Metal catalyst-free N-allylation/alkylation of imidazole and benzimidazole with Morita–Baylis–Hillman (MBH) alcohols and acetates

• Olfa Mhasni,
• Jalloul Bouajila and
• Farhat Rezgui

Beilstein J. Org. Chem. 2023, 19, 1251–1258, doi:10.3762/bjoc.19.93

• biological activities [1][2][3][4][5][6][7]. In this context, the imidazole moiety is widely known as one of the most important groups which plays efficient roles in bioactive compounds [8]. For instance, a number of N-substituted imidazole derivatives, such as miconazole, ketoconazole, genaconazole, and

Isolation of fungi using the diffusion chamber device FIND technology

• Benjamin Libor,
• Henrik Harms,
• Stefan Kehraus,
• Ekaterina Egereva,
• Max Crüsemann and
• Gabriele M. König

Beilstein J. Org. Chem. 2019, 15, 2191–2203, doi:10.3762/bjoc.15.216

• growth of M. violaceum with an inhibition zone of 3 mm in diameter (miconazole, half concentrated, was used as positive control with an inhibition zone of 10 mm; see Supporting Information File 1, Table S3 for full experimental data). Detailed chemical investigation of H. cf. alpina including structure

• the appropriate test organism was significantly inhibited compared to a negative control; total inhibition: no growth at all in the appropriate zone. Benzylpenicillin (1 mg/mL MeOH), streptomycin (1 mg/mL MeOH) and miconazole (0.5 mg/mL DCM) were used as positive controls. Cytotoxicity assay HEK293

Cyclodextrin–polysaccharide-based, in situ-gelled system for ocular antifungal delivery

• Anxo Fernández-Ferreiro,
• Noelia Fernández Bargiela,
• María Santiago Varela,
• Maria Gil Martínez,
• Maria Pardo,
• Antonio Piñeiro Ces,
• José Blanco Méndez,
• Miguel González Barcia,
• Maria Jesus Lamas and
• Francisco.J. Otero-Espinar

Beilstein J. Org. Chem. 2014, 10, 2903–2911, doi:10.3762/bjoc.10.308

• ]. Specifically, azole-based medications, which include imidazoles (e.g., miconazole, clotrimazole, and ketoconazole) and triazoles (e.g., fluconazole, itraconazole, posaconazole, and voriconazole), inhibit ergosterol synthesis in the cell wall [4]. Fluconazole is considered to be a good therapeutic option for

Encapsulation of biocides by cyclodextrins: toward synergistic effects against pathogens

• Véronique Nardello-Rataj and
• Loïc Leclercq

Beilstein J. Org. Chem. 2014, 10, 2603–2622, doi:10.3762/bjoc.10.273

• typical examples of CDs/biocide inclusion on textile are reported. In 2008, Wang et al. incorporated the miconazole nitrate (Figure 6) into the cavity of MCT-β-CD covalently bound onto cloth fibers. The miconazole salts are antifungal agents with additional antibacterial and antiparasitic actions [63

• ]. The optimal conditions were obtained at 150–160 °C for 5–8 min, with MCT-β-CD 60–100 g/L, Na2CO3 50–60 g/L leading to a grafting yield of about 5%. UV spectrophotometry on modified and unmodified fabrics revealed that the miconazole nitrate entrapped in the functionalized textile with MCT-β-CD was

• higher compared to the unmodified one (up to 8.2-fold). As expected, the antifungal activity against C. albicans was enhanced for the MCT-β-CD grafted textile impregnated with miconazole nitrate. The finished fabric retains its antibacterial property even after ten washes unlike the unmodified textile

Advances in synthetic approach to and antifungal activity of triazoles

• Kumari Shalini,
• Nitin Kumar,
• Sushma Drabu and
• Pramod Kumar Sharma

Beilstein J. Org. Chem. 2011, 7, 668–677, doi:10.3762/bjoc.7.79

• azoles are a class of synthetic compounds that possess one or more azole rings. Whilst both imidazole and triazole are five membered ring heterocycles, imidazole contains two ring nitrogen atoms, whereas triazoles have three. However, compared with imidazoles (clotrimazole, ketoconazole, miconazole

Synthesis of some novel hydrazono acyclic nucleoside analogues

• Mohammad N. Soltani Rad,
• Ali Khalafi-Nezhad and
• Somayeh Behrouz

Beilstein J. Org. Chem. 2010, 6, No. 49, doi:10.3762/bjoc.6.49

• Abstract The syntheses of novel hydrazono acyclic nucleosides similar to miconazole scaffolds are described. In this series of acyclic nucleosides, pyrimidine as well as purine and other azole derivatives replaced the imidazole function in miconazole and the ether group was replaced with a hydrazone moiety

• ; hydrazone; ketone; miconazole; Introduction In recent years, fungal infections have become an important complication and a major cause of morbidity and mortality in immune-compromised individuals who suffer from tuberculosis, cancer or AIDS, and who undergo organ transplants [1][2]. Up to now, there has

• has led to an ongoing search for safe and efficient chemotherapeutic agents with potent broad-spectrum antifungal activities. Some of the best known antifungal azole drugs having rational versatility in structures are miconazole (A), oxiconazole (B) and related compounds, namely aryl azoles (Figure 1

Sordarin, an antifungal agent with a unique mode of action

• Huan Liang

Beilstein J. Org. Chem. 2008, 4, No. 31, doi:10.3762/bjoc.4.31

• , itraconazole, ketoconazole, miconazole) (Figure 1). However, these drugs elicit severe side effects, for instance, nephrotoxicity; furthermore, they are ineffective against emerging resistant fungal strains. Therefore, the search for new antimycotic agents continues unabated. While the development of new