Strategies of targeting CYP51 for IFIs therapy: Emerging prospects, opportunities and challenges

R Zhang, Y Wang, A Wu, J Wang, J Zhang - European Journal of Medicinal …, 2023 - Elsevier
CYP51, a monooxygenase associated with the sterol synthesis pathway, is responsible for
the catalysis of the 14-methyl hydroxylation reaction of lanosterol precursors. This enzyme is …

Roles for structural biology in the discovery of drugs and agrochemicals targeting sterol 14α-demethylases

BC Monk, MV Keniya - Journal of Fungi, 2021 - mdpi.com
Antifungal drugs and antifungal agrochemicals have significant limitations. These include
several unintended consequences of their use including the growing importance of intrinsic …

Pyrimidinetrione‐imidazoles as a Unique Structural Type of Potential Agents towards Candida Albicans: Design, Synthesis and Biological Evaluation

YF Sui, MF Ansari, CH Zhou - Chemistry–An Asian Journal, 2021 - Wiley Online Library
Substantial morbidity and mortality of fungal infections have aroused concerns all over the
world, and common Candida spp. currently bring about severe systemic infections. A series …

Design, synthesis, and activity evaluation of novel dual-target inhibitors with antifungal and immunoregulatory properties

B Sun, W Liu, Q Wang, Y Liu, S Yu… - Journal of Medicinal …, 2023 - ACS Publications
Dual-target (CYP51/PD-L1) plays an important role in the process of fungal proliferation and
immune suppression. A series of novel quinazoline compounds with dual-target inhibition …

Construction and Evaluation of Novel Dual-function Antifungal Inhibitors and Covalent Organic Framework Carriers Based on the Infection Microenvironment

Y Liu, Q Wang, S Yu, M Liu, J Han… - Journal of Medicinal …, 2023 - ACS Publications
In this study, PD-L1 and CYP51 were selected as key dual-target enzymes, which play an
important role in the process of fungal proliferation and immune suppression. A series of …

Molecular insights into human transmembrane protease serine-2 (TMPS2) inhibitors against SARS-CoV2: homology modelling, molecular dynamics, and docking …

SM Kishk, RM Kishk, ASA Yassen, MS Nafie, NA Nemr… - Molecules, 2020 - mdpi.com
The severe acute respiratory syndrome coronavirus 2 (SARS-CoV2), which caused novel
corona virus disease-2019 (COVID-19) pandemic, necessitated a global demand for studies …

Synthesis, biological evaluation and computational studies of pyrazole derivatives as Mycobacterium tuberculosis CYP121A1 inhibitors

LA Alshabani, A Kumar, SJ Willcocks… - RSC Medicinal …, 2022 - pubs.rsc.org
A series of imidazole and triazole diarylpyrazole derivatives were prepared using an efficient
5-step synthetic scheme and evaluated for binding affinity with Mycobacterium tuberculosis …

[HTML][HTML] 4th generation nonsteroidal aromatase inhibitors: An iterative SAR-guided design, synthesis, and biological evaluation towards picomolar dual binding …

AG Eissa, D Barrow, J Gee, LE Powell… - European Journal of …, 2022 - Elsevier
One in every eight women will be diagnosed with breast cancer during their lifetime and
approximately 70% of all patients are oestrogen receptor (ER) positive depending upon …

Synthesis, optimization, antifungal activity, selectivity, and CYP51 binding of new 2-Aryl-3-azolyl-1-indolyl-propan-2-ols

N Lebouvier, F Pagniez, YM Na, D Shi, P Pinson… - Pharmaceuticals, 2020 - mdpi.com
A series of 2-aryl-3-azolyl-1-indolyl-propan-2-ols was designed as new analogs of
fluconazole (FLC) by replacing one of its two triazole moieties by an indole scaffold. Two …

Design, Synthesis, and Evaluation of Quinoline‐1,2,3‐Triazole Hybrids as CYP51 Inhibitors: In Silico Study and In Vitro Antimicrobial Assessment

BK Chabhadiya, HN Naik, BA Mohite, I Ahmad… - …, 2024 - Wiley Online Library
Novel Quinoline‐triazole hybrid derivatives (9 a–9 l) were designed and synthesized via
click reaction methodology to develop lead compounds with good antibacterial and …