New 1H-1,2,4-triazolyl derivatives as antimicrobial agents. Synthesis, biological evaluation and molecular docking
Chem Biodivers. 2024 Feb 29:e202400316. doi: 10.1002/cbdv.202400316. Online ahead of print.ABSTRACTThirteen new 1H-1,2,4-triazolyl derivatives were synthesized, and six of them were selected based on docking prediction for the investigation of their antimicrobial activity against five bacterial and eight fungal strains. All compounds demonstrated antibacterial activity with MIC lower than that of the ampicillin and chloramphenicol. In general, the most sensitive bacteria appeared to be P.fluorescens, while the plant pathogen X.campestris was the most resistant. The antifungal activity of the compounds was much better than ...
Source: Chemistry and Biodiversity - February 29, 2024 Category: Biochemistry Authors: Athina Athanasios Geronikaki Natalia Sucman Eugenia Stingaci Lucian Lupascu Anastasia Smetanscaia Vladimir Valica Livia Uncu Sergiu Shova Anthi Petrou Jasmina Glamo člija Marina Sockovic Fliur Macaev Source Type: research
Preparation, characterization, and evaluation of ketoconazole-loaded pineapple cellulose green nanofiber gel
In conclusion, ketoconazole-loaded pineapple nanofiber gel could be considered as a promising delivery system for topical applications.PMID:38365159 | DOI:10.1016/j.ijbiomac.2024.130221 (Source: International Journal of Biological Macromolecules)
Source: International Journal of Biological Macromolecules - February 16, 2024 Category: Biochemistry Authors: Pooja Rani Rimpy Pahwa Vikas Verma Meenakshi Bhatia Source Type: research
Preparation, characterization, and evaluation of ketoconazole-loaded pineapple cellulose green nanofiber gel
In conclusion, ketoconazole-loaded pineapple nanofiber gel could be considered as a promising delivery system for topical applications.PMID:38365159 | DOI:10.1016/j.ijbiomac.2024.130221 (Source: International Journal of Biological Macromolecules)
Source: International Journal of Biological Macromolecules - February 16, 2024 Category: Biochemistry Authors: Pooja Rani Rimpy Pahwa Vikas Verma Meenakshi Bhatia Source Type: research
Molecules, Vol. 29, Pages 864: Design, Synthesis, Antifungal Evaluation, Structure & ndash;Activity Relationship (SAR) Study, and Molecular Docking of Novel Spirotryprostatin A Derivatives
Molecules, Vol. 29, Pages 864: Design, Synthesis, Antifungal Evaluation, Structure–Activity Relationship (SAR) Study, and Molecular Docking of Novel Spirotryprostatin A Derivatives
Molecules doi: 10.3390/molecules29040864
Authors:
Yang-Min Ma
Xia Miao
Bin Jia
Zhao-Yang Sun
Si-Yue Ma
Cong Yan
Phytopathogenic fungi cause plant diseases and economic losses in agriculture. To efficiently control plant pathogen infections, a total of 19 spirotryprostatin A derivatives and 26 spirooxindole derivatives were designed, synthesized, and tested for their antifungal activity against ten plant pathogens. Add...
Source: Molecules - February 15, 2024 Category: Chemistry Authors: Yang-Min Ma Xia Miao Bin Jia Zhao-Yang Sun Si-Yue Ma Cong Yan Tags: Article Source Type: research
Steroidal hydrazones as antimicrobial agents: biological evaluation and molecular docking studies
SAR QSAR Environ Res. 2024 Feb;35(2):137-155. doi: 10.1080/1062936X.2024.2309183. Epub 2024 Feb 5.ABSTRACTMost of pharmaceutical agents display several or even many biological activities. It is obvious that testing even one compound for thousands of biological activities is a practically not reasonable task. Therefore, computer-aided prediction is the method of choice for the selection of the most promising bioassays for particular compounds. Using PASS Online software, we determined the probable antimicrobial activity of the 31 steroid derivatives. Experimental testing of the antimicrobial activity of the tested compounds...
