Oxadiazole: A highly versatile scaffold in drug discovery

Abstract

As a pharmacologically important heterocycle, oxadiazole paved the way to combat the problem associated with the confluence of many commercially available drugs with different pharmacological profiles. The present review focuses on the potential applications of five-membered heterocyclic oxadiazole derivatives, especially 1,2,4-oxadiazole, 1,2,5-oxadiazole, and 1,3,4-oxadiazole, as therapeutic agents. Designing new hybrid molecules containing the oxadiazole moiety is a better solution for the development of new drug molecules. The designed molecules may accumulate a biological profile better than those of the drugs currently available on the market. The present review will guide the way for researchers in the field of medicinal chemistry to design new biologically active molecules based on the oxadiazole nucleus. Antitubercular, antimalarial, anti-inflammatory, anti-HIV, antibacterial, and anticancer activities of various oxadiazoles have been reviewed extensively here.

Therapeutic potential of 1,3,4-oxadiazoles as potential lead compounds for the treatment of Alzheimer's disease

“…13 Oxadiazole ring is a highly versatile building block in several medicines and in the scope of future drug development. 16 Several activities were reported with 1,3,4-oxadiazole containing compounds including; anti-hypertensive (Tiodazosin), anti-inammatory, anti-fungal, antibacterial, antiviral (Raltegravir), anticonvulsant, hypnotic (Fenadiazole), anticancer (Zibotentan), anti-AD, and many others. 7,[16][17][18][19][20][21] Also, several oxadiazole derivatives were reported in literature as MAO and ChE inhibitors (Fig.…”

Synthesis, Antifungal Ergosterol Inhibition, Antibiofilm Activities, and Molecular Docking on β-Tubulin and Sterol 14-Alpha Demethylase along with DFT-Based Quantum Mechanical Calculation of Pyrazole Containing Fused Pyridine–Pyrimidine Derivatives

“… They have broad-spectrum antifungal activity against the majority of filamentous fungi, but several of them are ineffective against invasive aspergillosis and have substantial drug resistance . Furthermore, widespread usage of existing antifungal medications has resulted in significant drug resistance . As a result, novel antifungal agents with outstanding action against a wide range of clinical fungal species are urgently needed.…”

Design, synthesis, antimicrobial evaluation, and in‐silico studies of some 4‐thiazolidinone hybrids bearing coumarin and pyridine moieties

“…Heterocyclic compounds have drawn the attention of scientific experts and pharmacologists in light of their biological significance [1,2]. It has been observed that hybrids of bioactive pharmacophores (pyridine, coumarin, and 4-thiazolidinone) in the current medications create a significant effect on the pharmaceutical profile [3][4][5][6][7][8]. This has provoked us to attempt the synthesis of bioactive molecules in which thiazolidinone moiety has been merged with other pharmaceutically active entities like coumarin and pyridine.…”