Synthesis and Biological Activity of Sterol 14α-Demethylase and Sterol C24-Methyltransferase Inhibitors

Synthesis and fungicidal activity of novel imidazole-based ketene dithioacetals

(2018) Stephane Jeanmart et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Sterol 14α-Demethylase Structure-Based Design of VNI ((R)-N-(1-(2,4-Dichlorophenyl)-2-(1H-imidazol-1-yl)ethyl)-4-(5-phenyl-1,3,4-oxadiazol-2-yl)benzamide)) Derivatives To Target Fungal Infections: Synthesis, Biological Evaluation, and Crystallographic Analysis

(2018) Laura Friggeri et al.   JOURNAL OF MEDICINAL CHEMISTRY

An overview of azoles targeting sterol 14α-demethylase for antileishmanial therapy

(2017) Saeed Emami et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

The Application of a Continuous Grignard Reaction in the Preparation of Fluconazole

(2017) Sudha Korwar et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Sterol methyltransferase a target for anti-amoeba therapy: towards transition state analog and suicide substrate drug design

(2017) Medhanie E. Kidane et al.   JOURNAL OF LIPID RESEARCH

Benznidazole and Posaconazole in Eliminating Parasites in Asymptomatic  T. Cruzi Carriers

(2017) Carlos A. Morillo et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

A convergent, scalable and stereoselective synthesis of azole CYP51 inhibitors

(2017) Galina Lepesheva et al.   TETRAHEDRON LETTERS

The Investigational Drug VT-1129 Is a Highly Potent Inhibitor of Cryptococcus Species CYP51 but Only Weakly Inhibits the Human Enzyme

(2016) Andrew G. S. Warrilow et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Evaluation of Parameters Impacting Drug Susceptibility in Intracellular Trypanosoma cruzi Assay Protocols

(2016) Gyongseon Yang et al.   SLAS Discovery

Novel Substrate Specificity and Temperature-Sensitive Activity of Mycosphaerella graminicola CYP51 Supported by the Native NADPH Cytochrome P450 Reductase

(2015) Claire L. Price et al.   APPLIED AND ENVIRONMENTAL MICROBIOLOGY

Fluorinated Sterols Are Suicide Inhibitors of Ergosterol Biosynthesis and Growth in Trypanosoma brucei

(2015) David J. Leaver et al.   CHEMISTRY & BIOLOGY

VFV as a New Effective CYP51 Structure-Derived Drug Candidate for Chagas Disease and Visceral Leishmaniasis

(2015) Galina I. Lepesheva et al.   JOURNAL OF INFECTIOUS DISEASES

Azole fungicides - understanding resistance mechanisms in agricultural fungal pathogens

(2015) Claire L Price et al.   PEST MANAGEMENT SCIENCE

Clotrimazole as a Potent Agent for Treating the Oomycete Fish Pathogen Saprolegnia parasitica through Inhibition of Sterol 14α-Demethylase (CYP51)

(2014) Andrew G. S. Warrilow et al.   APPLIED AND ENVIRONMENTAL MICROBIOLOGY

Design and optimization of highly-selective fungal CYP51 inhibitors

(2014) William J. Hoekstra et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Drug Strategies Targeting CYP51 in Neglected Tropical Diseases

(2014) Jun Yong Choi et al.   CHEMICAL REVIEWS

Discovery of an ergosterol-signaling factor that regulatesTrypanosoma bruceigrowth

(2014) Brad A. Haubrich et al.   JOURNAL OF LIPID RESEARCH

Randomized Trial of Posaconazole and Benznidazole for Chronic Chagas' Disease

(2014) Israel Molina et al.   NEW ENGLAND JOURNAL OF MEDICINE

C-24-methylation of 26-fluorocycloartenols by recombinant sterol C-24-methyltransferase from soybean: evidence for channel switching and its phylogenetic implications

(2013) Presheet Patkar et al.   BIOCHEMICAL JOURNAL

New Chemotherapeutic Strategies Against Malaria, Leishmaniasis and Trypanosomiases

(2013) M. Zucca et al.   CURRENT MEDICINAL CHEMISTRY

VNI Cures Acute and Chronic Experimental Chagas Disease

(2013) Fernando Villalta et al.   JOURNAL OF INFECTIOUS DISEASES

Azole Antimycotics - A Highway to New Drugs or a Dead End?

