Therapeutic potential of oxadiazole or furadiazole containing compounds

Abstract

As we know that, Oxadiazole or furadi azole ring containing derivatives are an important class of heterocyclic compounds. A heterocyclic five-membered ring that possesses two carbons, one oxygen atom, two nitrogen atoms, and two double bonds is known as oxadiazole. They are derived from furan by the replacement of two methylene groups (= CH) with two nitrogen (-N =) atoms. The aromaticity was reduced with the replacement of these groups in the furan ring to such an extent that it shows conjugated diene character. Four different known isomers of oxadiazole were existed such as 1,2,4-oxadiazole, 1,2,3-oxadiazole, 1,2,5-oxadiazole & 1,3,4-oxadiazole. Among them, 1,3,4-oxadiazoles & 1,2,4-oxadiazoles are better known and more widely studied by the researchers due to their broad range of chemical and biological properties. 1,3,4-oxadiazoles have become important synthons in the development of new drugs. The derivatives of the oxadiazole nucleus (1,3,4-oxadiazoles) show various biological activities such as antibacterial, anti-mycobacterial, antitumor, anti-viral and antioxidant activity, etc. as reported in the literature. There are different examples of commercially available drugs which consist of 1,3,4-oxadiazole ring such as nitrofuran derivative (Furamizole) which has strong antibacterial activity, Raltegravir as an antiviral drug and Nesapidil drug is used in anti-arrhythmic therapy. This present review summarized some pharmacological activities and various kinds of synthetic routes for 2, 5-disubstituted 1,3,4-oxadiazole, and their derived products.

Design, Synthesis, In Silico and In Vitro Studies for New Nitric Oxide-Releasing Indomethacin Derivatives with 1,3,4-Oxadiazole-2-thiol Scaffold

“…Moreover, it was reported that 1,3,4-oxadiazole scaffold has been found to be a potent antioxidant pharmacophore, and chemical modulation of the conventional drugs with this scaffold resulted in a synergistic effect, enhancing the antioxidant efficiency of the parent drug [47,49,50,83,84]. In our research, the presence of 1,3,4-oxadiazole scaffold significantly enhanced antioxidant activity for the majority of the NO-IND-OXDs.…”

“…On the other hand, the oxadiazole scaffold serves as core for many synthetic compounds of great interest in medicinal chemistry [47][48][49]. Its use offers several advantages: (i) it is an essential part of the pharmacophore, based on its ligand binding role; (ii) it acts as a flat aromatic linker assuring an appropriate molecule orientation; (iii) it induces metabolic stability, water solubility and lower lipophilicity; (iv) it can easily chemically modulate the compounds which contain carbonyl groups such as amides, carbamates, esters and hydoxamic esters [32,50,51].…”

Synthesis, X-ray diffraction analysis, quantum chemical studies and α-amylase inhibition of probenecid derived S-alkylphthalimide-oxadiazole-benzenesulfonamide hybrids

“…Besides α -amylase inhibition, 1,3,4-oxadizole-based compounds have been found in commercially available drugs such as raltegravir as an antiviral agent, furamizole as an antibacterial agent, nesapidil as an antiarrhythmic agent and tiodazosin as an antihypertensive agent 35 . The structures of commercial drugs are shown in ( Figure 1(b) ).…”

Antimicrobial Activity of 1,3,4-Oxadiazole Derivatives

“…Oxadiazoles are five-membered heterocyclic compounds containing two nitrogen atoms and one oxygen atom in their structure. We can distinguish several isomeric forms of oxadiazole, which occur in the structure of many drugs, e.g., anticancer zibotentan [5], antimicrobial furamizole [6], antiviral raltegravir [7], ataluren for Duchenne muscular dystrophy [8] and others (Figure 1).…”