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Fragment-Based Discovery of 2-Aminoquinazolin-4(3H)-ones As Novel Class Nonpeptidomimetic Inhibitors of the Plasmepsins I, II, and IV.
2-Aminoquinazolin-4(3H)-ones were identified as a novel class of malaria digestive vacuole plasmepsin inhibitors by using NMR-based fragment screening against Plm II. Initial fragment hitExpand
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Plasmodium subtilisin-like protease 1 (SUB1): Insights into the active-site structure, specificity and function of a pan-malaria drug target
Release of the malaria merozoite from its host erythrocyte (egress) and invasion of a fresh cell are crucial steps in the life cycle of the malaria pathogen. Subtilisin-like protease 1 (SUB1) is aExpand
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Virtual Screening for Selective Allosteric mGluR1 Antagonists and Structure–Activity Relationship Investigations for Coumarine Derivatives
A virtual screening study towards novel noncompetitive antagonists of the metabotropic glutamate receptor 1 (mGluR1) is described. Alignment‐free topological pharmacophore descriptors (CATS) wereExpand
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Amino-alkyl-cyclohexanes as a novel class of uncompetitive NMDA receptor antagonists.
Because of its widespread involvement in the physiology and pathology of the CNS, the glutamatergic system has gained considerable attention as a potential target for development of new agents for aExpand
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Ether-directed diastereoselectivity in catalysed Overman rearrangement : comparative studies of metal catalysts
Abstract Ether-directed diastereoselectivity in Overman rearrangement of δ-methoxy and δ-TBDMSO substituted allylic trichloroacetimidates has been explored using PtCl 2 , PtCl 4 , AuCl and AuCl 3Expand
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A novel class of amino-alkylcyclohexanes as uncompetitive, fast, voltage-dependent, N-methyl-D-aspartate (NMDA) receptor antagonists – in vitro characterization
SummaryThe fact that potent NMDA receptor channel blockers produce phencyclidine-like psychotropic symptoms in man and rodents implies that uncompetitive antagonism of NMDA receptors may not be aExpand
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Tetrahydro-1,3-oxazepines via Intramolecular Amination of Cyclopropylmethyl Cation.
An efficient synthesis of tetrahydro-1,3-oxazepines was developed involving the regioselective intramolecular amination of cyclopropylmethyl cation. The cation was generated by the abstraction of oneExpand
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A Polymorphism in leuS Confers Reduced Susceptibility to GSK2251052 in a Clinical Isolate of Staphylococcus aureus
ABSTRACT GSK2251052 is a broad-spectrum antibacterial inhibitor of leucyl tRNA-synthetase (LeuRS) that has been evaluated in phase II clinical trials. Here, we report the identification of a clinicalExpand
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EU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology
Compound screening in biological assays and subsequent optimization of hits is indispensable for the development of new molecular research tools and drug candidates. To facilitate such discoveries,Expand
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Quinoxaline-Based Inhibitors of Malarial Protease PfSUB1*
2,3-Bis(phenylamino)quinoxalines have been identified as a novel class of malarial protease PfSUB1 inhibitors by screening of Malaria Box compounds. The synthesis of analog series and investigationExpand
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