The synthesis, antifungal and apoptotic effects of triazole-oxadiazoles against Candida species.

Eur J Med Chem

Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Anadolu University, Eskisehir, Turkey.

Published: January 2018

In search of potent and safe antifungal agents, herein, we report the synthesis, characterization and biological activities of triazole-oxadiazole compounds. The structural verification of the molecules was carried out by H NMR, C NMR and mass spectral data. The in vitro antifungal and apoptotic activity were investigated against C. albicans, C. parapsilosis, C. krusei and C. glabrata. The compounds namely N-(4-nitrophenyl)-2-[(5-(2-((4-methyl-4H-1,2,4-triazol-3-yl)thio)ethyl)-1,3,4-oxadiazol-2-yl)thio]acetamide (4e) and N-(6-fluorobenzothiazol-2-yl)-2-[(5-(2-((4-methyl-4H-1,2,4-triazol-3-yl)thio)ethyl)-1,3,4-oxadiazol-2-yl)thio]acetamide (4i) were detected as the most potent compounds against C. albicans and C. glabrata (MIC = 62.5 μg/mL). According to studies on their mechanism of action, it was confirmed that compound 4i has apoptotic effect on four Candida via Annexin V-PI with flow cytometry. The MTT assay revealed that all compounds were determined to be non-toxic against healthy cells in the tested concentrations.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejmech.2017.12.020DOI Listing

Publication Analysis

Top Keywords

antifungal apoptotic
8
synthesis antifungal
4
apoptotic effects
4
effects triazole-oxadiazoles
4
triazole-oxadiazoles candida
4
candida species
4
species search
4
search potent
4
potent safe
4
safe antifungal
4

Similar Publications

Background: Acute myeloid leukemia (AML) is a heterogeneous hematological malignancy caused by disorders in stem cell differentiation and excessive proliferation resulting in clonal expansion of dysfunctional cells called myeloid blasts. The combination of chemotherapeutic agents with natural product-based molecules is promising in the treatment of AML. In this study, we aim to investigate the anti-cancer effect of Rapamycin and Niacin combination on THP-1 and NB4 AML cell lines.

View Article and Find Full Text PDF

Microbial exopolysaccharides (EPSs) possess valuable biological functions and fascinating physicochemical properties. On the other hand, lung cancer is the primary contributor to global cancer-related deaths. However, health and safety concerns have prevented the identification and approval of any medications, including chemotherapeutic agents, for lung cancer treatment to date.

View Article and Find Full Text PDF
Article Synopsis
  • The study examined how low dose cyclosporin A (CsA) can protect rat kidneys from damage caused by ischemia-reperfusion (IR) injury, focusing on mechanisms of cell death.
  • Three groups were tested: a control group, an IR group (exposed to restricted blood flow), and an IR + CsA group (received CsA before the IR procedure).
  • Results showed that CsA significantly improved kidney function and reduced injury markers compared to the IR group, indicating its protective effects against IR-related kidney damage.
View Article and Find Full Text PDF

Objective: Breast cancer represents the most prevalent type of tumor throughout the world. Considering the side effects caused by the available treatments, the resistance acquired by cells to cytotoxic agents, and metastasis, it is necessary to search for new sources of antitumor and antimetastatic therapies. Given the numerous antitumor studies involving the synthesis of substances derived from the naphthoquinone lapachol, we investigated the antineoplastic potential of a new synthetic substance (APO-3) derived from lapachol, alone and in combination with the chemotherapeutic agent paclitaxel (PTX), against 4T1 cells, a murine breast cancer cell line.

View Article and Find Full Text PDF

Sclareolide as Antifungal Strategy Against : Unveiling Its Mechanisms of Action.

Microorganisms

November 2024

Department of Biosciences and Oral Diagnosis, Institute of Science and Technology, Sao Paulo State University (UNESP), Sao Jose dos Campos, São Paulo 12245-000, Brazil.

Cryptococcal infection commonly begins as an opportunistic infection in humans, however, this can escalate to a systemic or life-threatening form in immunocompromised individuals. Here, we aim to identify novel antifungal molecules from plants resources. Sclareolide, a phytochemical classified as a sesquiterpene lactone, was assessed against H99.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!