Search Results - "Walczyński, Krzysztof"
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Guanidine Derivatives: How Simple Structural Modification of Histamine H3R Antagonists Has Led to the Discovery of Potent Muscarinic M2R/M4R Antagonists
Published in ACS chemical neuroscience (07-07-2021)“…This article describes the discovery of novel potent muscarinic receptor antagonists identified during a search for more active histamine H3 receptor (H3R)…”
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Synthesis and Biological Evaluation of Thiazole-Based Derivatives with Potential against Breast Cancer and Antimicrobial Agents
Published in International journal of molecular sciences (01-09-2022)“…Investigating novel, biologically-active coordination compounds that may be useful in the design of breast anticancer, antifungal, and antimicrobial agents is…”
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Metal-based compounds: Synthesis and characterization of new thiazole-based iridium and palladium complexes with potential anticancer and other biological activities
Published in Polyhedron (15-11-2024)“…Six new Pd(II) and Ir(III) thiazole-based complexes were synthesized and characterized by EA, ICP, FTIR, TGA-MS and SEM-EDX. In order to evaluate the…”
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4‑Oxypiperidine Ethers as Multiple Targeting Ligands at Histamine H3 Receptors and Cholinesterases
Published in ACS chemical neuroscience (20-03-2024)“…This study examines the properties of a novel series of 4-oxypiperidines designed and synthesized as histamine H3R antagonists/inverse agonists based on the…”
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Structures 4-n-propyl Piperazines as Non-Imidazole Histamine H3 Antagonists
Published in Materials (22-11-2021)“…Seven new low-temperature structures of 4-n-propylpiperazine derivatives, potential H3 receptor antagonists, have been determined by X-ray crystallography,…”
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Guanidines: Synthesis of Novel Histamine H3R Antagonists with Additional Breast Anticancer Activity and Cholinesterases Inhibitory Effect
Published in Pharmaceuticals (Basel, Switzerland) (30-04-2023)“…This study examines the properties of novel guanidines, designed and synthesized as histamine H3R antagonists/inverse agonists with additional pharmacological…”
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Non-Imidazole Histamine H₃ Ligands. Part VII. Synthesis, In Vitro and In Vivo Characterization of 5-Substituted-2-thiazol-4-n-propylpiperazines
Published in Molecules (Basel, Switzerland) (03-02-2018)“…H₃ receptors present on histaminergic and non-histaminergic neurons, act as autoreceptors or heteroreceptors controlling neurotransmitter release and…”
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Structure–Activity Relationships of New 1‐substitutedmethyl‐4‐[5‐( N ‐methyl‐ N ‐propylamino)pentyloxy]piperidines and Selected 1‐[( N ‐substituted‐ N‐ methyl)‐3‐propyloxy]‐5‐( N ‐methy‐l‐ N ‐propyl)‐pentanediamines as H 3 ‐Antagonists
Published in Chemical biology & drug design (01-01-2014)“…Novel, potent non‐imidazole histamine H 3 receptor antagonists have been prepared and in vitro tested as H 3 ‐receptor antagonists (the electrically evoked…”
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Search for multifunctional agents against Alzheimer’s disease among non-imidazole histamine H3 receptor ligands. In vitro and in vivo pharmacological evaluation and computational studies of piperazine derivatives
Published in Bioorganic chemistry (01-09-2019)“…[Display omitted] •Cholinesterase inhibition ability of fifty histamine H3 receptor ligands was assessed in vitro.•Four promising multi-target-directed ligands…”
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Loratadine analogues as MAGL inhibitors
Published in Bioorganic & medicinal chemistry letters (01-04-2015)“…[Display omitted] Compound 12a (JZP-361) acted as a potent and reversible inhibitor of human recombinant MAGL (hMAGL, IC50=46nM), and was found to have almost…”
