Synthesis, structure-activity relationship and biological evaluation of indole derivatives as anti-Candida albicans agents
Bioorg Chem. 2024 Mar 16;146:107293. doi: 10.1016/j.bioorg.2024.107293. Online ahead of print.ABSTRACTIn this work, we synthesized a series of indole derivatives to cope with the current increasing fungal infections caused by drug-resistant Candida albicans. All compounds were evaluated for antifungal activities against Candida albicans in vitro, and the structure-activity relationships (SARs) were analyzed. The results indicated that indole derivatives used either alone or in combination with fluconazole showed good activities against fluconazole-resistant Candida albicans. Further mechanisms studies demonstrated that com...
Source: Bioorganic Chemistry - March 20, 2024 Category: Chemistry Authors: Yandan Wu Aimei Sun Fei Chen Yin Zhao Xianhu Zhu Tianbao Zhang Guanghui Ni Ruirui Wang Source Type: research
Synthesis, structure-activity relationship and biological evaluation of indole derivatives as anti-Candida albicans agents
Bioorg Chem. 2024 Mar 16;146:107293. doi: 10.1016/j.bioorg.2024.107293. Online ahead of print.ABSTRACTIn this work, we synthesized a series of indole derivatives to cope with the current increasing fungal infections caused by drug-resistant Candida albicans. All compounds were evaluated for antifungal activities against Candida albicans in vitro, and the structure-activity relationships (SARs) were analyzed. The results indicated that indole derivatives used either alone or in combination with fluconazole showed good activities against fluconazole-resistant Candida albicans. Further mechanisms studies demonstrated that com...
Source: Bioorganic Chemistry - March 20, 2024 Category: Chemistry Authors: Yandan Wu Aimei Sun Fei Chen Yin Zhao Xianhu Zhu Tianbao Zhang Guanghui Ni Ruirui Wang Source Type: research
Evaluating cardiac disorders associated with triazole antifungal agents based on the US Food and Drug Administration Adverse Event reporting system database
Conclusion:Isavuconazole might be the safest of the five TAAs for cardiac AEs. TAA-associated cardiac disorders may result in serious adverse outcomes. Therefore, in addition to AEs on the drug label, we should pay attention to new AEs unrecorded on the drug label during the clinical use of TAAs. (Source: Frontiers in Pharmacology)
Source: Frontiers in Pharmacology - March 20, 2024 Category: Drugs & Pharmacology Source Type: research
Comparing the efficacy of fluconazole and cryotherapy Versus cryotherapy alone on treating cutaneous leishmaniasis: a triple-blind randomized clinical trial
This study aimed t... (Source: BMC Infectious Diseases)
Source: BMC Infectious Diseases - March 20, 2024 Category: Infectious Diseases Authors: Ahmad Reza Parhizkar, Mehdi Sharafi, Susan Mansuri, Maryam Hadibarhaghtalab, Sima Afrashteh, Hossein Fatemian and Mahsa Rostami Chijan Tags: Research Source Type: research
Evaluation of the Vitek 2 system for antifungal susceptibility testing of Candida auris using a representative international panel of clinical isolates: overestimation of amphotericin B resistance and underestimation of fluconazole resistance
Journal of Clinical Microbiology, Ahead of Print. (Source: Journal of Clinical Microbiology)
Source: Journal of Clinical Microbiology - March 19, 2024 Category: Microbiology Authors: Maria SiopiIoannis PachoulisSevasti LeventakiBram SpruijtenburgJacques F. MeisSpyros PournarasGeorgia VrioniAthanasios TsakrisJoseph Meletiadis1Clinical Microbiology Laboratory, “Attikon” University General Hospital, Medical School, National and Kapod Source Type: research
Antifungal therapy for the treatment of CNS infections
AbstractPurpose of reviewA review of existing and emerging therapies for the treatment of fungal infections of the CNS is presented, highlighting more recent studies. Newly authorized and emerging therapies and the data surrounding their use are also introduced.Recent findingsEarly data suggests Ibrexafungerp, a newly released antifungal for the treatment of vulvovaginal candidiasis, does not have a significant role in the treatment of CNS infections. Combination therapy including therapy with terbinafine appears promising for difficult-to-treat fungal infections of the CNS. Antifungal treatment remains pathogen-specific b...
