Current development of 1,2,3-triazole derived potential antimalarial scaffolds: Structure- activity relationship (SAR) and bioactive compounds

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dc.contributor.authorAbdul Rahman, S. Maheen
dc.contributor.authorBhatti, Jasvinder Singh
dc.contributor.authorThareja, Suresh
dc.contributor.authorMonga, Vikramdeep
dc.date.accessioned2024-01-21T10:54:15Z
dc.date.accessioned2024-08-14T07:41:00Z
dc.date.available2024-01-21T10:54:15Z
dc.date.available2024-08-14T07:41:00Z
dc.date.issued2023-07-30T00:00:00
dc.description.abstractMalaria is among one of the most devastating and deadliest parasitic disease in the world claiming millions of lives every year around the globe. It is a mosquito-borne infectious disease caused by various species of the parasitic protozoan of the genus Plasmodium. The indiscriminate exploitation of the clinically used antimalarial drugs led to the development of various drug-resistant and multidrug-resistant strains of plasmodium which severely reduces the therapeutic effectiveness of most frontline medicines. Therefore, there is urgent need to develop novel structural classes of antimalarial agents acting with unique mechanism of action(s). In this context, design and development of hybrid molecules containing pharmacophoric features of different lead molecules in a single entity represents a unique strategy for the development of next-generation antimalarial drugs. Research efforts by the scientific community over the past few years has led to the identification and development of several heterocyclic small molecules as antimalarial agents with high potency, less toxicity and desired efficacy. Triazole derivatives have become indispensable units in the medicinal chemistry due to their diverse spectrum of biological profiles and many triazole based hybrids and conjugates have demonstrated potential in vitro and in vivo antimalarial activities. The manuscript compiled recent developments in the medicinal chemistry of triazole based small heterocyclic molecules as antimalarial agents and discusses various reported biologically active compounds to lay the groundwork for the rationale design and discovery of triazole based antimalarial compounds. The article emphasised on biological activities, structure activity relationships, and molecular docking studies of various triazole based hybrids with heterocycles such as quinoline, artemisinins, naphthyl, naphthoquinone, etc. as potential antimalarial agents which could act on the dual stage and multi stage of the parasitic life cycle. � 2023 Elsevier Masson SASen_US
dc.identifier.doi10.1016/j.ejmech.2023.115699
dc.identifier.issn2235234
dc.identifier.urihttp://10.2.3.109/handle/32116/4261
dc.identifier.urlhttps://linkinghub.elsevier.com/retrieve/pii/S0223523423006669
dc.language.isoen_USen_US
dc.publisherElsevier Masson s.r.l.en_US
dc.subjectAntimalarialen_US
dc.subjectHeterocyclic compoundsen_US
dc.subjectInfectious diseasesen_US
dc.subjectMalariaen_US
dc.subjectPlasmodium falciparumen_US
dc.subjectQuinolineen_US
dc.subjectTriazoleen_US
dc.titleCurrent development of 1,2,3-triazole derived potential antimalarial scaffolds: Structure- activity relationship (SAR) and bioactive compoundsen_US
dc.title.journalEuropean Journal of Medicinal Chemistryen_US
dc.typeReviewen_US
dc.type.accesstypeClosed Accessen_US

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