In vitro antileishmanial activity and selectivity profile of quinazolinone derivatives against Leishmania major

Baycan Mor

In vitro antileishmanial activity and selectivity profile of quinazolinone derivatives against Leishmania major

Abstract

Aims: This study aimed to evaluate the in vitro antileishmanial activity of five quinazolinone derivatives against Leishmania major (L. major) promastigotes and to determine their cytotoxicity toward human umbilical vein endothelial cells (HUVECs) and corresponding selectivity indices (SI). Methods: The quinazolinone derivatives (K1–K5) were tested against logarithmic-phase L. major promastigotes over a concentration range of 3.125–200 µM, with miltefosine used as the reference drug. Antileishmanial activity was assessed after 24 h using the cell viability detection kit-8 (CVDK-8). Cytotoxicity was evaluated in HUVECs, and half-maximal inhibitory concentration (IC50) values were determined by nonlinear regression. SI was calculated as the ratio of the HUVEC IC50 to the L. major IC50. Results: All five quinazolinone derivatives exhibited concentration-dependent antileishmanial activity against L. major, with IC50 values ranging from 29.66 to 41.11 µM. Their HUVEC IC50 values ranged from 69.73 to 91.53 µM. Miltefosine showed greater antileishmanial activity (IC50=21.54 µM) but higher cytotoxicity toward HUVECs (IC50=9.93 µM). Accordingly, K1–K5 showed SI values ranging from 2.15 to 2.38, whereas the SI of miltefosine was 0.46. Conclusion: The five quinazolinone derivatives exhibited in vitro antileishmanial activity against L. major promastigotes and higher SI values than miltefosine under the present experimental conditions. However, the SI values of 2.15–2.38 indicate modest selectivity and should be interpreted cautiously. Further evaluation in intracellular amastigote models is required to determine whether the observed antileishmanial activity is maintained in a host-cell-associated system.

Keywords

Ethical Statement

This study was conducted entirely in vitro using commercially obtained HUVEC cells and laboratory-cultured Leishmania major promastigotes. No human participants, human-derived samples collected specifically for this study, or experimental animals were used. Therefore, ethics committee approval and informed consent were not required.

Thanks

The author would like to thank Prof. Dr. Ahmet Özbilgin and Assoc. Prof. Dr. Feyzi Sinan Tokalı for their contributions to the study.

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Details

Primary Language

English

Subjects

Medical Parasitology

Journal Section

Research Article

Authors

Baycan Mor ^*
0000-0001-9480-3143
Türkiye

Publication Date

October 25, 2026

Submission Date

August 25, 2026

Acceptance Date

October 24, 2026

Published in Issue

Year 2026 Volume: 7 Number: 5

IZ

https://izlik.org/JA82UJ84JF

Cite

RIS / Bibtex

APA

Mor, B. (2026). In vitro antileishmanial activity and selectivity profile of quinazolinone derivatives against Leishmania major. Journal of Medicine and Palliative Care, 7(5), 1205-1210. https://izlik.org/JA82UJ84JF

AMA

1.Mor B. In vitro antileishmanial activity and selectivity profile of quinazolinone derivatives against Leishmania major. J Med Palliat Care / JOMPAC / jompac. 2026;7(5):1205-1210. https://izlik.org/JA82UJ84JF

Chicago

Mor, Baycan. 2026. “In Vitro Antileishmanial Activity and Selectivity Profile of Quinazolinone Derivatives Against Leishmania Major”. Journal of Medicine and Palliative Care 7 (5): 1205-10. https://izlik.org/JA82UJ84JF.

EndNote

Mor B (October 1, 2026) In vitro antileishmanial activity and selectivity profile of quinazolinone derivatives against Leishmania major. Journal of Medicine and Palliative Care 7 5 1205–1210.

IEEE

[1]B. Mor, “In vitro antileishmanial activity and selectivity profile of quinazolinone derivatives against Leishmania major”, J Med Palliat Care / JOMPAC / jompac, vol. 7, no. 5, pp. 1205–1210, Oct. 2026, [Online]. Available: https://izlik.org/JA82UJ84JF

ISNAD

Mor, Baycan. “In Vitro Antileishmanial Activity and Selectivity Profile of Quinazolinone Derivatives Against Leishmania Major”. Journal of Medicine and Palliative Care 7/5 (October 1, 2026): 1205-1210. https://izlik.org/JA82UJ84JF.

JAMA

1.Mor B. In vitro antileishmanial activity and selectivity profile of quinazolinone derivatives against Leishmania major. J Med Palliat Care / JOMPAC / jompac. 2026;7:1205–1210.

MLA

Mor, Baycan. “In Vitro Antileishmanial Activity and Selectivity Profile of Quinazolinone Derivatives Against Leishmania Major”. Journal of Medicine and Palliative Care, vol. 7, no. 5, Oct. 2026, pp. 1205-10, https://izlik.org/JA82UJ84JF.

Vancouver

1.Baycan Mor. In vitro antileishmanial activity and selectivity profile of quinazolinone derivatives against Leishmania major. J Med Palliat Care / JOMPAC / jompac [Internet]. 2026 Oct. 1;7(5):1205-10. Available from: https://izlik.org/JA82UJ84JF