Exploring antimalarial potential: Conjugating organometallic moieties with organic fragments for enhanced efficacy

[Display omitted] In the search for novel ligands with efficacy against various diseases, particularly parasitic diseases, molecular hybridization of organometallic units into biologically active scaffolds has been hailed as an appealing strategy in medicinal chemistry. The conjugation to organometa...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic chemistry 2024-08, Vol.149, p.107510, Article 107510
Main Authors: Aqilah Zahirah Norazmi, Nur, Hafizah Mukhtar, Nur, Ravindar, Lekkala, Suhaily Saaidin, Aimi, Huda Abd Karim, Nurul, Hamizah Ali, Amatul, Kartini Agustar, Hani, Ismail, Norzila, Yee Ling, Lau, Ebihara, Masahiro, Izzaty Hassan, Nurul
Format: Article
Language:English
Subjects:
Animals
Antimalarial
Antimalarials - chemical synthesis
Antimalarials - chemistry
Antimalarials - pharmacology
Conjugation
Humans
Malaria - drug therapy
Molecular hybridization
Molecular Structure
Organometallic
Organometallic Compounds - chemical synthesis
Organometallic Compounds - chemistry
Organometallic Compounds - pharmacology
Parasitic Sensitivity Tests
Plasmodium falciparum - drug effects
Structure-Activity Relationship
Transition metal
Citations: Items that this one cites
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:[Display omitted] In the search for novel ligands with efficacy against various diseases, particularly parasitic diseases, molecular hybridization of organometallic units into biologically active scaffolds has been hailed as an appealing strategy in medicinal chemistry. The conjugation to organometallic fragments can be achieved by an appropriate linker or by directly coordinating the existing drugs to a metal. The success of Ferroquine (FQ, SR97193), an effective chloroquine–ferrocene conjugate currently undergoing the patient-exploratory phase as a combination therapy with the novel triaminopyrimidine ZY-19489 for malaria, has sparked intense interest in organometallic compound drug discovery. We present the evolution of organometallic antimalarial agents over the last decade, focusing on the parent moiety’s class and the type of organometallics involved. Four main organometallic antimalarial compounds have been chosen based on conjugated organic moieties: existing antimalarial drugs, other clinical drugs, hybrid drugs, and promising scaffolds of thiosemicarbazones, benzimidazoles, and chalcones, in particular. The presented insights contribute to the ongoing discourse on organometallic compound drug development for malaria diseases.
ISSN:0045-2068
1090-2120
1090-2120
DOI:10.1016/j.bioorg.2024.107510