SavedAdd your journal

Journals / Iğdır Üniversitesi Fen Bilimleri Enstitüsü Dergisi / 2023 / Cilt: 13 - Sayı: 1

Synthesis of Some New 1,2,3-Triazole-Arylidenehydrazide Hybrid Compounds and Determination of Their Antimicrobial Activities

Bazı Yeni 1,2,3-Triazol-arilidenhidrazid Hibrit Bileşiklerinin Sentezi ve Anti-mikrobiyal Etkinliklerinin Belirlenmesi

Halil ŞENOL
Harika Öykü DİNÇ
Beyza Nur TAK
Pages
468–481
Publication Date
2023-03-01
DOI
—
🏛️Bibliographic metadata and full text access for this article are provided via DergiPark.
DergiPark Record ↗
✨

AI Summary & Key Takeaways

AI Insight
⚡ TL;DR(Too Long; Didn't Read)

The MIC values of the anti-fungal activities of the compounds were found as 62.5 μM, while the MIC values of the anti-bacterial activities were determined as 62.5-125 μM.

📌 3 Key Takeaways

🎯
Objective & Hypothesis:At the present time, due to the low bioavailability of many of the drugs used against cancer and other microorganisms and their side effects such as toxicity, there is a need for new drugs in the treatment.
📊
Key Findings & Data:In this study, 18 new 1,2,3-triazole/arylidenehydrazide hybrid compounds were synthesized.
💡
Conclusion & Impact:The MIC values of the anti-fungal activities of the compounds were found as 62.5 μM, while the MIC values of the anti-bacterial activities were determined as 62.5-125 μM.
🔬Design:Research Article
📍Scope:Comprehensive Sample
⚙️Variables:3-triazol · Hibrit bileşik · Arilidenhidrazid

Abstract

At the present time, due to the low bioavailability of many of the drugs used against cancer and other microorganisms and their side effects such as toxicity, there is a need for new drugs in the treatment. Although an increasing number of anticancer or antibiotic drugs are being developed every day, the low selectivity of these drugs and the acquisition of multidrug resistance prevent successful treatment. Therefore, there is a great need for the discovery of new, potent and selective agents to destroy or at least stop the proliferation of tumor cells or microorganisms. In this study, 18 new 1,2,3-triazole/arylidenehydrazide hybrid compounds were synthesized. Anti-microbial activities of these compounds (17a-r) were investigated on Staphylococcus Aureus and Escherichia coli and Candida albicans. The results were compared with the anti-microbial drug ceftazidime. The MIC values of the anti-fungal activities of the compounds were found as 62.5 μM, while the MIC values of the anti-bacterial activities were determined as 62.5-125 μM.

Özet

Günümüzde kansere ve diğer mikroorganizmalara karşı kullanılan ilaçların pek çoğunun biyoyararlanımının düşük olması ve başta toksisite gibi yan etkilerinden dolayı tedavide yeni ilaçların varlığına ihtiyaç duyulmaktadır. Her gün artan sayıda anti-kanser veya antibiyotik ilaç geliştirilmesine rağmen, bu ilaçların seçiciliklerinin düşük olması ve çoklu ilaç direncinin kazanılması, başarılı bir tedavinin önüne geçmektedir. Bu nedenle, tümör hücrelerini veya mikroorganizmaları yok etmek veya en azından çoğalmasını durdurmak için yeni, güçlü ve seçici ajanlarının keşfine önemli ölçüde ihtiyaç duyulmaktadır. Bu çalışma kapsamında 18 adet yeni 1,2,3-triazol/arilidenhidrazid yapısında hibrit bileşik sentezlendi. Elde edilen 18 yeni bileşiğin (17a-r) Staphylococcus Aureus ve Escheric1hia coli bakteri türleri ve Candida albicans mantar türü üzerindeki anti-mikrobiyal etkinlikleri araştırıldı. Elde edilen sonuçlar anti-mikrobiyal ilaç seftazidim ile karşılaştırıldı. Bileşiklerin anti fungal etkinliklerinin MİK değerleri 62.5 μM olarak bulunurken anti-bakteriyel etkinliklerinin MİK değerleri 62.5-125 μM olarak belirlendi.

