Displaying publications 1 - 20 of 76 in total

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  1. Triazole hybrid compounds: A new frontier in malaria treatment
    Ravindar L, Hasbullah SA, Rakesh KP, Hassan NI
    Eur J Med Chem, 2023 Nov 05;259:115694.
    PMID: 37556947 DOI: 10.1016/j.ejmech.2023.115694
    Reviewing the advancements in malaria treatment, the emergence of triazole hybrid compounds stands out as a groundbreaking development. Combining the advantages of triazole and other moieties, these hybrid compounds offer a new frontier in the battle against malaria. Their potential as effective antimalarial agents has captured the attention of researchers and holds promise for overcoming the challenges posed by drug-resistant malaria strains. We focused on their broad spectrum of antimalarial activity of diverse hybridized 1,2,3-triazoles and 1,2,4-triazoles, structure-activity relationship (SAR), drug-likeness, bioavailability and pharmacokinetic properties reported since 2018 targeting multiple stages of the Plasmodium life cycle. This versatility makes them highly effective against both drug-sensitive and drug-resistant strains of P. falciparum, making them invaluable tools in regions where resistance is prevalent. The synergistic effects of combining the triazole moiety with other pharmacophores have resulted in even greater antimalarial potency. This approach has the potential to circumvent existing resistance mechanisms and provide a more sustainable solution to malaria treatment. While triazole hybrid compounds show great promise, further research and clinical trials are warranted to fully evaluate their safety, efficacy and long-term effects. As research progresses, these compounds can potentially revolutionize the field and contribute to global efforts to eradicate malaria, ultimately saving countless lives worldwide.
    Matched MeSH terms: Triazoles/pharmacology; Triazoles/therapeutic use
  2. Transitions of smectic A to tilted phases in thin free standing films of liquid crystal
    Lum CY, Ong LH, ÄŒepic M
    Sains Malaysiana, 2011;40:1123-1127.
    The transition of orthogonal smectic A (SmA) phase to the tilted phases, upon lowering the temperature, is explored with a discrete phenomenological model and the phase diagrams are presented. The results show that the transition of SmA to uniplanar structures can be affected by the effect of chirality. The areas showing the uniplanar phase in the phase diagrams diminish with the increase in effect of chirality.
    Matched MeSH terms: Triazoles
  3. Fulltext Behavior of Tilted Angle Shear Connectors
    Khorramian K, Maleki S, Shariati M, Ramli Sulong NH
    PLoS One, 2015;10(12):e0144288.
    PMID: 26642193 DOI: 10.1371/journal.pone.0144288
    According to recent researches, angle shear connectors are appropriate to transfer longitudinal shear forces across the steel-concrete interface. Angle steel profile has been used in different positions as L-shaped or C-shaped shear connectors. The application of angle shear connectors in tilted positions is of interest in this study. This study investigates the behaviour of tilted-shaped angle shear connectors under monotonic loading using experimental push out tests. Eight push-out specimens are tested to investigate the effects of different angle parameters on the ultimate load capacity of connectors. Two different tilted angles of 112.5 and 135 degrees between the angle leg and steel beam are considered. In addition, angle sizes and lengths are varied. Two different failure modes were observed consisting of concrete crushing-splitting and connector fracture. By increasing the size of connector, the maximum load increased for most cases. In general, the 135 degrees tilted angle shear connectors have a higher strength and stiffness than the 112.5 degrees type.
    Matched MeSH terms: Triazoles
  4. Direction of flexoelectric polarization in smectic CG* phases of chiral smectic liquid crystals
    Teng YT, Lye HO
    Sains Malaysiana, 2014;43:145-150.