Source: Current Fungal Infection Reports - March 16, 2024 Category: Infectious Diseases Source Type: research
A physiologically ‐based pharmacokinetic/pharmacodynamic modeling approach for drug–drug‐gene interaction evaluation of S‐warfarin with fluconazole
This study provides a whole-body physiologically-based pharmacokinetic/PD (PBPK/PD) model of S-warfarin for predicting the effects of drug–drug−gene interactions on S-warfarin PKs and PDs. The PBPK/PD model of S-warfarin was developed in PK-Sim and MoBi. Drug-depende nt parameters were obtained from the literature or optimized. Of the 34 S-warfarin plasma concentration-time profiles used, 96% predicted plasma concentrations within twofold range compared to observed data. For S-warfarin plasma concentration-time profiles withCYP2C9 genotype, 364 of 386 predicted plasma concentration values (~94%) fell within the twofold...
Source: CPT: Pharmacometrics and Systems Pharmacology - March 15, 2024 Category: Drugs & Pharmacology Authors: Kuo Geng,
Chaozhuang Shen,
Xiaohu Wang,
Xingwen Wang,
Wenxin Shao,
Wenhui Wang,
Tao Chen,
Hua Sun,
Haitang Xie Tags: ARTICLE Source Type: research
Natural Isatin Derivatives Against Black Fungus: In Silico Studies
Curr Microbiol. 2024 Mar 12;81(5):113. doi: 10.1007/s00284-024-03621-z.ABSTRACTDuring this coronavirus pandemic, when a lot of people are already severely afflicted with SARS-CoV-19, the dispersion of black fungus is making it worse, especially in the Indian subcontinent. Considering this situation, the idea for an in silico study to identify the potential inhibitor against black fungal infection is envisioned and computational analysis has been conducted with isatin derivatives that exhibit considerable antifungal activity. Through this in silico study, several pharmacokinetics properties like absorption, distribution, me...
Source: Current Microbiology - March 13, 2024 Category: Microbiology Authors: Md Saddam Hossain Md Anisur Rahman Prithbey Raj Dey Md Parvez Khandocar Md Yeakub Ali Mahajabin Snigdha Henrique Douglas Melo Coutinho Muhammad Torequl Islam Source Type: research
Natural Isatin Derivatives Against Black Fungus: In Silico Studies
Curr Microbiol. 2024 Mar 12;81(5):113. doi: 10.1007/s00284-024-03621-z.ABSTRACTDuring this coronavirus pandemic, when a lot of people are already severely afflicted with SARS-CoV-19, the dispersion of black fungus is making it worse, especially in the Indian subcontinent. Considering this situation, the idea for an in silico study to identify the potential inhibitor against black fungal infection is envisioned and computational analysis has been conducted with isatin derivatives that exhibit considerable antifungal activity. Through this in silico study, several pharmacokinetics properties like absorption, distribution, me...
Source: Current Microbiology - March 13, 2024 Category: Microbiology Authors: Md Saddam Hossain Md Anisur Rahman Prithbey Raj Dey Md Parvez Khandocar Md Yeakub Ali Mahajabin Snigdha Henrique Douglas Melo Coutinho Muhammad Torequl Islam Source Type: research
Physiologically based pharmacokinetic modeling to predict the clinical effect of azole antifungal agents as CYP3A inhibitors on azelnidipine pharmacokinetics
In this study, a physiologically based pharmacokinetic (PBPK) model of the cytochrome P450 3A (CYP3A) substrate azelnidipine was developed using in vitro and clinical data to predict the effects of azole antifungals on azelnidipine pharmacokinetics. Modeling and simulations were conducted using the Simcyp™ PBPK simulator. The azelnidipine model consisted of a full PBPK model and a first-order absorption model. CYP3A was assumed as the only azelnidipine elimination route, and CYP3A clearance was optimized using the pharmacokinetic profile of single-dose 5-mg azelnidipine in healthy participants. The model reproduced the r...
Source: Drug Metabolism and Pharmacokinetics - March 8, 2024 Category: Drugs & Pharmacology Authors: Akiko Watanabe Masakatsu Kotsuma Source Type: research
