Design and Synthesis of New Coumarin-Bistriazole Hybrids as Potenial Drug Candidates

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Arvas B., Yolaçan Ç., Aydoğan F.

8th International Bahçeşehir University (BAU) Drug Design Congress, İstanbul, Turkey, 15 - 17 December 2022, pp.1

  • Publication Type: Conference Paper / Summary Text
  • City: İstanbul
  • Country: Turkey
  • Page Numbers: pp.1
  • Yıldız Technical University Affiliated: Yes


Design and Synthesis of New Coumarin-Bistriazole Hybrids as Potential Drug Candidates


Coumarin derivatives are natural or synthetic heterocyclic molecules with oxygen. They are considered as pharmacological flavonoids. Coumarin derivatives have attracted researchers’ attention due to their wide range of biological activity such as antitumor, anticoagulant, antioxidant, antiviral, antiinflamatory, antimicrobial, antibacterial, etc  [1,2].

Triazoles can be used as binders on the peptides or aromatic rings  and may exert bioisosteric effects. They can bind to a biological target with a high affinity by hydrogen bonding, dipole-dipole and π-stacking interactions. This demonstrates the unquestionable importance of triazoles in pharmaceutical chemistry [3].

Recently, medicinal chemists have focused on combination of two or more pharmacophores in one molecule to produce an hybrid molecule. These hybrid molecules can show enhanced or even new biological activities.


After the synthesis of the coumarin skeleton, alkylation reactions on the 5- and 7-positions of the coumarin skeleton were performed. Then, the synthesis of azide derivatives was carried out by the reaction of obtained alkylation products with NaN3. Finally, 1,2,3-triazole ring was obtained by click reaction of synthesized azide derivatives and dipolarophils.

Result and Discussion:

Coumarin ring formation and alkylation reactions were performed by well known and easily applicable methods. To construct the 1,2,3-trizole rings, click reactions were accomplished under mild conditions in good yields. The structures of all new coumarin-bistrizole hybrides were confirmed by their spectral data.


In conclusion, a serie of new coumarin-bistriazole derivatives with the potential to display a variety of biological activities have been designed and synthesized.  

Keywords: Coumarin, triazole, biological activity, heterocyclic compound, organic synthesis

This work was supported by Yildiz Technical University Scientific Research Foundation [project number FDK-2021-4263].


 [1] O. Kayser, H. Kolodziej, Antibacterial Activity of Simple Coumarins: Structural Requirements for Biological Activity, Z. Naturforsch. 1999, 54c, 169-174.

[2] L.Wu, X. Wang, W. Xu, F. Farzaneh, R. Xu, The structure and pharmacological functions of coumarins and their derivatives, Cur. Med. Chem. 2009, 16, 4236-4260. 

[3] Dheer, D., Singh, V., &Shankar, R. (2017). ‘‘Medicinal attributes of 1, 2, 3-triazoles: Current developments’’, Bioorganic Chemistry, 71, 30-54.