Synthesis and Evaluation of Antifungal Activity of Novel 1,3,4-Oxadiazole Derivatives

Aswathy  Ramesh; Rakesh Kumar Jat; R  Arunkumar

doi:10.22270/ijmspr.v10i1.85

Authors

Aswathy Ramesh PhD scholar, JJT University, Rajasthan, Jhunjhunu, India
Rakesh Kumar Jat HOD, Department of Pharmacy, JJT University, Rajasthan, Jhunjhunu, India
R Arunkumar Principal, Holygrace Academy of Pharmacy, Thrissur, Kerala, India

DOI:

https://doi.org/10.22270/ijmspr.v10i1.85

Keywords:

1,3,4-oxadiazole, antifungal activity, Disc diffusion method, MIC

Abstract

Here new eight derivatives of 1,3,4-oxadiazole were synthesised from salicylic acid and phenyl acetic acid by ring condensation mechanism. The synthesized derivatives were characterized and structures were confirmed by various spectral analysis. Antifungal activity studies revealed that Ox1, Ox2 and Ox4 exhibit promising activity.

Keywords: 1,3,4-oxadiazole, antifungal activity, Disc diffusion method, MIC,

Author Biographies

Aswathy Ramesh , PhD scholar, JJT University, Rajasthan, Jhunjhunu, India

PhD scholar, JJT University, Rajasthan, Jhunjhunu, India

Rakesh Kumar Jat, HOD, Department of Pharmacy, JJT University, Rajasthan, Jhunjhunu, India

HOD, Department of Pharmacy, JJT University, Rajasthan, Jhunjhunu, India

R Arunkumar , Principal, Holygrace Academy of Pharmacy, Thrissur, Kerala, India

Principal, Holygrace Academy of Pharmacy, Thrissur, Kerala, India

References

Chandrakantha B, Shetty P, Nambiar V, Isloor N, Isloor AM, Synthesis, characterization and biological activity of some new 1, 3, 4-oxadiazole bearing 2-flouro-4-methoxyphenyl moiety, European Journal of Medicinal Chemistry, (2010); 45:1206 – 1210 https://doi.org/10.1016/j.ejmech.2009.11.046 PMid:20004043

De-Oliveira CS, Lira BF, Barbosa-Filho JM, Lorenzo JGF, de-Menezes CP, de-Lima O, dos-Santos JMCG, de-Athayde-Filho PF, Synthesis and testing of 3-acetyl-2, 5-disubstituted-2, 3-dihydro-1, 3, 4-oxadiazole derivatives for antifungal activity against selected Candida species, Journal of the Brazilian Chemical Society, 2013; 24:1-5 https://doi.org/10.1590/S0103-50532013000100016

Filimonov DA, Poroikov VV, Karaicheva EI, Computer-aided prediction of biological activity spectra of chemical substances on the basis of their structural formulae: computerized system PASS, Experimental and Clinical Pharmacology (Rus.), 1995; 4:56-62

Henry DI, Clinical Microbiology Procedure Handbook, American society for microbiology/ Washington, D.C., 1992 ;1

/ Joule JA, Mills K, Smith G F. Heterocyclic Chemistry https://www.en.wikipedia.org/wiki/Oxadiazole , 3:452

Lipinski CA, Lombardo F, Dominy BW, Feeney PJ, Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings, Advanced Drug Delivery Reviews, 2001; 2:3-25.

Parikh PK, Marvaniya HM, Prof.Dr.Sen DJ, Synthesis and biological evaluation of 1, 3, 4-oxadiazole derivatives as potential antibacterial and antifungal agents, International Journal of Drug Development and Research, 2011; 3(2):248-255

Pattan SR, Rabra PA, Pattan JS, Bukitager AA, Wakale VS, Musmade DS, Synthesis and evaluation of some novel substituted 1, 3, 4-oxadiazole and pyrazole derivatives for antitubercular activity, Indian Journal of Chemistry, 2009; 48B:1453-1456 https://doi.org/10.1002/chin.201006125

Pavia, Lampman, Kriz, Engel, Introduction to Organic Laboratory Techniques: A Microscale Approach, Saunders College Publishing, 1999

Prakash O, Kumar M, Kumar R, Sharma C, Aneja KR, Hypervalent iodine (III) mediated synthesis of novel unsymmetrical 2, 5-disubstituted 1, 3, 4-oxadiazoles as antibacterial anti-fungal agents, European Journal of Medicinal Chemistry, 2010; 45:4252-4257 https://doi.org/10.1016/j.ejmech.2010.06.023 PMid:20630627

Saini R, Rai AK, Kesari AN, Yar MS, Synthesis and biological evaluation of 2, 5-disubstituted-1, 3, 4-oxadiazoles, Asian Journal of Research and Chemistry, 2009; 2: 34-36.

Schwalve, Moore and Goodwin, Antimicrobial susceptibility testing protocols, CRC Press, 2007 https://doi.org/10.1201/9781420014495

Sharma S, Sharma PK, Kumar N, Dhude R, A review: oxadiazole: their Chemistry and Pharmacological potential, Der Pharma Chemica, 2010; 2: 253-263

Tomi IHR, Al-Qaisi AHJ, Al-Qaisi ZHJ, Synthesis, characterization and effect of bis-1, 3, 4-oxadiazole containing glycine moiety on the activity of some transferase enzymes. IBN Al-Haitham, Journal for Pure and Applied Sciences, 2010; 23:1-13. https://doi.org/10.1016/j.jksus.2010.06.002

Ur-Rehman A, Siddiqui S, Abbasi MA, Abbas N, Khan KM, Shahid M, Mahmood Y, Akthar MN, Lajis NH, Synthesis, antibacterial screening and haemolytic activity of S-substituted derivatives of 5-benzyl-1, 3, 4-oxadiazole-2-thiol, International Journal of Pharmacy and Pharmaceutical Sciences, 2012; 4:676-680