Title:Coumarin-1,2,3-triazole Hybrid Molecules: An Emerging Scaffold for Combating Drug Resistance
Volume: 21
Issue: 8
Author(s): Harish C. Upadhyay*
Affiliation:
- Laboratory of Chemistry, Department of Applied Sciences, Rajkiya Engineering College (Affiliated to Dr. A.P.J. Abdul Kalam Technical University, Lucknow), Churk, Sonbhadra-231206,India
Keywords:
Drug-resistance, Coumarin, 1, 2, 3-Triazole, Hybrid molecules, Antibacterial, Antitubercular.
Abstract: Undoubtedly, antibiotics have saved billions of lives, but lack of novel antibiotics, development
of resistance mechanisms in almost all clinical isolates of bacteria, and recurrent infections
caused by persistent bacteria hamper the successful treatment of the infections. Due to the widespread
emergence of resistance, even the new families of anti-microbial agents have a short life expectancy.
Drugs acting on a single target often lead to drug resistance and are associated with various
side effects. For overcoming this problem, either multidrug therapy, or a single drug acting on
multiple targets may be used. The latter is called ‘hybrid molecules,’ which are formed by clubbing
two biologically active pharmacophores together, with or without an appropriate linker. In this
rapidly evolving era, the development of natural product-based hybrid molecules may be a super-alternative
to multidrug therapy, for combating drug resistance caused by various bacterial and fungal
strains. Coumarins (benzopyran-2-one) are one of the earliest reported plant secondary metabolites
having a clinically proven diverse range of pharmacological properties. On the other hand,
1,2,3-triazole is a common pharmacophore in many drugs responsible for polar interactions, improving
the solubility and binding affinity to biomolecular targets. In this review, we discuss recent
advances in Coumarin-1,2,3-triazole hybrids as potential anti-bacterial agents, aiming to provide a
useful platform for the exploration of new leads with a broader spectrum, more effectiveness and
less toxicity with multiple modes of action for the development of cost-effective and safer drugs in
the future.
