14-alpha Demethylase Inhibitors

Compounds that specifically inhibit STEROL 14-DEMETHYLASE. A variety of azole-derived ANTIFUNGAL AGENTS act through this mechanism.

Also Known As:

14alpha-Demethylase Inhibitors; CYP51 Inhibitors; Lanosterol 14 alpha-Demethylase Inhibitors; 14 alpha Demethylase Inhibitors; 14alpha Demethylase Inhibitors; Inhibitors, 14-alpha Demethylase; Inhibitors, 14alpha-Demethylase; Inhibitors, CYP51; Lanosterol 14 alpha Demethylase Inhibitors

Networked: 18 relevant articles (2 outcomes, 3 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Chemical Actions and Uses
- Pharmacologic Actions: 160

Experts

1.	Podust, Larissa M: 4 articles (03/2015 - 05/2008)
2.	Johnston, Jonathan B: 3 articles (03/2015 - 06/2010)
3.	McKerrow, James H: 3 articles (03/2015 - 06/2010)
4.	Choi, Jun Yong: 2 articles (03/2015 - 08/2014)
5.	Kellar, Danielle: 2 articles (03/2015 - 08/2014)
6.	Roush, William R: 2 articles (03/2015 - 08/2014)
7.	Vieira, Debora F: 2 articles (03/2015 - 08/2014)
8.	An, Ran: 1 article (04/2021)
9.	Guo, Chun: 1 article (04/2021)
10.	Guo, Meng-Bi: 1 article (04/2021)

Related Diseases

1.	Mycoses (Diseases, Fungus) 01/01/2021 - "The worldwide increase in the incidence of opportunistic fungal infections and the emerging resistance to available azole-based antifungal drugs, raise the need to develop structurally distinct and selective fungal CYP51 inhibitors. " 05/30/2008 - "This enzyme is a primary target in treatment of fungal infections in organisms ranging from humans to plants, and development of more potent and selective CYP51 inhibitors is an important biological objective. " 04/15/2021 - "Lead optimization generates selenium-containing miconazole CYP51 inhibitors with improved pharmacological profile for the treatment of fungal infections." 01/01/2019 - "Based on the analysis of the squalene cyclooxygenase (SE) and 14α-demethylase (CYP51) inhibitors pharmacophore feature and the dual-target active sites, a series of compounds with amide-pyridine scaffolds have been designed and synthesized to treat the increasing incidence of drug-resistant fungal infections. "
2.	Infections 01/01/2017 - "Here we performed a comparative investigation of two protozoon-specific CYP51 inhibitors, VNI and its CYP51 structure-based derivative VFV, in the murine models of infection caused by the Y strain of T. " 08/28/2014 - "CYP51 inhibitors have been developed to treat infections caused by fungi, and more recently the protozoan parasite Trypanosoma cruzi, the causative agent of Chagas disease. " 12/01/2016 - "Combining macrophages as host cells and Giemsa staining as the read-out, we demonstrate that posaconazole and other CYP51 inhibitors are unable to achieve complete clearance of an established T. cruzi infection in vitro in spite of the fact that these compounds are active at significantly lower concentrations than the reference drugs benznidazole and nifurtimox. "
3.	Chagas Disease (American Trypanosomiasis) 04/10/2018 - "Identification of Pyrazolo[3,4-e][1,4]thiazepin based CYP51 inhibitors as potential Chagas disease therapeutic alternative: In vitro and in vivo evaluation, binding mode prediction and SAR exploration." 04/16/2014 - "Nitroheterocyclic compounds are more efficacious than CYP51 inhibitors against Trypanosoma cruzi: implications for Chagas disease drug discovery and development." 12/01/2013 - "cruzi-specific CYP51 inhibitors can provide an immediate treatment for Chagas disease, either on their own or in combination with the currently available drugs." 12/01/2012 - "The research over the next few years will help define the role of CYP51 inhibitors, alone or in combination with other drugs, for managing patients with Chagas disease." 08/28/2014 - "CYP51 inhibitors have been developed to treat infections caused by fungi, and more recently the protozoan parasite Trypanosoma cruzi, the causative agent of Chagas disease. "
4.	Communicable Diseases (Infectious Diseases) 01/01/2022 - "Design, Synthesis, and Biological Evaluation of Dual-Target COX-2/CYP51 Inhibitors for the Treatment of Fungal Infectious Diseases." 11/08/2017 - "The study and development of azole-based CYP51 inhibitors is an active area of research across disciplines of biochemistry, pharmacology and infectious disease. "
5.	Amebiasis (Amoebiasis) 08/01/2015 - "In this study, we investigate the amebicidal activities of the pharmaceutical triazole CYP51 inhibitors fluconazole, itraconazole, and voriconazole against Acanthamoeba castellanii and Acanthamoeba polyphaga and assess their potential as therapeutic agents against Acanthamoeba infections in humans. "

Related Drugs and Biologics

1.	posaconazole
2.	Selenium
3.	Nifurtimox
4.	Miconazole (Monistat)
5.	benzonidazole (benznidazole)
6.	Azoles
7.	Voriconazole (Vfend)
8.	Itraconazole (Sporanox)
9.	Fluconazole (Zonal)
10.	Triazoles