Studies on a novel series of 3(2H)-pyridazinones: Synthesis, molecular modelling, antimicrobial activity

Zeynep Özdemir; Mehmet Abdullah Alagöz; Alp Giray Akdemir; Azime Berna Özçelik; Berrin Özçelik; Mehtap Uysal

Studies on a novel series of 3(2H)-pyridazinones: Synthesis, molecular modelling, antimicrobial activity

Abstract

Efforts to develop new potent and effective antimicrobial compounds with lower side effects are important not only for controlling serious infections but also for cancer, surgical operations, and preventing possible infections which are related to other threats. Therefore, it is getting more important to develop new antibacterial and antifungal compounds with wide spectrum, systemic effect and lower side effects. In this study eight new 3(2H)- pyridazinone derivatives were synthesized and their antimicrobial activities were evaluated by using broth microdilution method agains two Gr (+) (Staphylococcus aureus, Enterococcus faecalis), two Gr (-) bacteria (Pseudomonas aeruginosa, Escherichia coli) and three yeasts like fungi (Candida albicans, Candida krusei). Compound D2a had the best antibacterial activity among the synthesized compounds. All compounds were more effective against the fungus than the bacteria. In this study, we performed molecular modelling studies to provide in depth understanding of their CYP51 inhibition. Antifungal susceptibility tests against standard Candida spp. including C. albicans revealed D2aas highly active compound. The molecular docking studies showed similarities in binding interactions in active site gorges of the enzymes with known inhibitors, such as VT1, fluconazole.

Keywords

References

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Details

Primary Language

English

Subjects

Pharmaceutical Chemistry, Pharmaceutical Microbiology

Journal Section

Research Article

Authors

Zeynep Özdemir ^*
Türkiye

Mehmet Abdullah Alagöz
Türkiye

Alp Giray Akdemir This is me
Türkiye

Azime Berna Özçelik
Türkiye

Berrin Özçelik
Türkiye

Mehtap Uysal
Türkiye

Publication Date

June 27, 2025

Submission Date

February 1, 2019

Acceptance Date

August 2, 2019

Published in Issue

Year 2019 Volume: 23 Number: 5

IZ

https://izlik.org/JA33MD38NM

Cite

RIS / Bibtex

APA

Özdemir, Z., Alagöz, M. A., Akdemir, A. G., Özçelik, A. B., Özçelik, B., & Uysal, M. (2025). Studies on a novel series of 3(2H)-pyridazinones: Synthesis, molecular modelling, antimicrobial activity. Journal of Research in Pharmacy, 23(5), 960-972. https://izlik.org/JA33MD38NM

AMA

1.Özdemir Z, Alagöz MA, Akdemir AG, Özçelik AB, Özçelik B, Uysal M. Studies on a novel series of 3(2H)-pyridazinones: Synthesis, molecular modelling, antimicrobial activity. J. Res. Pharm. 2025;23(5):960-972. https://izlik.org/JA33MD38NM

Chicago

Özdemir, Zeynep, Mehmet Abdullah Alagöz, Alp Giray Akdemir, Azime Berna Özçelik, Berrin Özçelik, and Mehtap Uysal. 2025. “Studies on a Novel Series of 3(2H)-Pyridazinones: Synthesis, Molecular Modelling, Antimicrobial Activity”. Journal of Research in Pharmacy 23 (5): 960-72. https://izlik.org/JA33MD38NM.

EndNote

Özdemir Z, Alagöz MA, Akdemir AG, Özçelik AB, Özçelik B, Uysal M (July 1, 2025) Studies on a novel series of 3(2H)-pyridazinones: Synthesis, molecular modelling, antimicrobial activity. Journal of Research in Pharmacy 23 5 960–972.

IEEE

[1]Z. Özdemir, M. A. Alagöz, A. G. Akdemir, A. B. Özçelik, B. Özçelik, and M. Uysal, “Studies on a novel series of 3(2H)-pyridazinones: Synthesis, molecular modelling, antimicrobial activity”, J. Res. Pharm., vol. 23, no. 5, pp. 960–972, July 2025, [Online]. Available: https://izlik.org/JA33MD38NM

ISNAD

Özdemir, Zeynep - Alagöz, Mehmet Abdullah - Akdemir, Alp Giray - Özçelik, Azime Berna - Özçelik, Berrin - Uysal, Mehtap. “Studies on a Novel Series of 3(2H)-Pyridazinones: Synthesis, Molecular Modelling, Antimicrobial Activity”. Journal of Research in Pharmacy 23/5 (July 1, 2025): 960-972. https://izlik.org/JA33MD38NM.

JAMA

1.Özdemir Z, Alagöz MA, Akdemir AG, Özçelik AB, Özçelik B, Uysal M. Studies on a novel series of 3(2H)-pyridazinones: Synthesis, molecular modelling, antimicrobial activity. J. Res. Pharm. 2025;23:960–972.

MLA

Özdemir, Zeynep, et al. “Studies on a Novel Series of 3(2H)-Pyridazinones: Synthesis, Molecular Modelling, Antimicrobial Activity”. Journal of Research in Pharmacy, vol. 23, no. 5, July 2025, pp. 960-72, https://izlik.org/JA33MD38NM.

Vancouver

1.Zeynep Özdemir, Mehmet Abdullah Alagöz, Alp Giray Akdemir, Azime Berna Özçelik, Berrin Özçelik, Mehtap Uysal. Studies on a novel series of 3(2H)-pyridazinones: Synthesis, molecular modelling, antimicrobial activity. J. Res. Pharm. [Internet]. 2025 Jul. 1;23(5):960-72. Available from: https://izlik.org/JA33MD38NM