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Search results for: INHIBITORY ENZYMU
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Cuticle hydrolysis in four medically important fly species by enzymes of the entomopathogenic fungusConidiobolus coronatus
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Simultaneous siRNA-mediated silencing of pairs of genes coding for enzymes involved in glycosaminoglycan synthesis.
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Endogenous oxidative DNA base modifications analysed with repair enzymes and GC/MS technique
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KU812 basophils express urocortin, CRH-R, MC1R and steroidogenic enzymes and secrete progesterone
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Structural insights, biocatalytic characteristics, and application prospects of lignin-modifying enzymes for sustainable biotechnology
PublicationLignin modifying enzymes (LMEs) have gained widespread recognition in depolymerization of lignin polymers by oxidative cleavage. LMEs are a robust class of biocatalysts that include lignin peroxidase (LiP), manganese peroxidase (MnP), versatile peroxidase (VP), laccase (LAC), and dye-decolorizing peroxidase (DyP). Members of the LMEs family act on phenolic, non-phenolic substrates and have been widely researched for valorization...
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The Role of Electrostatics in Enzymes: Do Biomolecular Force Fields Reflect Protein Electric Fields?
PublicationPreorganization of large, directionally oriented, electric fields inside protein active sites has been proposed as a crucial contributor to catalytic mechanism in many enzymes, and it may be efficiently investigated at the atomistic level with molecular dynamics simulations. Here, we evaluate the ability of the AMOEBA polarizable force field, as well as the additive Amber ff14SB and Charmm C36m models, to describe the electric...
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Prediction of Bioactive Peptides From Chicken Feather and Pig Hair Keratins Using In Silico Analysis Based on Fragmentomic Approach
PublicationBackground: Keratin is among the most abundant structural proteins of animal origin, however it remains broadly underutilized. Objective: Bioinformatic investigation was performed to evaluate selected keratins originating from mass-produced waste products, i.e., chicken feathers and pig hair, as potential sources of bioactive peptides. Methods: Pepsin, trypsin, chymotrypsin, papain, and subtilisin were used for in silico keratinolysis...
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Investigating the disease- modifying properties of sclerotiorin in Alzheimer's therapy using acetylcholinesterase inhibition
PublicationAlzheimer's disease (AD) is a progressive neurodegenerative disorder caused due to the damage and loss of neurons in specific brain regions. It is the most common form of dementia observed in older people. The symptoms start with memory loss and gradually cause the inability to speak and do day-to-day activities. The cost of caring for those affected individuals is huge and is probably beyond most developing countries capability....
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Meat Proteins as Dipeptidyl Peptidase IV Inhibitors and Glucose Uptake Stimulating Peptides for the Management of a Type 2 Diabetes Mellitus In Silico Study
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Efficacy of high-dose corticosteroid-based treatment for chronic lymphocytic leukemia patients with p53 abnormalities in the era of B-cell receptor inhibitors
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Microbial acetylcholinesterase inhibitors for Alzheimer’s therapy: recent trends on extraction, detection, irradiation-assisted production improvement and nano-structured drug delivery
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Synthesis, anticandidal activity of N3-(4-methoxyfumaroyl)-(S)-2,3-diaminopropanoic amide derivatives – Novel inhibitors of glucosamine-6-phosphate synthase
PublicationNovel FMDP amiders 4-6 have been synthesized and tested against Candida strains. The anticandidal activity has been confined only to Candida albicans. Anticandidal activity of the tested amides has correlated with their inhibitory activity of glucosamine-6-phosphate synthase in cell free extract from Candida albicans.
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Development of biocompatible iron oxide-silicon oxide core-shell nanoparticles as subcellular delivery platform for glucosamine-6-phosphate synthase inhibitors
PublicationIn order to develop the preparation of iron oxide-silica coreshell nanoparticles (CSNPs), thesis deeply explores the cetyltrimethylammonium (CTA+) directed silica coating methods of the oleic-acid capped iron oxide nanoparticles (OA-IONPs) initialized under near-neutral pH conditions. It is demonstrated that the initial alkaline hydrolysis of ethyl acetate in the presence of CTA+ and OA-IONPs induces an unusual ligand exchange...
