Latest Update on Pharmacological Activities of 1,3,4-Oxadiazole Derivatives

Kumar, Brijesh; Kumar, Arvind

doi:10.4172/2157-7013.1000233

Cited by 15 publications

(8 citation statements)

References 19 publications

(22 reference statements)

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“…The cup plate agar diffusion method was used for the determination of the zone of inhibition. The results of antibacterial activity were summarized in (Table 3, Kumar et al [43]).…”

Section: Structure-activity Relationship Of 134-oxadiazole Derivativesmentioning

confidence: 99%

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Therapeutic potential of oxadiazole or furadiazole containing compounds

Siwach

Verma

2020

BMC Chemistry

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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.

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“…The cup plate agar diffusion method was used for the determination of the zone of inhibition. The results of antibacterial activity were summarized in (Table 3, Kumar et al [43]).…”

Section: Structure-activity Relationship Of 134-oxadiazole Derivativesmentioning

confidence: 99%

“…Kumar et al [ 43 ] developed 2-((1, 1′-biphenyl)-4-yl)-5-(substituted phenyl)-1,3,4-oxadiazole by using Scheme 3 . The antibacterial activity of these derivatives was evaluated against different Gram + ve ( S. aureus ) and Gram -ve ( K. pneumonia, E. coli , and P. aeruginosa ) strains using ofloxacin as a reference standard.…”

Section: Antimicrobial Activitymentioning

confidence: 99%

Therapeutic potential of oxadiazole or furadiazole containing compounds

Siwach

Verma

2020

BMC Chemistry

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“…The oxadiazole nucleus has emerged as one of the potential pharmacophores in medicinal chemistry [1][2][3][4]. Substituted oxadiazoles and their analogs have also been used as precursors for synthesis of various biologically active molecules [5][6][7], and also showed various activities such as antibacterial [8][9][10], antimycobacterial [11], antifungal [12,13], antiparasitic [14], anti-inflammatory [15], anti-allergy [16,17], analgesic [18], anticonvulsant [19,20], antihypoglycemic [21], insecticidal [22], anticancer properties [23,24].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Cytotoxicity and Antimicrobial Evaluation of Some New 2-Aryl,5-Substituted 1,3,4-Oxadiazoles and 1,3,4-Thiadiazoles

et al. 2018

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The synthesis of 2-(5-methyl-2-nitrophenyl)-5-(substituted)-1,3,4-oxadiazoles (5a-e) and thiadiazoles (6a-e) was carried out by refluxing of N-(5-methyl-2-nitrobenzoyl)-2-substituted carbohydrazide with phosphorous oxychloride and Lawesson's reagent respectively. The N-(5-methyl-2-nitrobenzoyl)-2-substituted carbohydrazides was synthesized by treating 2(5-methyl-2-nitrobenzohydrazide) with various aryl acids in the presence of HATU and DIPEA. Compounds 6a, 5c and 5d exhibited significant cytotoxic properties when compared to standard podophyllotoxin. Further, the compounds were also studied for their antibacterial activities.

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“…Oliveira and co-workers reported synthesis and anti-staphylococcal activity of 1, 3, 4-oxadiazolines against strains of S.aureus, resistant to methicillin and amino glycosides and that encode efflux proteins (multidrug drugs resistant-MDR more active than the standard drug chloramphenicol [12]. The antibacterial and antifungal activity of 2-(5-amino-1,3,4oxadiazol-2-yl)-4-bromophenol and 5-(3,5-dibromophenyl)-1,3,4-oxadiazol-2-amine were investigated against grampositive bacteria, gram-negative bacteria and fungal species approximately equal to the standard drugs of treatment streptomycin and Griseofulvin [13]. 2,5-disubstituted 1,3,4 oxadiazoles were reported as potent antibacterial and antifungal agents [14] (Figure 1).…”

Section: Introductionmentioning

confidence: 99%

An approach to design, in silico predictions and molecular docking studies of 1,3,4-oxadiazolyl sulphonamides as possible inhibitors of bacterial Mur enzymes, the amino acid ligases in peptidoglycan synthesis

Banu¹

2017

JARB

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The extensive use of antibiotics in hospitals and community since their introduction into medical practice has created major evolutionary pressures in bacteria to develop various resistance mechanisms. This phenomenon has led to increased morbidity, mortality and health care costs. The search for new antibacterial agents directed towards novel targets became highly imperative. The biosynthetic pathway of cytoplasmic peptidoglycan precursor is currently gaining much interest as a target site for antibacterial therapy. Since the mid-1990s, many inhibitors of the Mur cytoplasmic enzymes have been reported, but none has yet led to the development of a clinically utilized therapeutic agent. In view of the potentiality of sulphonamide and 1,3,4-oxadiazole moieties, it was planned to incorporate both the scaffolds. Thus a series of 4-Amino-N-[(5-phenyl-1,3,4-oxadiazol-2-yl)methyl] substituted benzene-1-sulfonamides (1-10) were designed, predicted for molecular properties and docking studies were conducted on Mur enzymes. The presence of the two pharmacophoric scaffolds, oxadiazole and sulphonamide influenced the good bioactive scores. Docking studies further supported the biological activities. The results indicated the possible inhibitory activity towards the Mur enzymes. The results also indicate the selectivity towards Mur A, Mur C, & Mur E enzymes. Of all the compounds, compound 6 and compound 9 with isopropyl substitution exhibited the highest scores against all the three Mur enzymes. Compound 7 showed good binding interactions with Mur C and Mur E.

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Latest Update on Pharmacological Activities of 1,3,4-Oxadiazole Derivatives

Cited by 15 publications

References 19 publications

Therapeutic potential of oxadiazole or furadiazole containing compounds

Therapeutic potential of oxadiazole or furadiazole containing compounds

Synthesis, Cytotoxicity and Antimicrobial Evaluation of Some New 2-Aryl,5-Substituted 1,3,4-Oxadiazoles and 1,3,4-Thiadiazoles

An approach to design, in silico predictions and molecular docking studies of 1,3,4-oxadiazolyl sulphonamides as possible inhibitors of bacterial Mur enzymes, the amino acid ligases in peptidoglycan synthesis

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