In vitro antifungal and antibiofilm activities of novel sulfonyl hydrazone derivatives against Candida spp.

Aydın, Merve; Öztürk, Ali; Duran, Tugce; Özmen, Ümmühan Özdemir; Sumlu, Esra; Ayan, Esra Bilen; Korucu, Emine Nedime

doi:10.1016/j.mycmed.2022.101327

Cited by 14 publications

(11 citation statements)

References 28 publications

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“…Briefly, the inoculum size was adjusted to 0.5–2.5 × 10 3 Candida cells/mL using RPMI1640 media (pH: 7.0) supplemented with 2% glucose. The microplates were incubated at 37 °C for 24–48 h. The first well with total growth inhibition was referred to as the minimum inhibitory concentration (MIC) …”

Section: Methodsmentioning

confidence: 99%

“…The microplates were incubated at 37 °C for 24−48 h. The first well with total growth inhibition was referred to as the minimum inhibitory concentration (MIC). 8 4.2.3. Effects on Mature Biofilm Formation.…”

Section: -((5-(23-diethylquinoxalin-6-yl)-4-ethyl-4h-124-triazol-3-yl...mentioning

confidence: 99%

“…7 Candida species are commensal organisms that can lead to infection ranging from minor to severe candidemia and invasive candidiasis. 8 The most crucial and harmful quality of Candida species is their capacity to create biofilms, which makes finding effective treatments and battling disease more difficult. 9 Biofilms are habitats in which microbial organisms are coated in a matrix of extracellular polymeric molecules (EPS).…”

Section: Introductionmentioning

confidence: 99%

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Synthesis, Antifungal Activities, Molecular Docking and Molecular Dynamic Studies of Novel Quinoxaline-Triazole Compounds

Osmaniye,

Baltacı Bozkurt,

Levent

et al. 2023

ACS Omega

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Uncontrolled use of antifungal drugs affects the development of resistance to existing drugs. Azole antifungals constitute a large part of antifungal therapy. Therefore, there is a need for new azole antifungals. Within the scope of this study, 17 new triazole derivative compounds were synthesized. Structure determinations were clarified by spectroscopic analysis methods ( 1 H-NMR, 13 C-NMR, HRMS). In addition, structure matching was completed using two-dimensional NMR techniques, HSQC, HMBC and NOESY. The antifungal effects of the compounds were evaluated on Candida strains by means of in vitro method. Compound 5d showed activity against Candida glabrata with a MIC 90 = 2 μg/mL. Compound 5d showed activity against Candida krusei with a MIC 90 = 2 μg/mL. This activity value, which is higher than fluconazole, is promising. In addition, the biofilm inhibition percentages of the compounds were calculated. Molecular docking and molecular dynamics simulations performed with compound 5d are in harmony with activity studies.

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Section: Methodsmentioning

confidence: 99%

Section: -((5-(23-diethylquinoxalin-6-yl)-4-ethyl-4h-124-triazol-3-yl...mentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Synthesis, Antifungal Activities, Molecular Docking and Molecular Dynamic Studies of Novel Quinoxaline-Triazole Compounds

Osmaniye,

Baltacı Bozkurt,

Levent

et al. 2023

ACS Omega

View full text Add to dashboard Cite

show abstract

“…Briefly, the inoculum size was adjusted to 0.5–2.5×10 3 Candida cells/mL using RPMI1640 media (pH:7.0) supplemented with 2 % glucose. The microplates were incubated at 37 °C for 24—48 h. The first well with total growth inhibition was referred to as the minimum inhibitory concentration (MIC) [36] …”

Section: Methodsmentioning

confidence: 99%

“…The microplates were incubated at 37 °C for 24-48 h. The first well with total growth inhibition was referred to as the minimum inhibitory concentration (MIC). [36]…”

Section: -((1-(4-(1h-imidazol-1-yl)phenyl)ethylidene)hydrazineylidend...mentioning

confidence: 99%

Synthesis of Imidazole‐2,3‐dihydrothiazole Compounds as VEGFR‐2 Inhibitors and Their Support with in Silico Studies