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Highly Specific Substrates of Proteinase 3 Containing 3-(2-Benzoxazol-5-yl)-l-alanine and Their Application for Detection of This Enzyme in Human Serum
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Toxoplasma gondii: Enzyme-Linked Immunosorbent Assay using different fragments of recombinant microneme protein 1 (MIC1) for detection of immunoglobulin G antibodies
PublicationTrzy rekombinantowe fragmenty białka antygenowego MIC1 Toxoplasma gondii (r-MIC1ex2, r-MIC1ex34 i r-MIC1) zostały wyprodukowane jako białka fuzyjne (zawierające dwie domeny oligohistydynowe na N- i C-końcu) w komórkach bakteryjnych Escherichia coli. Homogenne preparaty antygenów rekombinantowych otrzymane z zastosowaniem jednoetapowego oczyszczania metodą chromatografii metalopowinowactwa, wykorzystano następnie do immunoidentyfikacji...
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Two small RNAs conserved in Enterobacteriaceae provide intrinsic resistance to antibiotics targeting the cell wall biosynthesis enzyme glucosamine-6-phosphate synthase
PublicationFormation of glucosamine-6-phosphate GlcN6P) by enzyme GlcN6P synthase (GlmS) represents the first step in bacterial cell envelope synthesis. In Escherichia coli, expression of glmS is controlled by small RNAs (sRNAs) GlmY and GlmZ. GlmZ activates the glmS mRNA by base-pairing. When not required, GlmZ is bound by adapter protein RapZ and recruited to cleavage by RNase E inactivating the sRNA. The homologous sRNA GlmY activates...
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Enzymy o aktywności aminotransferazy kwasu L-α-aminoadypinowego z Candida albicans - właściwości i rola w metabolizmie komórki grzybowej
PublicationCandida albicans jest elementem naturalnej flory drobnoustrojowej człowieka. Podobieństwo komórek grzybowych i ssaczych, wzrost częstości występowania infekcji grzybiczych wraz ze stopniowym wzrostem pojawiania się oporności patogenów stwarza potrzebę poszukiwania nowych związków przeciwgrzybowych. Jedną z dróg obraną przez naukowców jest analiza szlaków biosyntezy aminokwasów egzogennych dla człowieka. Przedmiotem badań w ramach...
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Roman Kotlowski dr hab. inż.
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Adsorption behavior and corrosion inhibitive characteristics of newly synthesized cyano-benzylidene xanthenes on copper/sodium hydroxide interface: Electrochemical, X-ray photoelectron spectroscopy and theoretical studies
PublicationElegant process for synthesis of 3-(7H-dibenzo[c,h]xanthen-7-yl)benzaldehyde (3), as new starting material to create a set of novel xanthene analogues, 2-(3-(7H-dibenzo[c,h]xanthen-7-yl)benzylidene)malononitrile (4), 3-(3-(7H-dibenzo[c,h]xanthen-7-yl)phenyl)-2-cyanoacrylic acid (5), and Ethyl-3-(3-(7H-dibenzo[c,h]xanthen-7-yl)phenyl)-2-cyanoacrylate (6), was achieved starting with available materials under mild conditions. Various...
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Phytochemical screening and biological evaluation of Greek sage (Salvia fruticosa Mill.) extracts
PublicationThis study explores the influence of extraction solvents on the composition and bioactivity of Salvia fruticosa extracts. Ultrasound-assisted extraction with water, ethanol and their mixtures in variable proportions was used to produce four different extracts. An untargeted UPLC/MS‑based metabolomics was performed to discover metabolites profile variation between the extracts. In the analyzed samples, 2704 features had been detected,...
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Drug-drug interaction potential of antitumor acridine agent C-1748: The substrate of UDP-glucuronosyltransferases 2B7, 2B17 and the inhibitor of 1A9 and 2B7
PublicationBackground The compound 9-(2′-hydroxyethylamino)-4-methyl-1-nitroacridine (C-1748), the promising antitumor agent developed in our laboratory was determined to undergo phase I metabolic pathways. The present studies aimed to know its biotransformation with phase II enzymes – UDP-glucuronosyltransferases (UGTs) and its potential to be engaged in drug-drug interactions arising from the modulation of UGT activity. Methods UGT-mediated...
