Synthesis of N1-arylidene-N2-quinolyl- and N2-acrydinylhydrazones as potent antimalarial agents active against CQ-resistant P. falciparum strains

Sandra Gemma; Gagan Kukreja; Caterina Fattorusso; Marco Persico; Maria P Romano; Maria Altarelli; Luisa Savini; Giuseppe Campiani; Ernesto Fattorusso; Nicoletta Basilico; Donatella Taramelli; Vanessa Yardley; Stefania Butini

doi:10.1016/j.bmcl.2006.07.060

Synthesis of N1-arylidene-N2-quinolyl- and N2-acrydinylhydrazones as potent antimalarial agents active against CQ-resistant P. falciparum strains

Bioorg Med Chem Lett. 2006 Oct 15;16(20):5384-8. doi: 10.1016/j.bmcl.2006.07.060. Epub 2006 Aug 4.

Authors

Sandra Gemma¹, Gagan Kukreja, Caterina Fattorusso, Marco Persico, Maria P Romano, Maria Altarelli, Luisa Savini, Giuseppe Campiani, Ernesto Fattorusso, Nicoletta Basilico, Donatella Taramelli, Vanessa Yardley, Stefania Butini

Affiliation

¹ Dipartimento Farmaco Chimico Tecnologico, Università di Siena, via Aldo Moro, 53100 Siena, Italy.

PMID: 16890433
DOI: 10.1016/j.bmcl.2006.07.060

Abstract

A series of N1-arylidene-N2-quinolyl- and N2-acrydinylhydrazones were synthesized and tested for their antimalarial properties. These compounds showed remarkable anti-plasmodial activity in vitro especially against chloroquine-resistant strains. Their potent biological activity makes them promising lead structures for the development of new antimalarial drugs.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Antimalarials / chemical synthesis*
Antimalarials / chemistry
Antimalarials / pharmacology*
Chloroquine / pharmacology*
Drug Resistance
Hydrazones / chemical synthesis*
Hydrazones / chemistry
Hydrazones / pharmacology*
Molecular Structure
Parasitic Sensitivity Tests
Plasmodium falciparum / drug effects*
Stereoisomerism
Structure-Activity Relationship

Substances

Antimalarials
Hydrazones
Chloroquine