    Polarization in antiferroelectric liquid crystals has two origins: The piezoelectric polarization which is of chiral origin and the flexoelectric polarization which originates in different orientation of tilts in neighboring layers. The flexoelectric polarization is perpendicular to the tilt direction only if the structure is uniformly helicoidally modulated. In structures like SmC*F11andSmC;12 the flexoelectric contribution might be significant and it can be non-parallel to the piezoelectric component. Hence it may deviates the direction of polarization from the perpendicular direction significantly. The angle formed by the polarization and the tilt is therefore general and as such the basic characteristic of the SmCG* phase can be recognized. It seems that this aspect was completely overlooked in the past. In this contribution we analyze the dependence of the polarization direction on the phase structures and on the values of piezoelectric and flexoelectric coefficients in the discrete phenomenological model.
    Matched MeSH terms: Triazoles
  5. Click chemistry approach: regioselective one-pot synthesis of some new 8-trifluoromethylquinoline based 1,2,3-triazoles as potent antimicrobial agents
    Garudachari B, Isloor AM, Satyanarayana MN, Fun HK, Hegde G
    Eur J Med Chem, 2014 Mar 3;74:324-32.
    PMID: 24486415 DOI: 10.1016/j.ejmech.2014.01.008
    Three series of 8-trifluoromethylquinoline based 1,2,3-triazoles derivatives (5a-c, 6a-d and 7a-c) were synthesized by multi-step reactions by click chemistry approach. Synthesized compounds were characterized by spectral studies and X-ray analysis. The final compounds were screened for their in-vitro antimicrobial activity by well plate method (zone of inhibition). Compounds 5c, 6b, 8b, 11 and 12 were found to be active against tested microbial strains. The results are summarized in Tables 5 and 6.
    Matched MeSH terms: Triazoles/chemical synthesis*; Triazoles/chemistry
  6. Fulltext Synthesis, characterization and antifungal evaluation of 5-substituted-4-amino-1,2,4-triazole-3-thioesters
    Hasan A, Thomas NF, Gapil S
    Molecules, 2011;16(2):1297-309.
    PMID: 21278680 DOI: 10.3390/molecules16021297
    A series of 5-substituted-4-amino-1,2,4-triazole-3-thioesters was synthesized by converting variously substituted organic acids successively into the corresponding esters, hydrazides, 5-substituted-1,3,4-oxadiazole-2-thiols, 5-substituted-1,2,4-triazole-2-thiols and 5-substituted-1,3,4-oxadiazole-2-thioesters. Finally the target compounds were obtained by refluxing 5-substituted-1,3,4-oxadiazole-2-thioesters in the presence of hydrazine hydrate and absolute alcohol. The structures of the synthesized compounds were established by physicochemical and spectroscopic methods. The synthesized compounds were evaluated for their in vitro antifungal activity. Some of the evaluated compounds possessed significant antifungal activity as compared to a terbinafine standard.
    Matched MeSH terms: Triazoles/chemical synthesis*; Triazoles/chemistry*
  7. Fulltext Prediction of Hexaconazole Concentration in the Top Most Layer of Oil Palm Plantation Soil Using Exploratory Data Analysis (EDA)
    Maznah Z, Halimah M, Shitan M, Kumar Karmokar P, Najwa S
    PLoS One, 2017;12(1):e0166203.
    PMID: 28060816 DOI: 10.1371/journal.pone.0166203
    Ganoderma boninense is a fungus that can affect oil palm trees and cause a serious disease called the basal stem root (BSR). This disease causes the death of more than 80% of oil palm trees midway through their economic life and hexaconazole is one of the particular fungicides that can control this fungus. Hexaconazole can be applied by the soil drenching method and it will be of interest to know the concentration of the residue in the soil after treatment with respect to time. Hence, a field study was conducted in order to determine the actual concentration of hexaconazole in soil. In the present paper, a new approach that can be used to predict the concentration of pesticides in the soil is proposed. The statistical analysis revealed that the Exploratory Data Analysis (EDA) techniques would be appropriate in this study. The EDA techniques were used to fit a robust resistant model and predict the concentration of the residue in the topmost layer of the soil.
    Matched MeSH terms: Triazoles/analysis; Triazoles/chemistry*
  8. Thiadiazole-, selenadiazole- and triazole-fused anthraquinones as G-quadruplex targeting anticancer compounds
    Andreeva DV, Vedekhina TS, Gostev AS, Dezhenkova LG, Volodina YL, Markova AA, et al.
