Pyrimidine-based antimalarials: design strategies and antiplasmodial effects

Quinoline-based antimalarial hybrid compounds

(2015) Stéphanie Vandekerckhove et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Ferrocene-pyrimidine conjugates: Synthesis, electrochemistry, physicochemical properties and antiplasmodial activities

(2015) Rakesh Chopra et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Primaquine–pyrimidine hybrids: Synthesis and dual-stage antiplasmodial activity

(2015) Hardeep Kaur et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids

(2015) Hardeep Kaur et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

4-Aminoquinoline-Pyrimidine hybrids: Synthesis, antimalarial activity, heme binding and docking studies

(2015) Deepak Kumar et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Genetic Diversity and Protective Efficacy of the RTS,S/AS01 Malaria Vaccine

(2015) Daniel E. Neafsey et al.   NEW ENGLAND JOURNAL OF MEDICINE

4-Aminoquinoline-pyrimidine-aminoalkanols: synthesis, in vitro antimalarial activity, docking studies and ADME predictions

(2015) Mohit Tripathi et al.   NEW JOURNAL OF CHEMISTRY

Highly active 4-aminoquinoline–pyrimidine based molecular hybrids as potential next generation antimalarial agents

(2015) Sunny Manohar et al.   RSC Advances

Pharmacokinetic Interactions between Primaquine and Chloroquine

(2014) Sasithon Pukrittayakamee et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Antimalarials in Development in 2014

(2014) David S. Barnett et al.   CHEMICAL REVIEWS

Ferroquine as an Oxidative Shock Antimalarial

(2014) Daniel Dive et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Development of potent and selective Plasmodium falciparum calcium-dependent protein kinase 4 (PfCDPK4) inhibitors that block the transmission of malaria to mosquitoes

(2014) Rama Subba Rao Vidadala et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Tetraoxane–Pyrimidine Nitrile Hybrids as Dual Stage Antimalarials

(2014) Rudi Oliveira et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of piperazine tethered 4-aminoquinoline-pyrimidine hybrids as potent antimalarial agents

(2014) Anuj Thakur et al.   RSC Advances

Synthesis, antimalarial activity, heme binding and docking studies of 4-aminoquinoline–pyrimidine based molecular hybrids

(2014) Deepak Kumar et al.   RSC Advances

The Ferroquine Antimalarial Conundrum: Redox Activation and Reinvasion Inhibition

(2013) Faustine Dubar et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Recent advances in malaria drug discovery

(2013) Marco A. Biamonte et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

An Endoperoxide-Based Hybrid Approach to Deliver Falcipain Inhibitors Inside Malaria Parasites

(2013) Rudi Oliveira et al.   ChemMedChem

Recent Developments in Rationally Designed Multitarget Antiprotozoan Agents

(2013) P. M. Njogu et al.   CURRENT MEDICINAL CHEMISTRY

Synthesis of 4-aminoquinoline–pyrimidine hybrids as potent antimalarials and their mode of action studies

(2013) Kamaljit Singh et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Regioselective synthesis of 6-substituted-2-amino-5-bromo-4(3H)-pyrimidinones and evaluation of their antiviral activity

(2013) Kamaljit Singh et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Highly Regioselective Addition of Organozinc Reagents to 2-Oxo-1,2-dihydropyrimidine-5-carboxylates Activated by BF3·OEt2: Synthesis of 2-Oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylates

(2013) Kamaljit Singh et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

A Randomized Comparison of Dihydroartemisinin-Piperaquine and Artesunate-Amodiaquine Combined With Primaquine for Radical Treatment of Vivax Malaria in Sumatera, Indonesia

(2013) A. P. Pasaribu et al.   JOURNAL OF INFECTIOUS DISEASES

Quinoline–Pyrimidine Hybrids: Synthesis, Antiplasmodial Activity, SAR, and Mode of Action Studies

(2013) Kamaljit Singh et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pharmacokinetics of Ferroquine, a Novel 4-Aminoquinoline, in Asymptomatic Carriers of Plasmodium falciparum Infections

(2012) Christian Supan et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Pyrido[1,2-a]pyrimidin-4-ones as antiplasmodial falcipain-2 inhibitors

(2012) U.R. Mane et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis, characterization and antimalarial activity of quinoline–pyrimidine hybrids

(2012) Stefan I. Pretorius et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Highly regioselective synthesis of N-3 organophosphorous derivatives of 3,4-dihydropyrimidin-2(1H)-ones and their calcium channel binding studies

(2012) Kamaljit Singh et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

2-Aminopyrimidine based 4-aminoquinoline anti-plasmodial agents. Synthesis, biological activity, structure–activity relationship and mode of action studies

(2012) Kamaljit Singh et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Factors Influencing the Specificity of Inhibitor Binding to the Human and Malaria Parasite Dihydroorotate Dehydrogenases

(2012) Paul T. P. Bedingfield et al.   JOURNAL OF MEDICINAL CHEMISTRY

Virtual Screening and Optimization Yield Low-Nanomolar Inhibitors of the Tautomerase Activity of Plasmodium falciparum Macrophage Migration Inhibitory Factor

(2012) Markus K. Dahlgren et al.   JOURNAL OF MEDICINAL CHEMISTRY

Bioisosteric Transformations and Permutations in the Triazolopyrimidine Scaffold To Identify the Minimum Pharmacophore Required for Inhibitory Activity against Plasmodium falciparum Dihydroorotate Dehydrogenase

