Title:Imidazole and Pyrazole: Privileged Scaffolds for Anti-Infective Activity
VOLUME: 15 ISSUE: 6
Author(s):K. Tabassum*, P. Ekta and P. Kavitkumar
Affiliation:Department of Pharmaceutical Chemistry & Quality Assurance, SVKM`s Dr. Bhanuben Nanavati College of Pharmacy, Mumbai, Maharashtra, Department of Pharmaceutical Chemistry & Quality Assurance, SVKM`s Dr. Bhanuben Nanavati College of Pharmacy, Mumbai, Maharashtra, Department of Pharmaceutical Chemistry & Quality Assurance, SVKM`s Dr. Bhanuben Nanavati College of Pharmacy, Mumbai, Maharashtra
Keywords:Imidazole, pyrazole, anti-bacterial, anti-fungal, anti-leishmanial, anti-viral.
Abstract:Heterocyclic scaffolds like imidazole and pyrazole are attractive options to medicinal and synthetic
chemists for the development of drugs. Nature utilizes the unique type of imidazole ring in numerous biological
molecules such as histamine, vitamin B12, deoxyribonucleic acid (DNA) and haemoglobin for exerting
various biological functions. This shows that the imidazole ring is vital to many physiological processes
and hence important for modulating altered physiology. Imidazole and pyrazole analogues have been reported
to show a varied spectrum of activities like antibacterial, antifungal, antiviral, antimalarial, antitubercular,
antileishmanial, anticancer, anti-inflammatory, antineuropathic, antiparasitic, antihistaminic, antihypertensive,
antiobesity, etc. and hence are valuable scaffolds for the development of new therapeutic agents. Many
azole-based antibacterial and antifungal agents have been extensively studied as drug candidates and some
of them are used clinically for instance ketoconazole, itraconazole, fluconazole, posaconazole and voriconazole,
which suggests their great development value. Myriad of structural modifications on these scaffolds
have provided a wide spectrum of activity and scope for the enhancement of activity. Reviews on the biological
importance of these scaffolds have been published over the past decade or two. However, we did not
come across reviews that combined the synthetic strategies of some bioactive substituted imidazole and pyrazole
compounds along with the impact of substitutions on their anti-infective activity. The pursuit of structurally
novel anti-infective imidazoles and pyrazoles with increased potency, broader spectrum and lower
toxicity is a highly challenging task and is of great interest in medicinal chemistry. This review will be useful
for synthesizing imidazole and pyrazole analogues for the development of new potent anti-infective
agents that will also help overcome the issue of emerging multidrug resistance observed with the existing
anti-infective drugs.