    Eur J Med Chem, 2024 Mar 15;268:116222.
    PMID: 38387333 DOI: 10.1016/j.ejmech.2024.116222
    G-quadruplex (G4) ligands attract considerable attention as potential anticancer therapeutics. In this study we proposed an original scheme for synthesis of azole-fused anthraquinones and prepared a series of G4 ligands carrying amino- or guanidinoalkylamino side chains. The heterocyclic core and structure of the terminal groups strongly affect on binding to G4-forming oligonucleotides, cellular accumulation and antitumor potency of compounds. In particular, thiadiazole- and selenadiazole- but not triazole-based ligands inhibit the proliferation of tumor cells (e.g. K562 leukemia) and stabilize primarily telomeric and c-MYC G4s. Anthraselenadiazole derivative 11a showed a good affinity to c-MYC G4 in vitro and down-regulated expression of c-MYC oncogene in cellular conditions. Further studies revealed that anthraselenadiazole 11a provoked cell cycle arrest and apoptosis in a dose- and time-dependent manner inhibiting K562 cells growth. Taken together, this work gives a valuable example that the closely related heterocycles may cause a significant difference in biological properties of G4 ligands.
    Matched MeSH terms: Triazoles/pharmacology
  9. Fulltext Conjugated Oligo-Aromatic Compounds Bearing a 3,4,5-Trimethoxy Moiety: Investigation of Their Antioxidant Activity Correlated with a DFT Study
    Kareem HS, Nordin N, Heidelberg T, Abdul-Aziz A, Ariffin A
    Molecules, 2016 Feb 17;21(2).
    PMID: 26901175 DOI: 10.3390/molecules21020224
    A series of heterocyclic compounds bearing the well-known free radical scavenging 3,4,5-trimethoxybenzyloxy group, was synthesized. The key compound 4-(3,4,5-trimethoxybenzyl-oxy)benzohydrazide was converted into thiosemicarbazide derivatives, which were subsequently cyclized with NaOH to provide 1,2,4-triazole derivatives. Alternative treatment of the acid hydrazide with carbon disulfide in the presence of KOH led to the corresponding 1,3,4-oxadiazole and various alkylated derivatives. The newly synthesized compounds were purified and the structures of the products were elucidated and confirmed on the basis of their analytical and spectral data. Their antioxidant activities were evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH(•)) and Ferric Reducing Antioxidant Power (FRAP) assays. The thiosemicarbazide derivatives were highly active in both antioxidant assays with the lowest IC50 value for DPPH radical scavenging. Theoretical calculations based on density functional theory (DFT) were performed to understand the relative importance of NH, SH and CH hydrogens on the radical scavenging activities of these compounds.
    Matched MeSH terms: Triazoles/chemical synthesis*; Triazoles/pharmacology; Triazoles/chemistry
  10. Fulltext Crystal structure of 4-({(1E,2E)-3-[3-(4-fluoro-phen-yl)-1-isopropyl-1H-indol-2-yl]allyl-idene}amino)-5-methyl-1H-1,2,4-triazole-5(4H)-thione
    Kulkarni AD, Rahman ML, Mohd Yusoff M, Kwong HC, Quah CK
    Acta Crystallogr E Crystallogr Commun, 2015 Nov 1;71(Pt 11):1411-3.
    PMID: 26594522 DOI: 10.1107/S2056989015020101
    The title compound, C23H22FN5S, exists in a trans conformation with respect to the methene C=C and the acyclic N=C bonds. The 1,2,4-triazole-5(4H)-thione ring makes dihedral angles of 88.66 (9) and 84.51 (10)°, respectively, with the indole and benzene rings. In the crystal, mol-ecules are linked by pairs of N-H⋯S hydrogen bonds, forming inversion dimers with an R 2 (2)(8) ring motif. The dimers are linked via C-H⋯π inter-actions, forming chains along [1-10]. The chains are linked via π-π inter-actions involving inversion-related triazole rings [centroid-centroid distance = 3.4340 (13) Å], forming layers parallel to the ab plane.
