Synthesis, biological activity evaluation and molecular docking studies of novel thiazole derivatives

Derya Osmaniye; Uğur Kayiş; Ülküye Dudu Gül; Yusuf Özkay; Zafer Asım Kaplancıklı

Article Details

Synthesis, biological activity evaluation and molecular docking studies of novel thiazole derivatives

Authors:

Derya Osmaniye | Uğur Kayiş | Ülküye Dudu Gül | Yusuf Özkay | Zafer Asım Kaplancıklı

Publisher:

Anadolu University

Main Topics:

Pharmacology and Pharmaceutical Sciences

Journal:

European Journal of Life Sciences Vol.2 Issue 1, pp.1-24

Document Type:

Article

Publication Date:

4/2023

Document Language:

English

Document ID (Org No.):

2001288262

pISSN:

2822-5333

Keywords:

Abstract:

 Resistance to existing drugs develops because of insensible use of antibacterial and antifungal drugs. Therefore, there is a need for the development of new drug candidate compounds. The thiazole ring has many biological activities. It is possible to include antibacterial and antifungal activities among these activities. In addition to these, the thiazole ring has been preferred because it is the bioisostere of the imidazole ring in the structure of many antifungal drugs. For this purpose, within the scope of this study, 7 new thiazole compounds were synthesized, and their structure determinations were carried out using HRMS, 1H-NMR, 13C-NMR spectroscopic methods. Their antibacterial and antifungal activities were investigated by in vitro methods. As a result of activity tests, compound 3e showed activity against C.krusei strain with MIC5031.25 ugmL. The potential effectiveness of the compound 3e on the 14alpha-demethylase enzyme PDB ID:3LD6 was tested by in silico studies.

 Resistance to existing drugs develops because of insensible use of antibacterial and antifungal drugs. Therefore, there is a need for the development of new drug candidate compounds. The thiazole ring has many biological activities. It is possible to include antibacterial and antifungal activities among these activities. In addition to these, the thiazole ring has been preferred because it is the bioisostere of the imidazole ring in the structure of many antifungal drugs. For this purpose, within the scope of this study, 7 new thiazole compounds were synthesized, and their structure determinations were carried out using HRMS, 1H-NMR, 13C-NMR spectroscopic methods. Their antibacterial and antifungal activities were investigated by in vitro methods. As a result of activity tests, compound 3e showed activity against C.krusei strain with MIC5031.25 ugmL. The potential effectiveness of the compound 3e on the 14alpha-demethylase enzyme PDB ID:3LD6 was tested by in silico studies.

 Resistance to existing drugs develops because of insensible use of antibacterial and antifungal drugs. Therefore, there is a need for the development of new drug candidate compounds. The thiazole ring has many biological activities. It is possible to include antibacterial and antifungal activities among these activities. In addition to these, the thiazole ring has been preferred because it is the bioisostere of the imidazole ring in the structure of many antifungal drugs. For this purpose, within the scope of this study, 7 new thiazole compounds were synthesized, and their structure determinations were carried out using HRMS, 1H-NMR, 13C-NMR spectroscopic methods. Their antibacterial and antifungal activities were investigated by in vitro methods. As a result of activity tests, compound 3e showed activity against C.krusei strain with MIC5031.25 ugmL. The potential effectiveness of the compound 3e on the 14alpha-demethylase enzyme PDB ID:3LD6 was tested by in silico studies.

 Resistance to existing drugs develops because of insensible use of antibacterial and antifungal drugs. Therefore, there is a need for the development of new drug candidate compounds. The thiazole ring has many biological activities. It is possible to include antibacterial and antifungal activities among these activities. In addition to these, the thiazole ring has been preferred because it is the bioisostere of the imidazole ring in the structure of many antifungal drugs. For this purpose, within the scope of this study, 7 new thiazole compounds were synthesized, and their structure determinations were carried out using HRMS, 1H-NMR, 13C-NMR spectroscopic methods. Their antibacterial and antifungal activities were investigated by in vitro methods. As a result of activity tests, compound 3e showed activity against C.krusei strain with MIC5031.25 ugmL. The potential effectiveness of the compound 3e on the 14alpha-demethylase enzyme PDB ID:3LD6 was tested by in silico studies.

Article Details

Synthesis, biological activity evaluation and molecular docking studies of novel thiazole derivatives

Authors:

Derya Osmaniye | Uğur Kayiş | Ülküye Dudu Gül | Yusuf Özkay | Zafer Asım Kaplancıklı

Publisher:

Anadolu University

Main Topics:

Pharmacology and Pharmaceutical Sciences

Journal:

European Journal of Life Sciences Vol.2 Issue 1, pp.1-24

Document Type:

Article

Publication Date:

4/2023

Document Language:

English

Document ID (Org No.):

2001288262

pISSN:

2822-5333

Thiazole

Antibacterial Activity

Antifungal Activity

Molecular Docking

Issues

Article Details

Synthesis, biological activity evaluation and molecular docking studies of novel thiazole derivatives

Authors: Derya Osmaniye | Uğur Kayiş | Ülküye Dudu Gül | Yusuf Özkay | Zafer Asım Kaplancıklı

Publisher: Anadolu University

Main Topics: Pharmacology and Pharmaceutical Sciences

Journal: European Journal of Life Sciences Vol.2 Issue 1, pp.1-24

Document Type: Article

Publication Date: 4/2023

Document Language: English

Document ID (Org No.): 2001288262

pISSN: 2822-5333

Thiazole

Antibacterial Activity

Antifungal Activity

Molecular Docking

Issues

Authors:

Derya Osmaniye | Uğur Kayiş | Ülküye Dudu Gül | Yusuf Özkay | Zafer Asım Kaplancıklı

Publisher:

Anadolu University

Main Topics:

Pharmacology and Pharmaceutical Sciences

Journal:

European Journal of Life Sciences Vol.2 Issue 1, pp.1-24

Document Type:

Article

Publication Date:

4/2023

Document Language:

English

Document ID (Org No.):

2001288262

pISSN:

2822-5333