28May 2017

IN VITRO ANTIMICROBIAL ACTIVITY OF NEW SUBSTITUTED 1,3,4-OXADIAZOLE DERIVATIVES.

  • Young Researchers and Elite Club, Urmia Branch, Islamic Azad University, Urmia, Iran.
  • Faculty of science, Urmia Branch, Islamic Azad University, Urmia, Iran.
  • Department of laboratory Sciences, School of Paramedicine, Tabriz Universityof Medical Sciences, Tabriz, Iran.
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Background: The need of new antimicrobial agents is justified because more microorganisms are being resistance to the currently available antibacterial drugs and this is bringing alarming threat to public health and causing growing concern among people across the globe. 1,3,4-Oxadiazole have shown a wide spectrum of antimicrobial activity. Some of the marketed drugs also possessed this heterocyclicmoiety. Objectives: We have previously synthesized new series of (5-aryl-1,3,4-oxadiazol-2-yl)(pyridin-2-yl)methanol derivatives (4a-4d) in fairly high yields. Here, we evaluated the antimicrobial activity of these derivatives against the following microorganisms: Staphylococcus epidermidis ATCC14990, Bacillus cereus PTCC 1015 , Pseudomonas aeruginosa ATCC 27853, Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Candida tropicalis PTCC 5028and Candida albicansATCC10239. Materials and Method: The broth macrodilutionand well agar diffusion methods were used for determination of inhibition zoom(IZ) and minimum inhibitory concentration (MIC) during preliminary evaluation of antimicrobial activity. Results: All of the synthesized compounds exhibited promising antibacterial activity against Staphylococcus aureus and Staphylococcus epidermidis. Conclusions: In this study, data suggest that compound (4a-4d) is a potent antibacterial compound with excellent MICs and acceptable selectivity index against Staphylococcal infections.