    Matched MeSH terms: Triazoles
  11. Fulltext Crystal structure of tetra-aqua-bis(3,5-di-amino-4H-1,2,4-triazol-1-ium)cobalt(II) bis-[bis-(pyridine-2,6-di-carboxyl-ato)cobaltate(II)] dihydrate
    Johnson A, Mbonu J, Hussain Z, Loh WS, Fun HK
    Acta Crystallogr E Crystallogr Commun, 2015 Jun 1;71(Pt 6):m139-40.
    PMID: 26090171 DOI: 10.1107/S2056989015010014
    The asymmetric unit of the title compound, [Co(C2H6N5)2(H2O)4][Co(C7H3NO4)2]2·2H2O, features 1.5 Co(II) ions (one anionic complex and one half cationic complex) and one water mol-ecule. In the cationic complex, the Co(II) atom is located on an inversion centre and is coordinated by two triazolium cations and four water mol-ecules, adopting an octa-hedral geometry where the N atoms of the two triazolium cations occupy the axial positions and the O atoms of the four water mol-ecules the equatorial positions. The two triazole ligands are parallel offset (with a distance of 1.38 Å between their planes). In the anionic complex, the Co(II) ion is six-coordinated by two N and four O atoms of the two pyridine-2,6-di-carboxyl-ate anions, exhibiting a slightly distorted octa-hedral coordination geometry in which the mean plane of the two pyridine-2,6-di-carboxyl-ate anions are almost perpendicular to each other, making a dihedral angle of 85.87 (2)°. In the crystal, mol-ecules are linked into a three-dimensional network via C-H⋯O, C-H⋯N, O-H⋯O and N-H⋯O hydrogen bonds.
    Matched MeSH terms: Triazoles
  12. Fulltext Crystal structure of 1-{1-[2-(phenyl-selan-yl)phen-yl]-1H-1,2,3-triazol-4-yl}cyclo-hexan-1-ol
    Camargo LR, Zukerman-Schpector J, Deobald AM, Braga AL, Tiekink ER
    Acta Crystallogr E Crystallogr Commun, 2015 Mar 1;71(Pt 3):o200-1.
    PMID: 25844248 DOI: 10.1107/S2056989015003242
    Two independent mol-ecules, A and B, comprise the asymmetric unit of the title compound, C20H21N3OSe. While the benzene ring directly bound to the central triazole ring is inclined to the same extent in both mol-ecules [dihedral angles = 40.41 (12) (mol-ecule A) and 44.14 (12)° (B)], greater differences are apparent in the dihedral angles between the Se-bound rings, i.e. 74.28 (12) (mol-ecule A) and 89.91 (11)° (B). Close intra-molecular Se⋯N inter-actions of 2.9311 (18) (mol-ecule A) and 2.9482 (18) Å (B) are noted. In the crystal, supra-molecular chains along the a axis are formed via O-H⋯N hydrogen bonding. These are connected into layers via C-H⋯O and C-H⋯N inter-actions; these stack along (01-1) without directional inter-molecular inter-actions between them.
    Matched MeSH terms: Triazoles
  13. Simultaneous enantioseparation of cyproconazole, bromuconazole, and diniconazole enantiomers by CD-modified MEKC
    Wan Ibrahim WA, Warno SA, Aboul-Enein HY, Hermawan D, Sanagi MM
    Electrophoresis, 2009 Jun;30(11):1976-82.