(2012) R. Musiol et al.   CURRENT MEDICINAL CHEMISTRY

Continuous-flow synthesis of activated vitamin D3 and its analogues

(2012) Shinichiro Fuse et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Estimating and Mapping the Population at Risk of Sleeping Sickness

(2012) Pere P. Simarro et al.   PLoS Neglected Tropical Diseases

CYP51 structures and structure-based development of novel, pathogen-specific inhibitory scaffolds

(2012) Tatiana Y. Hargrove et al.   International Journal for Parasitology-Drugs and Drug Resistance

Biosynthesis of Cholesterol and Other Sterols

(2011) W. David Nes   CHEMICAL REVIEWS

Structural complex of sterol 14α-demethylase (CYP51) with 14α-methylenecyclopropyl-Δ7-24, 25-dihydrolanosterol

(2011) Tatiana Y. Hargrove et al.   JOURNAL OF LIPID RESEARCH

Successful Treatment with Posaconazole of a Patient with Chronic Chagas Disease and Systemic Lupus Erythematosus

(2010) María-Jesús Pinazo et al.   AMERICAN JOURNAL OF TROPICAL MEDICINE AND HYGIENE

Mechanism of Binding of Prothioconazole toMycosphaerella graminicolaCYP51 Differs from That of Other Azole Antifungals

(2010) Josie E. Parker et al.   APPLIED AND ENVIRONMENTAL MICROBIOLOGY

Purification, characterization and inhibition of sterol C24-methyltransferase from Candida albicans

(2010) Kulothungan Ganapathy et al.   ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS

Cloning, mechanistic and functional analysis of a fungal sterol C24-methyltransferase implicated in brassicasterol biosynthesis

(2010) Maristela Pereira et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS

Structural Insights into Inhibition of Sterol 14α-Demethylase in the Human PathogenTrypanosoma cruzi

(2010) Galina I. Lepesheva et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Conazoles

(2010) Jan Heeres et al.   MOLECULES

Structural Characterization of CYP51 from Trypanosoma cruzi and Trypanosoma brucei Bound to the Antifungal Drugs Posaconazole and Fluconazole

(2010) Chiung-Kuang Chen et al.   PLoS Neglected Tropical Diseases

Cutaneous leishmaniasis treated with itraconazole

(2009) A. Baroni et al.   Dermatologic Therapy

Crystal Structures of Trypanosoma brucei Sterol 14α-Demethylase and Implications for Selective Treatment of Human Infections

(2009) Galina I. Lepesheva et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Steroidal Triterpenes: Design of Substrate-Based Inhibitors of Ergosterol and Sitosterol Synthesis

(2009) Jialin Liu et al.   MOLECULES

Cloning, functional expression and phylogenetic analysis of plant sterol 24C-methyltransferases involved in sitosterol biosynthesis

(2009) Anjanasree K. Neelakandan et al.   PHYTOCHEMISTRY

Identification of Three Classes of Heteroaromatic Compounds with Activity against Intracellular Trypanosoma cruzi by Chemical Library Screening

(2009) Esther Bettiol et al.   PLoS Neglected Tropical Diseases

Sterol 24-C-methyltransferase: An enzymatic target for the disruption of ergosterol biosynthesis and homeostasis in Cryptococcus neoformans

(2008) W. David Nes et al.   ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS

Synthesis and antifungal activity of 1,2,3-triazole containing fluconazole analogues

(2008) Nilkanth G. Aher et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

CYP51: A Major Drug Target in the Cytochrome P450 Superfamily

(2008) Galina I. Lepesheva et al.   LIPIDS

Antifungal agents – clinical pharmacokinetics and drug interactions

(2008) Hans-Peter Lipp   MYCOSES