Search Results - "GREINER, Istvan"
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One-Step, Catalyst-Free Continuous-Flow Method for the Rapid and Safe Synthesis of 1‑Substituted 1H‑Tetrazoles
Published in Organic process research & development (20-09-2024)“…1-Substituted 1H-tetrazoles are valuable building blocks in medicinal chemistry; however, their limited synthetic accessibility constrains their use. A new…”
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2
Continuous Synthesis and Purification by Coupling a Multistep Flow Reaction with Centrifugal Partition Chromatography
Published in Angewandte Chemie International Edition (17-07-2017)“…Continuous‐flow multistep synthesis is combined with quasi‐continuous final‐product purification to produce pure products from crude reaction mixtures. In the…”
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3
Synthesis and Characterization of New V 1A Antagonist Compounds: The Separation of Four Atropisomeric Stereoisomers
Published in Journal of medicinal chemistry (22-07-2021)Get full text
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4
Biomimetic Synthesis of Drug Metabolites in Batch and Continuous‐Flow Reactors
Published in Chemistry : a European journal (02-07-2018)“…A medium‐throughput screening (MTS) of biomimetic drug metabolite synthesis is developed by using an iron porphyrin catalyst. The microplate method, in…”
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5
Discovery of novel steroidal histamine H 3 receptor antagonists/inverse agonists. Part 2. Versatile steroidal carboxamide derivatives
Published in Bioorganic & medicinal chemistry letters (15-10-2019)“…To further proceed with our previous work, novel steroid-based histamine H receptor antagonists were identified and characterized. Using an 'amine-to-amide'…”
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6
Discovery of novel steroidal histamine H 3 receptor antagonists/inverse agonists
Published in Bioorganic & medicinal chemistry letters (01-10-2017)“…Emerging from an HTS campaign, novel steroid-based histamine H receptor antagonists were identified and characterized. Structural moieties of the hit compounds…”
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7
“Greener” synthesis of bisphosphonic/dronic acid derivatives
Published in Green processing and synthesis (01-04-2014)“…According to literature, the synthesis of dronic acid derivatives from the corresponding carboxylic acids using phosphorus trichloride and phosphorous acid as…”
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8
The route from problem to solution in multistep continuous flow synthesis of pharmaceutical compounds
Published in Bioorganic & medicinal chemistry (01-12-2017)“…[Display omitted] Recent advances in the field of continuous flow chemistry allow the multistep preparation of complex molecules such as APIs (Active…”
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9
A Mechanistic Study on the Formation of Dronic Acids
Published in Molecules (Basel, Switzerland) (14-12-2021)“…Dronic acid derivatives, important drugs against bone diseases, may be synthesized from the corresponding substituted acetic acid either by reaction with…”
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10
Selective NR1/2B N-Methyl-d-aspartate Receptor Antagonists among Indole-2-carboxamides and Benzimidazole-2-carboxamides
Published in Journal of medicinal chemistry (08-03-2007)“…(4-Benzylpiperidine-1-yl)-(6-hydroxy-1H-indole-2-yl)-methanone (6a) derived from (E)-1-(4-benzylpiperidin-1-yl)-3-(4-hydroxy-phenyl)-propenone (5) was…”
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11
C-N Bond Formation by Consecutive Continuous-Flow Reductions towards A Medicinally Relevant Piperazine Derivative
Published in Molecules (Basel, Switzerland) (02-04-2021)“…A new, continuous-flow consecutive reduction method was developed for the C-N bond formation in the synthesis of the key intermediate of the antipsychotic drug…”
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12
Discovery of Novel Steroid-Based Histamine H3 Receptor Antagonists/Inverse Agonists
Published in Journal of medicinal chemistry (14-03-2024)“…Steroid-based histamine H3 receptor antagonists (d-homoazasteroids) were designed by combining distinct structural elements of HTS hit molecules. They were…”
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13
Discovery and Characterization of RGH-122, a Potent, Selective, and Orally Bioavailable V1a Receptor Antagonist
Published in Journal of medicinal chemistry (11-01-2024)“…The V1a receptor is a major contributor in mediating the social and emotional effects of arginine-vasopressin (AVP); therefore it represents a promising target…”
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14
Optimization of Novel α7 Nicotinic Acetylcholine Receptor Positive Allosteric Modulators and the Discovery of a Preclinical Development Candidate Molecule (RGH-560)
Published in Journal of medicinal chemistry (14-12-2023)“…During optimization of a previously identified lead compound, attempts were made to optimize the reactive indole structural element, the suboptimal metabolic…”
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15
Design, synthesis and biological evaluation of novel cyclic malonamide derivatives as selective RIPK1 inhibitors
Published in Bioorganic & medicinal chemistry letters (01-03-2024)“…[Display omitted] Receptor-interacting serine/threonine-protein kinase 1 (RIPK1) plays a key role in cell death and inflammation. RIPK1 is a well-established…”
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16
Harnessing dual-mode RIPK1 ligands for cross-species anti-necroptosis inhibitor compounds
Published in Bioorganic & medicinal chemistry letters (15-11-2024)“…[Display omitted] •Synthesis and biological evaluation of novel mixed type RIPK1 inhibitors.•Installation of a rigid acetylene moiety enhanced the…”
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17
Fragment Based Optimization of Metabotropic Glutamate Receptor 2 (mGluR2) Positive Allosteric Modulators in the Absence of Structural Information
Published in Journal of medicinal chemistry (10-01-2019)“…Metabotropic glutamate receptor 2 (mGluR2) positive allosteric modulators (PAMs) have been implicated as potential pharmacotherapy for psychiatric conditions…”
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18
Fragment-Based Optimization of Dihydropyrazino-Benzimidazolones as Metabotropic Glutamate Receptor‑2 Positive Allosteric Modulators against Migraine
Published in Journal of medicinal chemistry (24-06-2021)“…Our previous scaffold-hopping attempts resulted in dihydropyrazino-benzimidazoles as metabotropic glutamate receptor-2 (mGluR2) positive allosteric modulators…”
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19
Novel-Type GABAB PAMs: Structure–Activity Relationship in Light of the Protein Structure
Published in ACS medicinal chemistry letters (14-03-2024)“…Selecting a known HTS hit with the pyrazolo[1,5-a]pyrimidine core, our project was started from CMPPE, and its optimization was driven by a ligand-based…”
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Synthesis of Hydroxymethylenebisphosphonic Acid Derivatives in Different Solvents
Published in Molecules (Basel, Switzerland) (11-08-2016)“…The syntheses of hydroxymethylenebisphosphonic acid derivatives (dronic acid derivatives) starting from the corresponding substituted acetic acids and…”
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