    PMID: 19517438 DOI: 10.1002/elps.200800499
    An efficient method for the simultaneous enantioseparation of cyproconazole, bromuconazole, and diniconazole enantiomers was developed by CD-modified MEKC using a dual mixture of neutral CDs as chiral selector. Three neutral CDs namely hydroxypropyl-beta-CD, hydroxypropyl-gamma-CD, and gamma-CD were tested as chiral selectors at different concentrations ranging from 10, 20, 30 and 40 mM, but enantiomers of the studied fungicides were not completely separated. The best dual chiral recognition mode for the simultaneous separation of cyproconazole, bromuconazole, and diniconazole enantiomers was achieved with a mixture of 27 mM hydroxypropyl-beta-CD and 3 mM hydroxypropyl-gamma-CD in 25 mM phosphate buffer (pH 3.0) containing 40 mM SDS to which methanol-acetonitrile (10%:5% v/v) was added as organic modifiers. The best separation was based on the appearance of 10 peaks simultaneously, with good resolution (R(s) 1.1-15.9), and peak efficiency (N>200,000). Good repeatabilities in the migration time, peak area, and peak height were obtained in terms of RSD ranging from (0.72 to 1.06)%, (0.39 to 3.49)%, and (1.90 to 4.84)%, respectively.
    Matched MeSH terms: Triazoles/isolation & purification*
  14. Fulltext Treated Rhizophora mucronata tannin as a corrosion inhibitor in chloride solution
    Agi A, Junin R, Rasol M, Gbadamosi A, Gunaji R
    PLoS One, 2018;13(8):e0200595.
    PMID: 30089104 DOI: 10.1371/journal.pone.0200595
    Treated Rhizopora mucronata tannin (RMT) as a corrosion inhibitor for carbon steel and copper in oil and gas facilities was investigated. Corrosion rate of carbon-steel and copper in 3wt% NaCl solution by RMT was studied using chemical (weight loss method) and spectroscopic (FTIR) techniques at various temperatures in the ranges of 26-90°C. The weight loss data was compared to the electrochemical by the application of Faraday's law for the conversion of corrosion rate data from one system to another. The inhibitive efficiency of RMT was compared with commercial inhibitor sodium benzotriazole (BTA-S). The best concentration of RMT was 20% (w/v), increase in concentration of RMT decreased the corrosion rate and increased the inhibitive efficiency. Increase in temperature increased the corrosion rate and decreased the inhibitive efficiency but, the rate of corrosion was mild with RMT. The FTIR result shows the presence of hydroxyl group, aromatic group, esters and the substituted benzene group indicating the purity of the tannin. The trend of RMT was similar to that of BTA-S, but its inhibitive efficiency for carbon-steel was poor (6%) compared to RMT (59%). BTA-S was efficient for copper (76%) compared to RMT (74%) at 40% (w/v) and 20% (w/v) concentration respectively. RMT was efficient even at low concentration therefore, the use of RMT as a cost effective and environmentally friendly corrosion inhibiting agent for carbon steel and copper is herein proposed.
    Matched MeSH terms: Triazoles/chemistry
  15. Impact of stabilizer on the environmental behavior of PVC films reinforced 1,2,4-triazole moiety
    Yousif E, Ahmed DS, Ahmed A, Abdallh M, Yusop RM, Mohammed SA
    Environ Sci Pollut Res Int, 2019 Sep;26(25):26381-26388.
    PMID: 31290046 DOI: 10.1007/s11356-019-05784-w
    A new Schiff base containing 1,2,4-triazole ring system (L) was synthesized and confirmed by 1HNMR, FTIR spectroscopy. The chemical modification of PVC with a new Schiff base (L) was synthesized to produce a homogenous blend (PVC-L). A homogenous blend (PVC-L) was added to copper chloride to produce PVC-L-Cu (II). The PVC films had been irradiated with ultraviolet light for a long period and confirmed by FTIR spectroscopy and weight loss; the surface morphology was inspected by scanning electron microscopy.
    Matched MeSH terms: Triazoles/chemistry*
  16. Fulltext Crystal structure of 3-(adamantan-1-yl)-4-(4-chloro-phen-yl)-1H-1,2,4-triazole-5(4H)-thione
    Al-Wabli RI, El-Emam AA, Alroqi OS, Chidan Kumar CS, Fun HK
    Acta Crystallogr E Crystallogr Commun, 2015 Feb 1;71(Pt 2):o115-6.