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The Effect of Long-Term Administration of Fatty Acid Amide Hydrolase Inhibitor URB597 on Oxidative Metabolism in the Heart of Rats with Primary and Secondary Hypertension
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PdCl2-catalyzed synthesis of a new class of isocoumarin derivatives containing aminosulfonyl / aminocarboxamide moiety: First identification of a isocoumarin based PDE4 inhibitor
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Simultaneous impedance and volumetric studies and additionally potentiodynamic polarization measurements of molasses as a carbon steel corrosion inhibitor in 1M hydrochloric acid solution
PublicationThe inhibition effect of molasses on the corrosion of low carbon steel in 1M hydrochloric acid solution was investigated by volumetric and electrochemical measurements. Potentiodynamic polarization and dynamic electrochemical impedance spectroscopy (DEIS) results were obtained and compared with to those, obtained with the hydrogen evolution technique. All results indicate that molasses functioned as a good inhibitor in 1M hydrochloric...
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PARP inhibition potentiates the cytotoxic activity of C-1305, a selective inhibitor of topoisomerase II, in human BRCA1-positive breast cancer cells
PublicationTwo cellular proteins encoded by the breast and ovarian cancer type 1 susceptibility (BRCA1 and BRCA2) tumor suppressor genes are essential for DNA integrity and the maintenance of genomic stability.Approximately 5-10% of breast and ovarian cancers result from inherited alterations or mutations in these genes.Remarkably, BRCA1/BRCA2-deficient cells are hypersensitive to selective inhibition of poly(ADPribose) polymerase 1 (PARP-1),...
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Mrówczan sodu z nowym pakietem inhibitorów korozji jako ekologiczny środek do odladzania infrastruktury lotniczej.
PublicationPrzedstawiono wyniki badań korozji kadmowej powłoki na stali oraz korozji po zanurzeniu stopów metali w mrówczanie sodu z nowym pakietem inhibitorów korozji, zawierającym synergiczną kompozycję poliasparaginianu sodu oraz imidazolu. Ponadto wyznaczono zdolność penetracji lodu przez badany układ. Właściwo- ści opracowanej kompozycji odladzającej porównano z właściwościami środków dostępnych na rynku. Uzyskane wyniki wskazują, że otrzymany...
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Nowe estrowe i amidowe pochodne inhibitorów syntazy glukozamino-6-fosforanu - synteza i aktywność biologiczna
PublicationPrzedmiotem rozprawy doktorskiej są modyfikacje chemiczne analogów glutaminy – kwasu N3-(4-metoksyfumaroilo)-S-2,3-diaminopropanowego (FMDP) oraz kwasu N3-[(E)-4-fenylo-4-okso-2-butenoilo]-S-2,3-diaminoaminopropanowego (BADP). Związki te są inhibitorami syntazy glukozamino-6-fosforanu i mimo ich silnych właściwości inhibicyjnych, nie wykazują zdolności do hamowania wzrostu drobnoustrojów. Brak aktywności przeciwdrobnoustrojowej...
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Genistein inhibits activities of methylenetetrahydrofolate reductase and lactate dehydrogenase, enzymes which use NADH as a substrate
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Antioxidative enzymes and expression of rbcL gene as tools to monitor heavy metal-related stress in plants
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Źródła, otrzymywanie i przydatność niektórych termostabilnych enzymów w przetwórstwie skrobi i mleka
PublicationPrezentowane wyniki wskazują na możliwość usprawnienia produkcji syropów skrobiowych przez zastosowanie rekombinantowej alfa-amylazy z Pyrococcus woesei i termostabilnej alfa-glukozydazy z Thermus thermophilus. Wykazano także przydatność rekombinantowej, termosta-bilnej beta-galaktozydazy z Pyrococcus woesei do wytwarzania bez-laktozowego mleka i serwatki. Enzym ten wykazuje dużą termostabil-ność i znaczną aktywność w szerokim...
