22Jan 2018

SYNTHESIS AND BIOLOGICAL ACTIVITIES OF 1, 3, 4-OXADIAZOLE DERIVATIVES: A REVIEW OF LITERATURE.

  • Department of Pharmaceutical Chemistry, National College of Pharmacy, Manassery, Mukkam, Kozhikode 673602.
Crossref Cited-by Linking logo
  • Abstract
  • Keywords
  • References
  • Cite This Article as
  • Corresponding Author

A series of derivatives of 1, 3, 4-oxadiazole having verities of biological activities can be synthesised by various methods. The activities include anticancer, antimicrobial, anti- inflammatory, anti- HIV, anti tubercular, anti diabetic, antifungal etc. In this article we have summarized various methods for synthesis of derivatives of 1, 3, 4-oxadiazole nucleus and evaluation of various biological activities.

  1. Ahsan MJ, Samy JG, Khalilullah H, Nomani MS, Saraswat P, Gaur R, Singh A. Molecular properties prediction and synthesis of novel 1, 3, 4-oxadiazole analogues as potent antimicrobial and antitubercular agents. Bioorganic & medicinal chemistry letters. 2011 Dec 15;21(24):7246-50.
  2. Desai NC, Dodiya AM, Rajpara KM, Rupala YM. Synthesis and antimicrobial screening of 1, 3, 4-oxadiazole and clubbed thiophene derivatives. Journal of Saudi Chemical Society. 2014 Jul 31;18(3):255-61.
  3. El-Din MM, El-Gamal MI, Abdel-Maksoud MS, Yoo KH, Oh CH. Synthesis and in vitro antiproliferative activity of new 1, 3, 4-oxadiazole derivatives possessing sulfonamide moiety. European journal of medicinal chemistry. 2015 Jan 27;90:45-52.
  4. Gudipati R, Anreddy RN, Manda S. Synthesis, characterization and anticancer activity of certain 3-{4-(5-mercapto-1, 3, 4-oxadiazole-2-yl) phenylimino} indolin-2-one derivatives. Saudi Pharmaceutical Journal. 2011 Jul 31;19(3):153-8.
  5. Kavitha S, Kannan K, Gnanavel S. Synthesis, characterization and biological evaluation of novel 2, 5 substituted-1, 3, 4 oxadiazole derivatives. Saudi Pharmaceutical Journal. 2017 Mar 31;25(3):337-45.
  6. Khan KM, Ashraf M, Ahmad I, Ejaz SA. Synthesis, characterization and biological screening of 5-substituted-1, 3, 4-oxadiazole-2yl-N-(2-methoxy-5-chlorophenyl)-2-sulfanyl acetamide. Pak. J. Pharm. Sci. 2013 Mar;26(2):345-52.
  7. Kotaiah Y, Harikrishna N, Nagaraju K, Rao CV. Synthesis and antioxidant activity of 1, 3, 4-oxadiazole tagged thieno [2, 3-d] pyrimidine derivatives. European Journal of Medicinal Chemistry. 2012 Dec 31;58:340-5.
  8. Kumar KA, Jayaroopa P, Kumar GV. Comprehensive review on the chemistry of 1, 3, 4-oxadiazoles and their applications. International Journal of ChemTech Research. 2012;4(4):1782-91.
  9. Lai H, Dou D, Aravapalli S, Teramoto T, Lushington GH, Mwania TM, Alliston KR, Eichhorn DM, Padmanabhan R, Groutas WC. Design, synthesis and characterization of novel 1, 2-benzisothiazol-3 (2H)-one and 1, 3, 4-oxadiazole hybrid derivatives: potent inhibitors of Dengue and West Nile virus NS2B/NS3 proteases. Bioorganic & medicinal chemistry. 2013 Jan 1;21(1):102-13.
  10. Modi V, Modi P. Oxadiazole: Synthesis, characterization and biological activities. Journal of Saudi Chemical Society. 2012 Jul 31;16(3):327-32.
  11. Ningaiah S, Bhadraiah UK, Doddaramappa SD, Keshavamurthy S, Javarasetty C. Novel pyrazole integrated 1, 3, 4-oxadiazoles: Synthesis, characterization and antimicrobial evaluation. Bioorganic & medicinal chemistry letters. 2014 Jan 1;24(1):245-8.