  1. Selvakumar K, Anandarajagopal K, Rajamanickam V, Ajaykumar T V, Jesindha B. 5-(2-aminophenyl)-1,3,4-oxadiazole-2(3h)thionederivatives:synthesis,characterization and antimicrobial evaluation. Int. J. Pharm. Sci. Rev. Res.2011;6(1): 64-67
  2. Dalia H. S. Synthesis, Characterization, Anti-Bacterial and Anti-Fungal Activities of New Quinoxaline 1,4-di-N-Oxide Derivatives. Int. J. Org. Chem. 2013; 3: 65-72
  3. Asif H, Moham A. Synthesis of novel 1,3,4-oxadiazole derivatives and their biological properties. Acta Pharm. 2009; 59: 223?233
  4. Ali, A., Mousavi, Z., Tajik, M., Assarzadeh, MJ.,Shafiee, A., (2014). Synthesis, analgesic and anti inflammatory activities of new methylimidazolyl-1,3,4-oxadiazoles and 1,2,4-triazoles. Daru. 2014; 22 (1): 22-34
  5. Tashfeen A, Shahid H, Najim A, Roberta L, Paolo L.C. In vitro antitumor and antiviral activities of new benzothiazole and 1,3,4-oxadiazole-2-thione derivatives. Acta Pharm. 2008; 58: 135?149
  6. Sanmati K. J, Arvind K. Y, Pragya N. 3D QSAR Analysis on Oxadiazole Derivatives as Anticancer Agents. Int. J. Pharm. Sci. Drug Res. 2011; 3(3): 230-235
  7. Rakesh S, Anuja Ch. various approaches for synthesis of 1,3,4-oxadiazole derivatives and their pharmacological activity. World J. Pharm. Pharm. Sci.. 2014; 3(10): 1474-1505
  8. Mohammad S.Y and Mohammad W.A. Synthesis And Anticonvulsant Activity Of Substituted Oxadiazole And Thiadiazole Derivatives. ActaPoloniaePharmaceutica. 2009; 66 (4): 393-397
  9. NouraddinH,SoodehS,Mohamad D, Mohammad H, Mehdi Khans et all. Synthesis and Antidiabetic Evaluation of Benzenesulfonamide Derivatives. Iran. J. Pharm. Res. 2013, 12 (2): 325-330
  10. Soltis MJ, Yeh HJ, Cole KA, Whittaker N, Wersto RP, Kohn EC. Identification and characterization of human metabolites of CAI [5-amino-1-1(4\'-chlorobenzoyl- 3,5dichlorobenzyl)-1,2,3-triazole- 4-carboxamide). Drug MetabDispos. 1996; 24(7):799-806
  11. Vincenzo S, AlessiaP,FabioB,BenedettaC,Monica D and et al. Discovery of Raltegravir, a Potent, Selective Orally Bioavailable HIV-Integrase Inhibitor for theTreatment of HIV-AIDS Infection. Med. Chem. 2008; 51: 5843?5855
  12. Chama Sh and Sanchit S. Biologically Active Oxadiazo. Asian J.Res.Pharm.Sci. 2015; 5(4): 227-233
  13. Mohammad A,Taqi A. Kh,Meraj A Kh. 1,2,4-oxadiazole nucleus with versatile
  14. biological applications. IJPSR. 2014; 5(07): 303-316
  15. Catalin V. M, Elena F, Peter G. J, HeikoF,Gerhard K, Heiner F and et al. Synthesis and characterization of novel bioactive1,2,4-oxadiazole natural product analogsbearing the N-phenylmaleimide? and N-phenylsuccinimide moieties. Beilstein J. Org. Chem.2013;9:2202?2215
  16. Ming-Xia S, Chang-Ji Z, Xian-Qing D, Zhi-Yu W and Hu-Ri P. The Synthesis and Anti-Bacterial Activities of N -carboxymethylRhodanines. 2014; Med chem. 2014; 4(5): 441-448
  17. Ali S. Efficient one-pot three-component reaction for the synthesis of (5-aryl-1,3,4-oxadiazol-2-yl)(pyridin-2-yl)methanol derivatives. Chem. Res.. 2015; 39:177?179
  18. Maryam K, NimaH.j, Ali S, Minoo Z and Narges D. Green synthesis and preliminary pharmacological evaluation of three-substituted thiazide derivatives as antibacterial agents.JCPR. 2015; 8(5): 149-154
  19. Fatemeh K, Ali S and Nima H.J. One-pot synthesis of 2-aryl-1,3,4-oxadiazole derivatives as potential antibacterial agents. JCPR. 2015; 7(10): 1028-1033
  20. Maryam K, NimaH.j, Ali S, Minoo Z and Narges D. Solvent free synthesis of alkyl 2-(dialkylamino)-phenylthiazole-5carboxylates derivatives and in vitro antimycobacterial activity of these compounds against Mycobacterium smegmatis. JCPR. 2015; 7(7): 338-345
  21. Chenielle D, Lois R, Alison N, Sylvia M, John L, Mohammed A. Antibacterial and antifungal analysis of crude extracts from the leaves of Callistemon viminalis. Journal of medical and pharmaceutical science.2009; 3(1): 1-7.
  22. FereshtehS,Akbar S. A,Saman S, Reza Z, Javad A.K, Kiarash G. Antibacterial activity
  23. Of Glycyrrhizaglabra against oral pathogens:aninvitro. Avicenna J. Phytomed. 2012; 2(3): 118-124
  24. Moses I, MaduagwuU,Osazuwa E. Evaluation of the Antifungal Activity of Aqueous and Alcoholic Extracts of Six Spices. Am. J. Plant Sci. 2016; 7:118-125
  25. Mohitosh Bi, MdAjijur R, Hajerakhand Anwar U. In vitro Antibacterial and Cytotoxic
  26. Activities of Two Compounds Isolated from Streptomyces sp. MBS. Bangladesh Pharm. J. 2012; 15 (1): 13-16
  27. Ali A, Aicha H, Said G, Radouane M, BouchraCh and Lalla I. Reveal antifungal activities of essential oils from LavanduladentataL. a way of valuing the arganeraie. Pharma Chem. 2016; 8(3):249-253
  28. Samija M, Kemal D, Elma V, AMAR O, D?enita S, Davorka synthesis of biscoumarin derivatives as antimicrobial agents. Asian J Pharm Clin Res. 2013; 6(3): 132-134.

[Maryam Kouhkan, Fatemeh Karimi, Ali Souldozi and Jalil Rashedi. (2017); IN VITRO ANTIMICROBIAL ACTIVITY OF NEW SUBSTITUTED 1,3,4-OXADIAZOLE DERIVATIVES. Int. J. of Adv. Res. 5 (May). 1468-1474] (ISSN 2320-5407). www.journalijar.com

Ali Souldozi
Faculty of science, Urmia Branch, Islamic Azad University, Urmia, Iran

DOI:

Article DOI: 10.21474/IJAR01/4269      
DOI URL: https://dx.doi.org/10.21474/IJAR01/4269

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