Osmaniye,

Bozkurt,

Kurban

et al. 2023

Chemistry & Biodiversity

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When the structure of VEGFR inhibitors is examined, it is seen that it consists of 4 pharmacophoric parts. In the light of this information, within the scope of this study, new 2‐((1‐(4‐(1H‐imidazol‐1‐yl)phenyl)ethylidene)hydrazineylidene)‐3‐ethyl‐4‐(substitutephenyl)‐2,3‐dihydrothiazole derivatives were synthesized. Structure determinations of the synthesized derivatives were made using spectroscopic methods. Firstly, the resulting compounds (4a‐4l) were subjected to the 24‐hour MTT test against MCF7, HepG2 and NIH3T3 cells. According to the MTT test results, compound 4h showed activity with IC50=4.566±0.246 µM and compound 4k with IC50=4.537±0.463 µM against HepG2 cell line. The antifungal activities and biofilm inhibition percentages of all compounds against infection problems that may develop in patients receiving chemotherapy were investigated. Compounds 4h and 4k which are active in the MTT test were tested for inhibition of VEGFR‐2 enzymes. Compound 4h displayed VEGFR‐2 inhibition with IC50=0.066±0.002 µM value; compound 4k did not show enzyme inhibition with an IC50>10 µM. Molecular docking studies were performed with two compounds (4k and 4h) and sorafenib to understand the dramatic difference for VEGFR‐2 inhibition. Molecular dynamics studies were performed with using 4h‐4ASE complex and both stability (RMSD, RMSF, Rg) and interaction potentials of the complex were analyzed and presented.

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Synthesis and in Silico Studies of Some New 1,2,3‐Triazolyltetrazole Bearing Indazole Derivatives as Potent Antimicrobial Agents

Gujja,

Sadineni,

Epuru

et al. 2023

Chemistry & Biodiversity

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Abstract1,2,3‐Triazole and tetrazole derivatives bearing pyrrolidines are found to exhibit notable biological activity and have become useful scaffolds in medicinal chemistry for application in lead discovery and optimization. Novel indazole bearing 1,2,3‐triazolyltetrazoles were designed as potential antimicrobial candidates. The structure of duel heterocyclics was validated by a spectroscopic technique of infrared (IR), nuclear magnetic resonance (1H and 13C NMR), and mass spectral data. Compounds 4b, 4c, 4d, and 4h were found to have a stronger antibacterial effect against Gram‐positive (S. aureus, B. subtilis, M. Luteus) and Gram‐negative (E. coli, P. aeruginosa) microorganisms with MICs ranging from 5±0.03–18±0.02 μM, respectively. Moreover, scaffolds 4a, 4h showed potent antifungal activity against A. flavus, M. gypsuem strains with MIC values of 10±0.02, 11±0.01 μM, which are similar activity that of the standard Itraconazole (MIC=8±0.02, 10±0.01 μM). The binding mode for compound 4 inside the catalytic pocket of S. aureus complexed with nicotinamide adenine dinucleotide phosphate and trimethoprim and produced a network of hydrophobic and hydrophilic interactions (3FRE). From in silico results, 4b demonstrated highly stable hydrogen binding amino acids Leu62(X) [N18…O, 2.47 Å], Arg44(X) [N17…N, 3.11 Å], Thr96(X) [N10…OG1, 3.05 Å], Gly94(X) [F7…N, 2.82 Å], and Gly43(X) [F7…N, 2.90 Å], which are plays a crucial role in ensuring efficient binding of the ligand in a crystal structure of antibacterial receptor. Furthermore, the physicochemical and ADME filtration molecular properties, estimation of toxicity, and bioactivity scores of these novel scaffolds were evaluated by using SwissADME and ADMETlab2.0 online protocols. Thus, the significant antimicrobial activity of indazole linked to duel heterocyclic compounds can be used for development of new antimicrobial agents with further modifications.

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In vitro antifungal and antibiofilm activities of novel sulfonyl hydrazone derivatives against Candida spp.

Cited by 14 publications

References 28 publications

Synthesis, Antifungal Activities, Molecular Docking and Molecular Dynamic Studies of Novel Quinoxaline-Triazole Compounds

Synthesis, Antifungal Activities, Molecular Docking and Molecular Dynamic Studies of Novel Quinoxaline-Triazole Compounds

Synthesis of Imidazole‐2,3‐dihydrothiazole Compounds as VEGFR‐2 Inhibitors and Their Support with in Silico Studies

Synthesis and in Silico Studies of Some New 1,2,3‐Triazolyltetrazole Bearing Indazole Derivatives as Potent Antimicrobial Agents

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