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Structure-Based Consensus Scoring Scheme for Selecting Class A Aminergic GPCR Fragments
TLDR
Aminergic G-protein coupled receptors (GPRCs) represent well-known targets of central nervous-system related diseases. Expand
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Spiro[pyrrolidine-3,3′-oxindoles] and Their Indoline Analogues as New 5-HT6 Receptor Chemotypes
Synthetic derivatives of spiro[pyrrolidinyl-3,3′-oxindole] alkaloids (coerulescine analogues) were investigated as new ligands for aminergic G-protein coupled receptors (GPCRs). The chemical startingExpand
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The first synthesis of furo[2,3-c]pyridazin-4(1H)-one derivatives
Abstract We report a five step method for the synthesis of furo[2,3- c ]pyridazin-4(1 H )-one derivatives representing a novel heteroaromatic ring-system. The first synthesis of 3-carboxylic andExpand
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Spiro[pyrrolidine-3,3'-oxindoles] as 5-HT7 receptor ligands.
Here we report the design and synthesis of spiro[pyrrolidine-3,3'-oxindole] derivatives representing a novel scaffold of 5-HT7 receptor ligands. The synthesized analogues were validated as lowExpand
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Erratum to: A desirability function-based scoring scheme for selecting fragment-like class A aminergic GPCR ligands
TLDR
A physicochemical property-based desirability scoring scheme for fragment-based drug discovery was developed for class A aminergic GPCR targeted fragment libraries. Expand
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Fingerprint-Based Machine Learning Approach to Identify Potent and Selective 5-HT2BR Ligands
TLDR
The identification of subtype-selective GPCR (G-protein coupled receptor) ligands is a challenging task. Expand
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A desirability function-based scoring scheme for selecting fragment-like class A aminergic GPCR ligands
TLDR
A physicochemical property-based desirability scoring scheme for fragment-based drug discovery was developed for class A aminergic GPCR targeted fragment libraries. Expand
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Synthesis and Biochemical Evaluation of Lid-Open d-Amino Acid Oxidase Inhibitors
Most of the known inhibitors of d-amino acid oxidase (DAAO) are small polar molecules recognized by the active site of the enzyme. More recently a new class of DAAO inhibitors has been disclosed thatExpand
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