Source: SAR and QSAR in Environmental Research - February 5, 2024 Category: Environmental Health Authors: M Merlani N Nadaraia N Barbakadze L Amiranashvili M Kakhabrishvili A Petrou T Carevi ć J Glamo člija A Geronikaki Source Type: research
Interaction of the antifungal ketoconazole and its diphenylphosphine derivatives with lipid bilayers: Insights into their antifungal action
Arch Biochem Biophys. 2024 Feb 1;753:109919. doi: 10.1016/j.abb.2024.109919. Online ahead of print.ABSTRACTKetoconazole (Ke) is an important antifungal drug, and two of its diphenylphosphinemethyl derivatives (KeP: Ph2PCH2-Ke and KeOP: Ph2P(O)CH2-Ke) have shown improved antifungal activity, namely against a yeast strain lacking ergosterol, suggesting alternative modes of action for azole compounds. In this context, the interactions of these compounds with a model of the cell membrane were investigated, using POPC (1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine) large unilamellar vesicles and taking advantage of the intri...
Source: Archives of Biochemistry and Biophysics - February 2, 2024 Category: Biochemistry Authors: Andreia Bento-Oliveira Rados ław Starosta Rodrigo F M de Almeida Source Type: research
The Efficacy of Ketoconazole Containing Regimens in Castration-Resistant Prostate Cancer: A Systematic Review and Meta-Analysis
Clin Genitourin Cancer. 2024 Jan 10:S1558-7673(24)00005-3. doi: 10.1016/j.clgc.2024.01.003. Online ahead of print.ABSTRACTCastration resistant prostate cancer (CRPC) is a challenging subset of prostate cancer associated with an extensive metastatic profile and high mortality. Ketoconazole is a nonselective steroid 17α-hydroxylase/17,20 lyase (CYP17A1) inhibitor and is employed as a second line treatment option for CRPC with an established efficacy profile in patients. The aim of this study is to assess the efficacy of ketoconazole containing regimens for CRPC in terms of prostate specific antigen (PSA) decline rate using ...
Source: Clinical Prostate Cancer - January 31, 2024 Category: Cancer & Oncology Authors: Obaid Ur Rehman Zain Ali Nadeem Eeshal Fatima Umar Akram Hiba Imran Ali Husnain Arsalan Nadeem Waqas Rasheed Source Type: research
Onychomycosis in Africa: Prevalence and Spectrum of Fungal Pathogens
AbstractPurpose of ReviewOnychomycosis is commonly reported in Africa, but data on its prevalence and spectrum of incriminated pathogens is fragmented in the literature. Understanding its epidemiology and profiling of the incriminated fungal pathogens would be very useful in managing patients as they are often difficult to treat, especially with the global emergence of antifungal resistance.Recent FindingsWe identified a total of 44 well-documented studies in 13 (24.1%) of the 54 African countries amounting to a total of 6773 cases of nail fungal infections: 4609 (68.0%) from North Africa, 1338 (19.6%) from West Africa, 52...
Source: Current Fungal Infection Reports - January 18, 2024 Category: Infectious Diseases Source Type: research
Physiologically ‐based pharmacokinetic modeling of prominent oral contraceptive agents and applications in drug–drug interactions
AbstractConsiderable interest remains across the pharmaceutical industry and regulatory landscape in capabilities to model oral contraceptives (OCs), whether combined (COCs) with ethinyl estradiol (EE) or progestin-only pill. Acceptance of COC drug –drug interaction (DDI) assessment using physiologically-based pharmacokinetic (PBPK) is often limited to the estrogen component (EE), requiring further verification, with extrapolation from EE to progestins discouraged. There is a paucity of published progestin component PBPK models to support th e regulatory DDI guidance for industry to evaluate a new chemical entity's (NCE'...
Source: CPT: Pharmacometrics and Systems Pharmacology - January 16, 2024 Category: Drugs & Pharmacology Authors: Gareth J. Lewis,
Deepak Ahire,
Kunal S. Taskar Tags: ARTICLE Source Type: research
Antifungal activity of the repurposed drug disulfiram against Cryptococcus neoformans
This study investigated the antifungal effects and the mechanism of action of DSF against C. neoformans to provide a new theoretical foundation for the treatment of Cryptococcal infections. In vitro studies demonstrated that DSF inhibited Cryptococcus growth at minimum inhibitory concentrations (MICs) ranging from 1.0 to 8.0 μg/mL. Combined antifungal effects have been observed for DSF with 5-fluorocytosine, amphotericin B, terbinafine, or ketoconazole. DSF exerts significant protective effects and synergistic effects combined with 5-FU for Galleria mellonella infected with C. neoformans. Mechanistic investigations showe...