    PMID: 25878859 DOI: 10.1107/S2056989015000596
    The title compound, C18H20ClN3S, is a functionalized triazoline-3-thione derivative. The benzene ring is almost perpendic-ular to the planar 1,2,4-triazole ring [maximum deviation = 0.007 (1) Å] with a dihedral angle of 89.61 (5)° between them and there is an adamantane substituent at the 3-position of the triazole-thione ring. In the crystal, N-H⋯S hydrogen-bonding inter-actions link the mol-ecules into chains extending along the c-axis direction. The crystal packing is further stabilized by weak C-H⋯π inter-actions that link adjacent chains into a two-dimensional structure in the bc plane. The crystal studied was an inversion twin with a 0.50 (3):0.50 (3) domain ratio.
    Matched MeSH terms: Triazoles
  17. Syntheses, in vitro α-amylase and α-glucosidase dual inhibitory activities of 4-amino-1,2,4-triazole derivatives their molecular docking and kinetic studies
    Yeye EO, Kanwal, Mohammed Khan K, Chigurupati S, Wadood A, Ur Rehman A, et al.
    Bioorg Med Chem, 2020 06 01;28(11):115467.
    PMID: 32327353 DOI: 10.1016/j.bmc.2020.115467
    Thirty-three 4-amino-1,2,4-triazole derivatives 1-33 were synthesized by reacting 4-amino-1,2,4-triazole with a variety of benzaldehydes. The synthetic molecules were characterized via1H NMR and EI-MS spectroscopic techniques and evaluated for their anti-hyperglycemic potential. Compounds 1-33 exhibited good to moderate in vitro α-amylase and α-glucosidase inhibitory activities in the range of IC50 values 2.01 ± 0.03-6.44 ± 0.16 and 2.09 ± 0.08-6.54 ± 0.10 µM as compared to the standard acarbose (IC50 = 1.92 ± 0.17 µM) and (IC50 = 1.99 ± 0.07 µM), respectively. The limited structure-activity relationship suggested that different substitutions on aryl part of the synthetic compounds are responsible for variable activity. Kinetic study predicted that compounds 1-33 followed mixed and non-competitive type of inhibitions against α-amylase and α-glucosidase enzymes, respectively. In silico studies revealed that both triazole and aryl ring along with different substitutions were playing an important role in the binding interactions of inhibitors within the enzyme pocket. The synthetic molecules were found to have dual inhibitory potential against both enzymes thus they may serve as lead candidates for the drug development and research in the future studies.
    Matched MeSH terms: Triazoles/chemical synthesis; Triazoles/pharmacology*; Triazoles/chemistry
  18. BSA Binding, molecular docking and in vitro biological screening of some new 1, 2, 4-triazole heterocycles bearing azinane nucleus
    Iqbal J, Rehman A, Abbasi MA, Siddiqui SZ, Khalid H, Laulloo SJ, et al.
    Pak J Pharm Sci, 2020 Jan;33(1):149-160.
    PMID: 32122843
    A series of new compounds (5a-q), derived from 5-(1-(4-nitrophenylsulfonyl) piperidin-4-yl)-4-phenyl-4H-1,2,4-triazole-3-thiol (3) were proficiently synthesized to evaluate their biological activities. 1-(4-Nitrophenylsulfonyl) piperidine-4-carbohydrazide (2) was refluxed with phenylisothiocyanate to yield an adduct which was cyclized to compound 3 by reflux reaction with 10 % potassium hydroxide. The targeted compounds 5a-q, were synthesized by stirring alkyl/aralkyl halides (4a-q) and compound 3 in a polar aprotic solvent. 1H-NMR, 13C-NMR, EI-MS and IR spectral techniques were employed to confirm the structures of all the synthesized compounds. The compounds were biologically evaluated for BSA binding studies followed by anti-bacterial, anti-inflammatory and acetylcholinesterase (AChE) activities. The active sites responsible for the best AChE inhibition were identified through molecular docking studies. Compound 5e bearing 4-chlorobenzyl moiety found most active antibacterial and anti-inflammatory agent among the synthesized compounds. The whole library of synthesized compounds except compounds 5d and 5f was found highly active for AChE inhibition and recommended for in vivo studies so that their therapeutic applications may come in utilization.
