title: Recent advances in novel heterocyclic scaffolds for the treatment of drug-resistant malaria.
abstract: Malaria is a major public health problem all over the world, particularly in tropical and subtropical countries due to the development of resistance and most deadly infection is caused by Plasmodium falciparum. There is a direct need for the discovery of new drugs with unique structures and mechanism of action to treat sensitive and drug-resistant strains of various plasmodia for radical cure of this disease. Traditional compounds such as quinine and related derivatives represent a major source for the development of new drugs. This review presents recent modifications of 4-aminoquinoline and 8-aminoquinolone rings as leads to novel active molecules which are under clinical trials. The review also encompasses the other heterocyclic compounds emerged as potential antimalarial agents with promising results such as acridinediones and acridinone analogues, pyridines and quinolones as antimalarials. Miscellaneous heterocyclics such as tetroxane derivatives, indole derivatives, imidazolopiperazine derivatives, biscationic choline-based compounds and polymer-linked combined antimalarial drugs are also discussed. At last brief introduction to heterocyclics in natural products is also reviewed. Most of them have been under clinical trials and found to be promising in the treatment of drug-resistant strains of Plasmodium and others can be explored for the same purpose.
authors.affiliation: a Department of Pharmaceutical Chemistry , Indo-Soviet Friendship (I.S.F.) College of Pharmacy , Moga , Punjab , India .|b Faculty of Pharmacy , Punjab Technical University , Jalandhar, Kapurthala , India .
authors.forename: Sahil
authors.initials: S
authors.lastname: Kumar
authors.affiliation: c Department of Pharmaceutical Chemistry , Shivalik College of Pharmacy , Nangal, Dist. Rupnagar , Punjab , India , and.
authors.forename: Rajesh K
authors.initials: RK
authors.lastname: Singh
authors.affiliation: a Department of Pharmaceutical Chemistry , Indo-Soviet Friendship (I.S.F.) College of Pharmacy , Moga , Punjab , India .
authors.forename: Babita
authors.initials: B
authors.lastname: Patial
authors.affiliation: a Department of Pharmaceutical Chemistry , Indo-Soviet Friendship (I.S.F.) College of Pharmacy , Moga , Punjab , India .
authors.forename: Sachin
authors.initials: S
authors.lastname: Goyal
authors.affiliation: a Department of Pharmaceutical Chemistry , Indo-Soviet Friendship (I.S.F.) College of Pharmacy , Moga , Punjab , India .|d Department of Pharmaceutical Chemistry , University Institute of Pharmaceutical Sciences, Panjab University , Chandigarh , India.
authors.forename: T R
authors.initials: TR
authors.lastname: Bhardwaj
mesh_terms: D000166:Acridines / Q000737:chemistry; D000634:Aminoquinolines / Q000737:chemistry / Q000494:pharmacology; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001688:Biological Products / Q000737:chemistry / Q000494:pharmacology; D002986:Clinical Trials as Topic; D004352:Drug Resistance, Microbial / Q000187:drug effects; D005296:Ferrous Compounds / Q000737:chemistry / Q000494:pharmacology; D006571:Heterocyclic Compounds / Q000737:chemistry*; D006801:Humans; D008288:Malaria / Q000188:drug therapy; D000075163:Metallocenes; D011728:Pyridones / Q000737:chemistry; D011743:Pyrimidines / Q000737:chemistry
chemical_list: D000166:Acridines; D000634:Aminoquinolines; D000962:Antimalarials; D001688:Biological Products; D005296:Ferrous Compounds; D006571:Heterocyclic Compounds; D000075163:Metallocenes; D011728:Pyridones; D011743:Pyrimidines; C025152:aminoquinolone; C479230:ferroquine; C001920:4-aminoquinoline
keywords: Antimalarial; Plasmodium; drug-resistance; heterocyclic analogs; malaria