Source: Frontiers in Pharmacology - January 11, 2024 Category: Drugs & Pharmacology Source Type: research
Exploring the Impact of CYP2D6 and UGT2B7 Gene-Drug Interactions, and CYP-mediated DDI on Oxycodone and Oxymorphone Pharmacokinetics using Physiologically-Based Pharmacokinetic Modelling and Simulation
Eur J Pharm Sci. 2024 Jan 1:106689. doi: 10.1016/j.ejps.2023.106689. Online ahead of print.ABSTRACTOxycodone is one of the most commonly used opioids to treat moderate to severe pain. It is metabolized mainly by CYP3A4 and CYP2D6, while only a small fraction of the dose is excreted unchanged into the urine. Oxymorphone, the metabolite primarily formed by CYP2D6, has a 40- to 60-fold higher mu-opioid receptor affinity than the parent compound. While CYP2D6-mediated gene-drug-interactions (GDIs) and drug-drug interactions (DDIs) are well-studied, they only account for a portion of the variability in oxycodone and oxymorphone...
Source: European Journal of Pharmaceutical Sciences - January 3, 2024 Category: Drugs & Pharmacology Authors: Marian Klose Rodrigo Cristofoletti Carolina de Miranda Silva Naveen Mangal Jacques Turgeon Veronique Michaud Lawrence J Lesko Stephan Schmidt Source Type: research
Prediction of drug-drug interactions between roflumilast and CYP3A4/1A2 perpetrators using a physiologically-based pharmacokinetic (PBPK) approach
This study aimed to develop a physiologically-based pharmacokinetic (PBPK) model to predict changes in the pharmacokinetics (PK) and pharmacodynamics (PD, PDE4 inhibition) of roflumilast (ROF) and ROF N-oxide when co-administered with eight CYP3A4/1A2 perpetrators. The population PBPK model of ROF and ROF N-oxide has been successfully developed and validated based on the four clinical PK studies and five clinical drug-drug interactions (DDIs) studies. In PK simulations, every ratio of prediction to observation for PK parameters fell within the range 0.7 to 1.5. In DDI simulations, except for tow peak concentration ratios (...
Source: BMC Pharmacology and Toxicology - January 3, 2024 Category: Drugs & Pharmacology Authors: Guangwei Jia Congcong Ren Hongyan Wang Caixia Fan Source Type: research
GSE248987 Antifungal activity of the repurposed drug disulfiram against Cryptococcus neoformans.
This study investigated the antifungal effect and mechanism of DSF againstC. neoformansto provide a new theoretical foundation for treating Cryptococcal infections. In vitro studies demonstrated that DSF inhibitedCryptococcusat minimum inhibitory concentrations (MICs) ranging from 1.0 to 8.0 μg/mL. Combined antifungal effects were also observed with 5-fluorocytosine, amphotericin B, terbinafine, or ketoconazole. In vivo, DSF exerted asignificantprotectiveeffectforGalleria mellonella infected with C. neoformans.Mechanistic investigations showed that DSF dose-dependently inhibited the me lanin, urease, acetaldehyde dehydrog...
Source: GEO: Gene Expression Omnibus - December 31, 2023 Category: Genetics & Stem Cells Tags: Expression profiling by high throughput sequencing Cryptococcus neoformans Source Type: research
Physiologically Based Pharmacokinetic Modelling of Prominent Oral Contraceptive Agents and Applications in Drug ‐Drug Interactions
AbstractConsiderable interest remains across the pharmaceutical industry and regulatory landscape in capabilities to model oral contraceptives (OCs), whether combined (COCs) with ethinyl estradiol (EE) or progestin-only pill (PoP). Acceptance of COC drug-drug interaction (DDI) assessment using PBPK is often limited to the estrogen component (EE), requiring further verification, with extrapolation from EE to progestins discouraged. There is a paucity of published progestin component PBPK models to support the regulatory DDI guidance for industry to evaluate a new chemical entity's (NCE) DDI potential with COCs. Guidance rec...
Source: CPT: Pharmacometrics and Systems Pharmacology - December 22, 2023 Category: Drugs & Pharmacology Authors: Gareth J. Lewis,
Deepak Ahire,
Kunal S. Taskar Tags: ARTICLE Source Type: research
