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Abstract

Synthesis and Antimicrobial Activity Evaluation of New Benzimidazole—Thiazole Derivatives †

by
Zafer Asim Kaplancikli
1,*,
Serkan Levent
1,2,
Derya Osmaniye
1,2 and
Yusuf Özkay
1,2
1
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey
2
Doping and Narcotic Compounds Analysis Laboratory, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey
*
Author to whom correspondence should be addressed.
†
Presented at the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain, 8 September 2017.
Proceedings 2017, 1(6), 658; https://doi.org/10.3390/proceedings1060658
Published: 19 October 2017
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
Versions Notes
Antibiotic resistance which was expedited by the use of antimicrobial drugs has been a significant global challenge for public health [1]. In addition to this, candidiasis is the most common fungal infection worldwide, causing important morbidity and mortality, especially in immunocompromised patients [2].
A literature survey has uncovered that the various derivatives of benzimidazole have been synthesized for their pharmalogical activities and many of them supported the finding that benzimidazole derivatives are potent against various microorganism strains [3]. On the other hand, benzimidazoles are a class of synthetic remedial agents; for example, chlormidazole and carbendazim are used with a view to curing patients infected with fungus species.
The compounds that include thiazole on the same structure have significant antimicrobial activity; Sulfathiazole, which is an antimicrobial drug, includes a thiazole moiety [4].
From this point of view, in the present study, new Benzimidazole-thiazole derivatives were synthesized. The structures of the synthesized compounds were elucidated using FT-IR, 1H-NMR, 13C-NMR, and HRMS spectral data. The synthesized compounds were screened for in vitro antimicrobial activity against pathogenic strains bacteria and candida. The effects of the selected compounds against ergosterol biosynthesis were observed by the LC-MS-MS method, which is based on quantification of the ergosterol level in C. albicans.

Author Contributions

Y.Ö., Z.A.K. conceived and designed the experiments; D.O. performed the synthesis; S.L. performed analysis studies; Y.Ö., S.I, D.O. and Z.A.K. wrote the paper. All authors have read and agreed to the published version of the manuscript.

Acknowledgments

This study was financially supported by Anadolu University Scientific Projects Fund, Project No.: 1705S312.

Conflicts of Interest

The authors declare no conflict of interest.

References

  1. Zhang, H.Z.; He, S.C.; Peng, Y.J.; Zhang, H.J.; Gopala, L.; Reddy Tangadanchu, V.K.; Gan, L.L.; Zhou, C.H. Design, synthesis and antimicrobial evaluation of novel benzimidazole-incorporated sulfonamide analogues. Eur. J. Med. Chem. 2017, 136, 165–183. [Google Scholar] [CrossRef] [PubMed]
  2. Tang, H.; Wub, J.; Zhang, W.; Zhao, L.; Zhang, Y.H.; Shen, C.W. Design, Synthesis and Biological Evaluation of Novel Non-Azole Derivatives as Potential Antifungal Agents. Chin. Chem. Lett. 2015, 26, 1161–1164. [Google Scholar] [CrossRef]
  3. Salahuddin Shaharyar, M.; Mazumder, A. Benzimidazoles: A biologically active compounds. Arab. J. Chem. 2017, 10, 157–173. [Google Scholar] [CrossRef]
  4. Ayati, A.; Emami, S.; Asadipour, A.; Shafiee, A.; Foroumadi, A. Recent applications of 1,3-thiazole core structure in the identification of new lead compounds and drug discovery. Eur. J. Med. Chem. 2015, 97, 699–718. [Google Scholar] [CrossRef] [PubMed]
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MDPI and ACS Style

Kaplancikli, Z.A.; Levent, S.; Osmaniye, D.; Özkay, Y. Synthesis and Antimicrobial Activity Evaluation of New Benzimidazole—Thiazole Derivatives. Proceedings 2017, 1, 658. https://doi.org/10.3390/proceedings1060658

AMA Style

Kaplancikli ZA, Levent S, Osmaniye D, Özkay Y. Synthesis and Antimicrobial Activity Evaluation of New Benzimidazole—Thiazole Derivatives. Proceedings. 2017; 1(6):658. https://doi.org/10.3390/proceedings1060658

Chicago/Turabian Style

Kaplancikli, Zafer Asim, Serkan Levent, Derya Osmaniye, and Yusuf Özkay. 2017. "Synthesis and Antimicrobial Activity Evaluation of New Benzimidazole—Thiazole Derivatives" Proceedings 1, no. 6: 658. https://doi.org/10.3390/proceedings1060658

APA Style

Kaplancikli, Z. A., Levent, S., Osmaniye, D., & Özkay, Y. (2017). Synthesis and Antimicrobial Activity Evaluation of New Benzimidazole—Thiazole Derivatives. Proceedings, 1(6), 658. https://doi.org/10.3390/proceedings1060658

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