🔖

Cite This Article

ŞENOL, H., DİNÇ, H. Ö., TAK, B. N. (2023). Synthesis of Some New 1,2,3-Triazole-Arylidenehydrazide Hybrid Compounds and Determination of Their Antimicrobial Activities. Iğdır Üniversitesi Fen Bilimleri Enstitüsü Dergisi, Cilt: 13 - Sayı: 1, 468–481. https://ajindex.com/articles/886425

📄 Full Text PDF Viewer

📄

PDF görüntüleyici hazırlanıyor...

References (11)

  1. Aparna, Y., Nirmala, G., Subhashini, N. J. P., Sharada, L. N. ve Sreekanth, S. (2020). Synthesis and Antimicrobial Activity of Novel Bis-1,2,3-triazol-1H-4-yl-substituted Aryl Benzimidazole-2-thiol Derivatives. Russian Journal of General Chemistry, 90 (8), 1501-1506.
  2. Bayrak, C., Senol, H., Sirtbasi, S., Sahin, E. ve Menzek, A. (2018). Synthesis and rearrangement reactions of 1,4-dihydrospiro[1,4-methanonaphthalene-9,1 '-cyclopropane] derivatives. Tetrahedron, 74 (40), 5839-5849.
  3. Cardoso, C. S., Silva, D. P. B., Silva, D. M., Fiorentino, I. F., Fajemiroye, J. O., Moreira, L. K. S., Vasconcelos, J. P., Sanz, G., Vaz, B. G., Liao, L. M., Lima, D. D., Dos Santos, F. C. A., Menegatti, R. ve Costa, E. A. (2020). Mechanisms involved in the antinociceptive and anti-inflammatory effects of a new triazole derivative: 5- 1-(4-fluorophenyl)-1H-1,2,3-triazol-4-yl -1H-tetrazole (LQFM-096). Inflammopharmacology, 28 (4), 877-892.
  4. Colin, S., Chinetti-Gbaguidi, G., Kuivenhoven, J. A. ve Staels, B. (2015). Emerging Small Molecule Drugs. High Density Lipoproteins: from Biological Understanding to Clinical Exploitation, 224, 617-630.
  5. Cramer, J., Schiebel, J., Wulsdorf, T., Grohe, K., Najbauer, E. E., Ehrmann, F. R., Radeva, N., Zitzer, N., Linne, U., Linser, R., Heine, A. ve Klebe, G. (2017). A False-Positive Screening Hit in Fragment-Based Lead Discovery: Watch out for the Red Herring. Angewandte Chemie-International Edition, 56 (7), 1908-1913.
  6. Davis, B. J. ve Roughley, S. D., 2017. Fragment-Based Lead Discovery. Annual Reports in Medicinal Chemistry, Vol 50: Platform Technologies in Drug Discovery and Validation ed., Ed: R.A. Goodnow. Annual Reports in Medicinal Chemistry, 371-439.
  7. De Fusco, C., Brear, P., Iegre, J., Georgiou, K. H., Sore, H. F., Hyvonen, M. ve Spring, D. R. (2017). A fragment-based approach leading to the discovery of a novel binding site and the selective CK2 inhibitor CAM4066. Bioorg Med Chem, 25 (13), 3471-3482.
  8. Dickson, M. ve Gagnon, J. P. (2004). Key factors in the rising cost of new drug discovery and development. Nature Reviews Drug Discovery, 3 (5), 417-429.
  9. Dimasi, J. A., Hansen, R. W. ve Grabowski, H. G. (2003). The price of innovation: new estimates of drug development costs. Journal of Health Economics, 22 (2), 151-185.
  10. Dogan, H. N., Rollas, S. ve Erdeniz, H. (1998). Synthesis, structure elucidation and antimicrobial activity of some 3-hydroxy-2-naphthoic acid hydrazide derivatives. Farmaco, 53 (7), 462-467.
  11. El-Sayed, H. A., Moustafa, A. H., Abd