(2012) Alka Marwaha et al.   JOURNAL OF MEDICINAL CHEMISTRY

Tuning and predicting biological affinity: aryl nitriles as cysteine protease inhibitors

(2012) Veronika Ehmke et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

A Plasmodium-encoded cytokine suppresses T-cell immunity during malaria

(2012) T. Sun et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Malarial dihydrofolate reductase as a paradigm for drug development against a resistance-compromised target

(2012) Y. Yuthavong et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Chemical resolution of enantiomers of 3,4-dihydropyrimidin-2(1H)-ones using chiral auxiliary approach

(2012) Kamaljit Singh et al.   TETRAHEDRON

Facile transformation of Biginelli pyrimidin-2(1H)-ones to pyrimidines. In vitro evaluation as inhibitors of Mycobacterium tuberculosis and modulators of cytostatic activity

(2011) Kamaljit Singh et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Structure-Guided Lead Optimization of Triazolopyrimidine-Ring Substituents Identifies PotentPlasmodium falciparumDihydroorotate Dehydrogenase Inhibitors with Clinical Candidate Potential

(2011) Jose M. Coteron et al.   JOURNAL OF MEDICINAL CHEMISTRY

Peptidomimetic nitriles as selective inhibitors for the malarial cysteine protease falcipain-2

(2011) Veronika Ehmke et al.   MedChemComm

The Antimalarial Ferroquine: Role of the Metal and Intramolecular Hydrogen Bond in Activity and Resistance

(2010) Faustine Dubar et al.   ACS Chemical Biology

Falcipain Inhibitors: Optimization Studies of the 2-Pyrimidinecarbonitrile Lead Series†

(2010) Jose M. Coterón et al.   JOURNAL OF MEDICINAL CHEMISTRY

Spectroscopic studies on the thermodynamic and thermal denaturation of the ct-DNA binding of methylene blue

(2010) Mudasir et al.   SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY

Regioselective addition reactions at C-2 of 3,4-dihydropyrimidinones. Synthesis and evaluation of multifunctionalized tetrahydropyrimidines

(2010) Kamaljit Singh et al.   TETRAHEDRON

Drug-Resistant Malaria: The Era of ACT

(2010) Jessica T. Lin et al.   Current Infectious Disease Reports

Hybrid Drugs for Malaria

(2009) J. Walsh et al.   CURRENT PHARMACEUTICAL DESIGN

Recent developments in the design and synthesis of hybrid molecules basedon aminoquinoline ring and their antiplasmodial evaluation

(2009) Vladimir V. Kouznetsov et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

An Efficacious Protocol for 4-Substituted 3,4-Dihydropyrimidinones: Synthesis and Calcium Channel Binding Studies

(2009) Kamaljit Singh et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Identification of a Metabolically Stable Triazolopyrimidine-Based Dihydroorotate Dehydrogenase Inhibitor with Antimalarial Activity in Mice

(2009) Ramesh Gujjar et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Tautomerase-Null Macrophage Migration-Inhibitory Factor (MIF) Gene Knock-In Mouse Model Reveals That Protein Interactions and Not Enzymatic Activity Mediate MIF-Dependent Growth Regulation

(2009) G. Fingerle-Rowson et al.   MOLECULAR AND CELLULAR BIOLOGY

Artemisinin Resistance inPlasmodium falciparumMalaria

(2009) Arjen M. Dondorp et al.   NEW ENGLAND JOURNAL OF MEDICINE

Chemical resolution of inherently racemic dihydropyrimidinones via a site selective functionalization of Biginelli compounds with chiral electrophiles: a case study

(2009) Kamaljit Singh et al.   TETRAHEDRON

Magnesium/methanol: an effective reducing agent for chemoselective reduction of pyrimidine-2(1H)-ones

(2009) Kamaljit Singh et al.   TETRAHEDRON LETTERS

New chemotypes for cathepsin K inhibitors

(2008) Naoki Teno et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

N1-Alkylated 3,4-dihydropyrimidine-2(1H)-ones: Convenient one-pot selective synthesis and evaluation of their calcium channel blocking activity

(2008) Kamaljit Singh et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Development of Potent Purine-Derived Nitrile Inhibitors of the Trypanosomal Protease TbcatB

(2008) Jeremy P. Mallari et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Human Macrophage Migration Inhibitory Factor (MIF)-CD74 Antagonists via Virtual Screening

(2008) Zoe Cournia et al.   JOURNAL OF MEDICINAL CHEMISTRY

Investigation of the Redox Behavior of Ferroquine, a New Antimalarial

(2008) Natascha Chavain et al.   MOLECULAR PHARMACEUTICS

Evidence of Artemisinin-Resistant Malaria in Western Cambodia

(2008) Harald Noedl et al.   NEW ENGLAND JOURNAL OF MEDICINE

Unprecedented single-pot protocol for the synthesis of N1, C6-linked bicyclic 3,4-dihydropyrimidinones via lithiation of Biginelli compounds

(2008) Kamaljit Singh et al.   TETRAHEDRON

Hybrid Molecules with a Dual Mode of Action: Dream or Reality?†

(2007) Bernard Meunier   ACCOUNTS OF CHEMICAL RESEARCH