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Melatonin stimulates the activity of protective antioxidative enzymes in myocardial cells of rats in the course of doxorubicin intoxication
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Molecular Characterization of a Novel Lytic Enzyme LysC from Clostridium intestinale URNW and Its Antibacterial Activity Mediated by Positively Charged N-Terminal Extension
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Experimental and Machine-Learning-Assisted Design of Pharmaceutically Acceptable Deep Eutectic Solvents for the Solubility Improvement of Non-Selective COX Inhibitors Ibuprofen and Ketoprofen
PublicationDeep eutectic solvents (DESs) are commonly used in pharmaceutical applications as excellent solubilizers of active substances. This study investigated the tuning of ibuprofen and ketoprofen solubility utilizing DESs containing choline chloride or betaine as hydrogen bond acceptors and various polyols (ethylene glycol, diethylene glycol, triethylene glycol, glycerol, 1,2-propanediol, 1,3-butanediol) as hydrogen bond donors. Experimental...
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Experimental and Machine-Learning-Assisted Design of Pharmaceutically Acceptable Deep Eutectic Solvents for the Solubility Improvement of Non-Selective COX Inhibitors Ibuprofen and Ketoprofen
PublicationDeep eutectic solvents (DESs) are commonly used in pharmaceutical applications as excellent solubilizers of active substances. This study investigated the tuning of ibuprofen and ketoprofen solubility utilizing DESs containing choline chloride or betaine as hydrogen bond acceptors and various polyols (ethylene glycol, diethylene glycol, triethylene glycol, glycerol, 1,2-propanediol, 1,3-butanediol) as hydrogen bond donors. Experimental...
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A. Computational analysis by molecular docking of thirty alkaloid compounds from medicinal plants as potent inhibitors of SARS-CoV-2 main protease(2020).
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Synthesis of 3-indolylmethyl substituted (pyrazolo/benzo)triazinone derivatives under Pd/Cu-catalysis: Identification of potent inhibitors of chorismate mutase (CM)
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Anti-cancer effect of Rumex obtusifolius in combination with arginase/nitric oxide synthase inhibitors via downregulation of oxidative stress, inflammation, and polyamine synthesis
PublicationCancer continues to be a leading cause of death worldwide, making the development of new treatment methods crucial in the fight against it. With cancer incidence rates increasing worldwide, ongoing research must focus on identifying new and effective ways to prevent and treat the disease. The combination of herbal extracts with chemotherapeutic agents has gained much interest as a novel strategy to combat cancer. Rumex obtusifolius...
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Regulacja topologii DNA przez topoizomerazę typu II, czyli jak struktura DNA wpływa na funkcjonowanie genów
PublicationW wielu ważnych procesach jakie zachodzą w komórce zmienia się topologia DNA i struktura chromatyny. Enzym, topoizomeraza typu II, jest jednym z ważnych czynników, który reguluje zmiany topologiczne i strukturalne w jądrze, przez co ma bezpośredni lub pośredni wpływ na takie procesy jak uporządkowanie struktury chromatyny poprzez wiązanie pętli chromatyny do szkieletu jądrowego, transkrypcję i replikację DNA, reperację uszkodzeń...
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Design, Chemical Synthesis and Kinetic Studies of Trypsin Chromogenic Substrates Based on the Proteinase Binding Loop of Cucurbita maxima Trypsin Inhibitor (CMTI-III)
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Analiza in silico bioaktywnych peptydów pochodzących z keratyny z piór drobiowych
PublicationKeratyna należy do najbardziej powszechnie występujących białek strukturalnych pochodzenia zwierzęcego. Stanowi ok. 90% masy piór wytwarzanych w dużych ilościach przez przemysł drobiarski. Ten odpadowy produkt pozostaje w dużym stopniu niezagospodarowany. Celem pracy była analiza bioinformatyczna pierwszorzędowej struktury keratyny z piór kurzych pod kątem występowania w niej peptydów bioaktywnych....
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Homoisocitrate dehydrogenase from Candida albicans: properties, inhibition, and targeting by an antifungal pro-drug
PublicationThe LYS12 gene from Candida albicans, coding for homoisocitrate dehydrogenase was cloned and expressed as a His-tagged protein in Escherichia coli. The purified gene product catalyzes the Mg2+- and K+-dependent oxidative decarboxylation of homoisocitrate to alpha-ketoadipate. The recombinant enzyme demonstrates strict specificity for homoisocitrate. SDS-PAGE of CaHIcDH revealed its molecular mass of 42.6±1 kDa, while in size-exclusion...
