Efficient and regioselective one-step synthesis of 7-aryl-5-methyl- and 5-aryl-7-methyl-2-amino-[1,2,4]triazolo[1,5-a]pyrimidine derivatives

Exploring the cycloheptathiophene-3-carboxamide scaffold to disrupt the interactions of the influenza polymerase subunits and obtain potent anti-influenza activity

(2017) Jenny Desantis et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and biological evaluation of [1,2,4]triazolo[1,5-a]pyrimidines as potent lysine specific demethylase 1 (LSD1/KDM1A) inhibitors

(2017) Shuai Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design and Synthesis of Novel and Selective Phosphodiesterase 2 (PDE2a) Inhibitors for the Treatment of Memory Disorders

(2017) Laurent Gomez et al.   JOURNAL OF MEDICINAL CHEMISTRY

Alkoxy base-mediated selective synthesis and new rearrangements of 1,2,4-triazolodipyrimidinones

(2017) Dmitry A. Pyatakov et al.   TETRAHEDRON LETTERS

Application of 1,2,4-triazolo[1,5 -a ]pyrimidines for the design of coordination compounds with interesting structures and new biological properties

(2016) Iwona Łakomska et al.   COORDINATION CHEMISTRY REVIEWS

Synthesis and structure activity relationship investigation of triazolo[1,5-a]pyrimidines as CB2 cannabinoid receptor inverse agonists

(2016) Mojgan Aghazadeh Tabrizi et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and screening of triazolopyrimidine scaffold as multi-functional agents for Alzheimer's disease therapies

(2016) Jitendra Kumar et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Development of potent chemical antituberculosis agents targeting Mycobacterium tuberculosis acetohydroxyacid synthase

(2016) In-Pil Jung et al.   INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS

4,6-Diphenylpyridines as Promising Novel Anti-Influenza Agents Targeting the PA–PB1 Protein–Protein Interaction: Structure–Activity Relationships Exploration with the Aid of Molecular Modeling

(2016) Iuni M. L. Trist et al.   JOURNAL OF MEDICINAL CHEMISTRY

Polymerase Acidic Protein–Basic Protein 1 (PA–PB1) Protein–Protein Interaction as a Target for Next-Generation Anti-influenza Therapeutics

(2016) Serena Massari et al.   JOURNAL OF MEDICINAL CHEMISTRY

Tetrahydro-2-naphthyl and 2-Indanyl Triazolopyrimidines Targeting Plasmodium falciparum Dihydroorotate Dehydrogenase Display Potent and Selective Antimalarial Activity

(2016) Sreekanth Kokkonda et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of monomeric and dimeric steroids containing [1,2,4]triazolo[1,5-a]pyrimidines

(2016) Ailed Arenas-González et al.   STEROIDS

A Triazolopyrimidine-Based Dihydroorotate Dehydrogenase Inhibitor with Improved Drug-like Properties for Treatment and Prevention of Malaria

(2016) Margaret A. Phillips et al.   ACS Infectious Diseases

Novel agonists of benzodiazepine receptors: Design, synthesis, binding assay and pharmacological evaluation of 1,2,4-triazolo[1,5-a]pyrimidinone and 3-amino-1,2,4-triazole derivatives

(2015) Mehrdad Faizi et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Pharmacokinetic, pharmacodynamic and metabolic characterization of a brain retentive microtubule (MT)-stabilizing triazolopyrimidine

(2015) Anne-Sophie Cornec et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Novel Selective Inhibitor ofLeishmania (Leishmania) amazonensisArginase

(2015) Edson R. da Silva et al.   Chemical Biology & Drug Design

Reactivity of 2-amino[1,2,4]triazolo[1,5-а]-pyrimidines with various saturation of the pyrimidine ring towards electrophiles

(2015) Alexander V. Astakhov et al.   Chemistry of Heterocyclic Compounds

Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: Optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches

(2015) Boshi Huang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Evaluation of 1,2,4-Triazolo[1,5-a]pyrimidines as Antibacterial Agents Against Enterococcus faecium

(2015) Huan Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Broad Anti-influenza Hybrid Small Molecule That Potently Disrupts the Interaction of Polymerase Acidic Protein–Basic Protein 1 (PA-PB1) Subunits

(2015) Serena Massari et al.   JOURNAL OF MEDICINAL CHEMISTRY

Diversity Oriented Synthesis of Polycyclic Heterocycles through the Condensation of 2-Amino[1,2,4]triazolo[1,5-a]pyrimidines with 1,3-Diketones

(2015) Dmitry A. Pyatakov et al.   JOURNAL OF ORGANIC CHEMISTRY

Partially hydrogenated 2-amino[1,2,4]triazolo[1,5-a]pyrimidines as synthons for the preparation of polycondensed heterocycles: reaction with α-bromoketones

(2015) Victor M. Chernyshev et al.   TETRAHEDRON

Base-catalyzed one-step synthesis of 5,7-disubstituted-1,2,4-triazolo[1,5-a]pyrimidines

(2015) Xinhua He et al.   TETRAHEDRON LETTERS

Synthesis and Biological Evaluation of 3-Alkyl-1,5-Diaryl-1H-Pyrazoles as Rigid Analogues of Combretastatin A-4 with Potent Antiproliferative Activity

(2015) Qile Xu et al.   PLoS One

Highly Enantioselective Michael Addition of 2-Fluoro-1,3-diketones to Nitroalkenes

(2014) Jacek Kwiatkowski et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Optimization of Small-Molecule Inhibitors of Influenza Virus Polymerase: From Thiophene-3-Carboxamide to Polyamido Scaffolds

(2014) Susan Lepri et al.   JOURNAL OF MEDICINAL CHEMISTRY

Reactivity of C-Amino-1,2,4-triazoles toward Electrophiles: A Combined Computational and Experimental Study of Alkylation by Halogen Alkanes

(2014) Victor M. Chernyshev et al.   JOURNAL OF ORGANIC CHEMISTRY

Structural Investigation of Cycloheptathiophene-3-carboxamide Derivatives Targeting Influenza Virus Polymerase Assembly

(2013) Serena Massari et al.   JOURNAL OF MEDICINAL CHEMISTRY

Partially hydrogenated 2-amino[1,2,4]triazolo[1,5-a]pyrimidines as synthons for the preparation of polycondensed heterocycles: reaction with chlorocarboxylic acid chlorides

(2013) Victor M. Chernyshev et al.   TETRAHEDRON

Small molecule inhibitors of influenza A and B viruses that act by disrupting subunit interactions of the viral polymerase

(2012) G. Muratore et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Dotting the i's in three-component Biginelli-like condensations using 3-amino-1,2,4-triazole as a 1,3-binucleophile

(2012) Yuriy V. Sedash et al.   RSC Advances

Extending pKa prediction accuracy: High-throughput pKa measurements to understand pKa modulation of new chemical series

(2010) Francesca Milletti et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

In silicopKaPrediction and ADME Profiling

(2009) Gabriele Cruciani et al.   CHEMISTRY & BIODIVERSITY

Enantioselective Copper-Catalyzed Reductive Michael Cyclizations

(2009) Claire L. Oswald et al.   ORGANIC LETTERS

Identification of a PA-Binding Peptide with Inhibitory Activity against Influenza A and B Virus Replication

(2009) Kerstin Wunderlich et al.   PLoS One

2-amino-4,5,6,7-tetrahydro-1,2,4-triazolo[1,5-a]pyrimidines: Synthesis and reactions with electrophilic reagents

(2008) V. M. Chernyshev et al.   RUSSIAN JOURNAL OF ORGANIC CHEMISTRY