    Matched MeSH terms: Triazoles/chemical synthesis; Triazoles/pharmacology*; Triazoles/chemistry
  19. α-Glucosidase inhibitory potential and hemolytic evaluation of newly synthesized 3,4,5-trisubstituted-1,2,4-triazole derivatives
    Nafeesa K, Aziz-Ur-Rehman -, Abbasi MA, Siddiqui SZ, Rasool S, Ali Shah SA, et al.
    Pak J Pharm Sci, 2019 Nov;32(6):2651-2658.
    PMID: 31969298
    A series of 1, 2, 4-triazole derivatives bearing piperidine moiety has been introduced as new anti-diabetic drug candidates with least cytotoxicity. p-Chlorophenylsulfonyl chloride (1) and ethyl nipecotate (2) were the starting reagents that resulted into corresponding 3,4,5-trisubstituted-1,2,4-triazole (6) through a series of steps. A series of electrophiles, 9a-e, were synthesized by reacting 4-bromobutyryl chloride (7) with differently substituted aromatic amines (8a-e) under basic aqueous medium. Target derivatives, 10a-e, were synthesized by the reaction of compound 6 with N-aryl-4-bromobutanamides (9a-e) in an aprotic solvent. Structures of all the derivatives were verified by spectroscopic analysis using IR, 1H-NMR, 13C-NMR and EIMS. Most of the derivatives revealed moderate to good α-glucosidase inhibitory activity with reference to acarbose. The moderate hemolytic potential demonstrated least toxicity.
    Matched MeSH terms: Triazoles/chemical synthesis*; Triazoles/pharmacology; Triazoles/chemistry
  20. Antifungal susceptibility profile and biofilm-producing capability of Candida tropicalis isolates in a tertiary medical centre
    Navarathinam SD, Neoh HM, Tan TL, Wahab AA, Mohd Nizam Tzar MN, Ding CH
    Malays J Pathol, 2023 Dec;45(3):417-424.
    PMID: 38155383
    BACKGROUND: Candida tropicalis is a globally distributed yeast that has been popping up in the medical literature lately, albeit for unenviable reasons. C. tropicalis is associated with substantial morbidity, mortality as well as drug resistance. The aims of this study were to ascertain the antifungal susceptibility profile and the biofilm-producing capability of this notorious yeast in our centre.

    METHODS: C. tropicalis isolates from sterile specimens were collected over a 12-month period. Conclusive identification was achieved biochemically with the ID 32 C kit. Susceptibility to nine antifungal agents was carried out using the colourimetric broth microdilution kit Sensititre YeastOne YO10. Biofilm-producing capability was evaluated by quantifying biomass formation spectrophotometrically following staining with crystal violet.

    RESULTS: Twenty-four non-repetitive isolates of C. tropicalis were collected. The resistance rates to the triazole agents were 29.2% for fluconazole, 16.7% for itraconazole, 20.8% for voriconazole and 8.3% for posaconazole-the pan-azole resistance rate was identical to that of posaconazole. No resistance was recorded for amphotericin B, flucysosine or any of the echinocandins tested. A total of 16/24 (66.7%) isolates were categorized as high biomass producers and 8/24 (33.3%) were moderate biomass producers. None of our isolates were low biomass producers.

    CONCLUSION: The C. tropicalis isolates from our centre were resistant only to triazole agents, with the highest resistance rate being recorded for fluconazole and the lowest for posaconazole. While this is not by itself alarming, the fact that our isolates were prolific biofilm producers means that even azole-susceptible isolates can be paradoxically refractory to antifungal therapy.

    Matched MeSH terms: Triazoles
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