various parasitic diseases.

An appraisal on synthetic and pharmaceutical perspectives of quinoxaline 1,4‐di‐N‐oxide scaffold

QdNOs exhibit multifaceted biological properties, offering potential for diverse uses in clinical practice and research, with current research guiding the development of novel synthetic techniques and derivatives.