  12. Puthiyapurayil P, Poojary B, Chikkanna C, Buridipad SK. Design, synthesis and biological evaluation of a novel series of 1, 3, 4-oxadiazole bearing N-methyl-4-(trifluoromethyl) phenyl pyrazole moiety as cytotoxic agents. European journal of medicinal chemistry. 2012 Jul 31;53:203-10.
  13. Qi DQ, Yu CM, You JZ, Yang GH, Wang XJ, Zhang YP. Synthesis, crystal structures, fluorescence and xanthine oxidase inhibitory activity of pyrazole-based 1, 3, 4-oxadiazole derivatives. Journal of Molecular Structure. 2015 Nov 15;1100:421-8.
  14. Ramazani A, Ahmadi Y, Mahyari A. One-pot efficient synthesis of fully substituted 1, 3, 4-oxadiazole derivatives from (N-isocyanimino) triphenylphosphorane, carboxylic acids, and aromatic bis-aldehydes. Synthetic Communications. 2011 Aug 1;41(15):2273-82.
  15. Rane RA, Bangalore P, Borhade SD, Khandare PK. Synthesis and evaluation of novel 4-nitropyrrole-based 1, 3, 4-oxadiazole derivatives as antimicrobial and anti-tubercular agents. European journal of medicinal chemistry. 2013 Dec 31;70:49-58.
  16. Raval JP, Akhaja TN, Jaspara DM, Myangar KN, Patel NH. Synthesis and in vitro antibacterial activity of new oxoethylthio-1, 3, 4-oxadiazole derivatives. Journal of Saudi Chemical Society. 2014 Apr 30;18(2):101-6.
  17. Roy PP, Bajaj S, Maity TK, Singh J. Synthesis and Evaluation of Anticancer Activity of 1, 3, 4-Oxadiazole Derivatives against Ehrlich Ascites Carcinoma Bearing Mice and Their Correlation with Histopathology of Liver. receptor. 2017 Apr 1;15:16.
  18. Singh AK, Lohani M, Parthsarthy R. Synthesis, characterization and anti-inflammatory activity of some 1, 3, 4-oxadiazole derivatives. Iranian journal of pharmaceutical research: IJPR. 2013;12(2):319.
  19. Sun J, Zhu H, Yang ZM, Zhu HL. Synthesis, molecular modeling and biological evaluation of 2-aminomethyl-5-(quinolin-2-yl)-1, 3, 4-oxadiazole-2 (3H)-thione quinolone derivatives as novel anticancer agent. European journal of medicinal chemistry. 2013 Feb 28;60:23-8.
  20. Tabatabai SA, Lashkari SB, Zarrindast MR, Gholibeikian M, Shafiee A. Design, synthesis and anticonvulsant activity of 2-(2-phenoxy) phenyl-1, 3, 4-oxadiazole derivatives. Iranian journal of pharmaceutical research: IJPR. 2013;12(Suppl):105.
  21. Valente S, Trisciuoglio D, De Luca T, Nebbioso A, Labella D, Lenoci A, Bigogno C, Dondio G, Miceli M, Brosch G, Del Bufalo D. 1, 3, 4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells. Journal of medicinal chemistry. 2014 Jul 8;57(14):6259-65.
  22. Xu WM, Han FF, He M, Hu DY, He J, Yang S, Song BA. Inhibition of tobacco bacterial wilt with sulfone derivatives containing an 1, 3, 4-oxadiazole moiety. Journal of agricultural and food chemistry. 2012 Jan 19;60(4):1036-41.
  23. Zhang XM, Qiu M, Sun J, Zhang YB, Yang YS, Wang XL, Tang JF, Zhu HL. Synthesis, biological evaluation, and molecular docking studies of 1, 3, 4-oxadiazole derivatives possessing 1, 4-benzodioxan moiety as potential anticancer agents. Bioorganic & medicinal chemistry. 2011 Nov 1;19(21):6518-24.

[Baijika P, Akash Marathakam, Midhula C C and Shadiha Saheed K. (2018); SYNTHESIS AND BIOLOGICAL ACTIVITIES OF 1, 3, 4-OXADIAZOLE DERIVATIVES: A REVIEW OF LITERATURE. Int. J. of Adv. Res. 6 (Jan). 1114-1122] (ISSN 2320-5407). www.journalijar.com

Baijika P
Department of pharmaceutical chemistry, National College of Pharmacy, Manassery, Mukkam, Kozhikode

DOI:

Article DOI: 10.21474/IJAR01/6328      
DOI URL: https://dx.doi.org/10.21474/IJAR01/6328

Download Full Paper

Download PDF No. of Downloads: 587 | No. of Views: 1183