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Synthesis and Preliminary Pharmacological Investigation of New N-Substituted-N-[ω-(ω-phenoxy-alkylpiperazin-1-yl)alkyl]guanidines as Non-Imidazole Histamine H3 Antagonists
Published in Archiv der Pharmazie (Weinheim) (01-06-2012)“…Novel, potent non‐imidazole histamine H3 receptor antagonists were prepared. Detailed structure–activity studies revealed that…”
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4-Hydroxypiperidines and Their Flexible 3-(Amino)propyloxy Analogues as Non-Imidazole Histamine H₃ Receptor Antagonist: Further Structure⁻Activity Relationship Exploration and In Vitro and In Vivo Pharmacological Evaluation
Published in International journal of molecular sciences (19-04-2018)“…Presynaptic histamine H₃ receptors (H₃R) act as auto- or heteroreceptors controlling, respectively, the release of histamine and of other neurotransmitters in…”
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Design, synthesis, and in vitro and in vivo characterization of 1-{4-[4-(substituted)piperazin-1-yl]butyl}guanidines and their piperidine analogues as histamine H 3 receptor antagonists
Published in MedChemComm (01-02-2019)“…Previously, we have shown that 1-substituted-[4-(7-phenoxyheptylpiperazin-1-yl)butyl]guanidine with electron withdrawing substituents at position 4 in the…”
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Non-imidazole histamine H 3 ligands: part V. synthesis and preliminary pharmacological investigation of 1-[2-thiazol-4-yl- and 1-[2-thiazol-5-yl-(2-aminoethyl)]-4- n -propylpiperazine derivatives
Published in Medicinal chemistry research (01-08-2013)“…Series of 1-[2-thiazol-4-yl-(2-aminoethyl)]- and 1-[2-thiazol-5-yl-(2-aminoethyl)]-4- -propylpiperazine derivatives have been prepared and in vitro tested as H…”
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Non-Imidazole Histamine H3 Ligands. Part VI. Synthesis and Preliminary Pharmacological Investigation of Thiazole-Type Histamine H3-Receptor Antagonists with Lacking a Nitrogen Nucleus in the Side Chain
Published in Medicinal chemistry (Shp-sariqah, United Arab Emirates) (01-02-2017)“…Antagonists to the H3 receptor are considered to be potential drugs for the treatment of Alzheimer's disease, attention deficit-hyperactive disorder, memory…”
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Novel pseudopolymorph of the active metabolite of perindopril
Published in Acta crystallographica. Section C, Crystal structure communications (01-09-2012)“…The dimethyl sulfoxide hemisolvate of perindoprilat [systematic name:…”
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Perindoprilat monohydrate
Published in Acta crystallographica. Section C, Crystal structure communications (01-11-2012)“…The title compound [systematic name: (1S)‐2‐((S)‐{1‐[(2S,3aS,7aS)‐2‐carboxyoctahydro‐1H‐indol‐1‐yl]‐1‐oxopropan‐2‐yl}azaniumyl)pentanoate monohydrate],…”
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Virtual Screening Approaches to Identify Promising Multitarget-Directed Ligands for the Treatment of Autism Spectrum Disorder
Published in Molecules (Basel, Switzerland) (07-11-2024)“…Autism spectrum disorder is a complex neurodevelopmental disorder. The available medical treatment options for autism spectrum disorder are very limited. While…”
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Non-imidazole histamine H3 ligands, Part IV: SAR of 1-[2-thiazol-5-yl-(2-aminoethyl)]-4-n-propylpiperazine derivatives
Published in European journal of medicinal chemistry (01-04-2009)“…A series of 1-[[2-thiazol-5-yl-(2-aminoethyl)]-4-n-propyl]piperazine derivatives have been prepared and in vitro tested as H(3)-receptor antagonists (the…”
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Preliminary studies of 1,5-benzoxazepine derivatives as potential histamine H 3 receptor antagonists
Published in Future medicinal chemistry (01-02-2024)“…Our research aimed to evaluate how the rigidification of the characteristic 3-aminopropyloxy linker by incorporating it into 1,5-benzoxazepines affects the…”
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