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The psychrotrophic yeast Sporobolomyces roseus LOCK 1119 as a source of a highly active aspartic protease for the in vitro production of antioxidant peptides
PublicationA psychrotrophic yeast strain producing a cold-adapted protease at low temperature was classified as Sporobolomyces roseus. In standard YPG medium, S. roseus LOCK 1119 synthesized an extracellular protease with an activity of approximately 560 U/L. Optimization of medium composition and process temperature considerably enhanced enzyme biosynthesis; an approximate 70% increase in activity (2060 U/L). The native enzyme was purified...
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Metodyka rozdzielania i oznaczania lotnych inhibitorów fermentacji w brzeczkach fermentacyjnych ciemnej fermentacji, techniką GC-MS
PublicationW pracy przedstawiono opracowaną w wyniku badań metodykę identyfikacji i oznaczania inhibitorów fermentacji w brzeczkach fermentacji ciemnej z biomasy ligno-celulozowej, z wykorzystaniem ekstrakcji ciecz-ciecz w sprzężeniu z chromatografią gazową ze spektrometrem mas (LLE-GC-MS). W ramach badań dokonano doboru korzystnych warunków ekstrakcji ciecz-ciecz, w tym: pH, objętości rozpuszczalnika ekstrakcyjnego, czasu ekstrakcji oraz warunków...
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Marta Wanarska dr hab. inż.
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Insect cuticular compounds affect Conidiobolus coronatus (Entomopthorales) sporulation and the activity of enzymes involved in fungal infection
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Modulation of the expression of enzymes metabolizing xenobiotics in rat liver and kidney by oral administration of cabbage and sauerkraut juice.
PublicationObydwa soki z kapusty mogą wpływać selektywnie na ekspresję genów zaangażowanych w aktywację i detoksykację kancerogenów. Efekt ten zależy od sposobu traktowania i może zależeć od rodzaju tkanki.
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Teloxantron inhibits the processivity of telomerase with preferential DNA damage on telomeres
PublicationTelomerase reactivation is one of the hallmarks of cancer, which plays an important role in cellular immortalization and the development and progression of the tumor. Chemical telomerase inhibitors have been shown to trigger replicative senescence and apoptotic cell death both in vitro and in vivo. Due to its upregulation in various cancers, telomerase is considered a potential target in cancer therapy. In this study, we identified...
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Antarctic marine bacterium Pseudoalteromonas sp. 22b as a source of cold adapted á-galaktosidase.
PublicationAntarktyczny morski szczep Pseudoalteromonas sp. 22b. jest źródłem wewnątrzkomórkowej beta-galaktozy. Enzym ten wykazuje wysoką aktywność hydrolizy laktozy w zakresie temperatur od 0 do 20 st. C oraz pH 6,0-8,0. W niniejszej pracy opisano metodykę uzyskania homogennego preparatu tego enzymu, oraz pełną charakterystykę jego własności enzymatycznych i kinetycznych.
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Solubilization of keratins and functional properties of their isolates and hydrolysates
PublicationThe keratinous wastes of the textile industry and poultry slaughterhouses may be used as sources of soluble keratins or hydrolysates. This review presents methods for processing raw keratin-based materials into bioproducts with functional and bioactive properties suitable for biomedical, cosmetic, food, and agricultural applications. Soluble keratin can be obtained by thermal treatment in some organic solvents, reduction, or oxidation...
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Hydrophobic derivatives of 2-amino-2-deoxy-D-glucitol-6-phosphate: a newtype of D-glucosamine-6-phosphate synthase inhibitors with antifungal action.
PublicationDokonano syntezy szeregu N-acylowych i estrowych pochodnych 2-amino-2-deok-sy-glucitolo-6-fosforanu (ADGP) i zbadano ich aktywność przeciwgrzybową oraz wobec enzymów zaangażowanych we wczesne etapy biosyntezy chityny w komórkach grzybów. Wszystkie badane pochodne okazały się słabszymi inhibitorami enzymu syntezy GlcN-6-P aniżeli ADGP, ale niektóre z nich wykazywały znacznie wyższą aktywność przeciwgrzybową niż związek macierzysty....