Synthesis and Pharmacological Evaluation of Fluorinated Quinoxaline‐Based κ‐Opioid Receptor (KOR) Agonists Designed for PET Studies
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DOI: 10.1002/cmdc.202000502
Abstract: κ‐Opioid receptors (KORs) play a predominant role in pain alleviation, itching skin diseases, depression and neurodegenerative disorders such as multiple sclerosis. Therefore, imaging of KOR by a fluorinated PET tracer was envisaged. Two strategies were… read more here.
Keywords: kor; pharmacological evaluation; evaluation fluorinated; fluorinated quinoxaline ... See more keywords
Synthesis and pharmacological activity of 2-(biphenyl-4-yl)imidazo[1,2-a]benzimidazoles
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DOI: 10.1007/s11172-017-1965-7
Abstract: An efficient method for the synthesis of novel 9H-imidazo[1,2-a]benzimidazole derivatives containing a biphenyl substituent at position 2 was developed. These compounds, belonging to the privileged substructures, have been tested for a wide range of pharmacological… read more here.
Keywords: activity biphenyl; synthesis pharmacological; pharmacological activity; imidazo ... See more keywords
Synthesis and pharmacological studies of 1-(2-amino-1-(4-methoxyphenyl) ethyl) cyclohexanol analogs as potential microbial agents
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DOI: 10.1016/j.arabjc.2012.12.009
Abstract: Abstract A novel series of Schiff bases 4a–n was prepared from 2-hydrazinyl-N-(2-(1-hydroxycyclohexyl)-2-(4-methoxyphenyl) ethyl)acetamide. Thiazolidinone 5a–n derivatives were prepared from the reaction of Schiff base and thioglycolic acid. The structures of the synthesized compounds were assigned… read more here.
Keywords: ethyl; studies amino; amino methoxyphenyl; synthesis pharmacological ... See more keywords
Synthesis and pharmacological screening of 4, 6-substituted di-(phenyl) pyrimidin-2-amines
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DOI: 10.1016/j.arabjc.2012.12.023
Abstract: Abstract A new series of 4, 6-substituted di-(phenyl) pyrimidin-2-amine ( IIa–d ) were synthesized by reacting chalcone derivatives with guanidine hydrochloride in the presence of dimethylformamide. The synthesized compounds were characterized by spectral analysis and… read more here.
Keywords: pharmacological screening; phenyl pyrimidin; synthesis pharmacological; substituted phenyl ... See more keywords
New quinolinic derivatives as melatonergic ligands: Synthesis and pharmacological evaluation.
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DOI: 10.1016/j.ejmech.2016.12.013
Abstract: New series of melatonergic ligands issued from two methoxy-quinolinic scaffolds (2-MQ and 3-MQ), were designed and synthesized. Herein we report the synthetic scheme and pharmacological results of the new prepared compounds. Investigation of compound 11a,… read more here.
Keywords: ligands synthesis; quinolinic derivatives; synthesis pharmacological; derivatives melatonergic ... See more keywords
Synthesis and Pharmacological Evaluation of New N-Sulfonylureas as NLRP3 Inflammasome Inhibitors: Identification of a Hit Compound to Treat Gout.
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DOI: 10.1021/acs.jmedchem.2c00149
Abstract: NLRP3 is involved in the pathophysiology of several inflammatory diseases. Therefore, there is high current interest in the clinical development of new NLRP3 inflammasome small inhibitors to treat these diseases. Novel N-sulfonylureas were obtained by… read more here.
Keywords: synthesis pharmacological; new sulfonylureas; pharmacological evaluation; nlrp3 inflammasome ... See more keywords
Synthesis and Pharmacological Characterization of Novel Peripheral Cannabinoid-1 Receptor Blockers Based on a Tricyclic Scaffold
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DOI: 10.1021/acs.jmedchem.4c03132
Abstract: The development of peripherally selective cannabinoid-1 receptor (CB1R) antagonists offers a promising strategy for obesity treatment. Here, we evaluated the efficacy of novel tricyclic CB1R antagonists, focusing on BNS808. Our findings demonstrate that BNS808 exhibits… read more here.
Keywords: cannabinoid receptor; cb1r antagonists; cannabinoid; drug ... See more keywords
Design, Synthesis, and Pharmacological Evaluation of Quinazoline and Quinoline Derivatives as Potent ENPP1 Inhibitors for Cancer Immunotherapy.
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DOI: 10.1021/acs.jmedchem.4c03207
Abstract: ENPP1, a transmembrane glycoprotein overexpressed in various cancers, has become a promising target for tumor immunotherapy. Several ENPP1 inhibitors have been reported, but only a few have been validated in vivo. Herein, based on the… read more here.
Keywords: enpp1 inhibitors; tumor; quinoline derivatives; synthesis pharmacological ... See more keywords
Synthesis and Pharmacological Evaluation of Heterocyclic Carboxamides: Positive Allosteric Modulators of the M1 Muscarinic Acetylcholine Receptor with Weak Agonist Activity and Diverse Modulatory Profiles.
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DOI: 10.1021/acs.jmedchem.7b01812
Abstract: Targeting allosteric sites at M1 muscarinic acetylcholine receptors is a promising strategy for the treatment of Alzheimer's disease. Positive allosteric modulators not only may potentiate binding and/or signaling of the endogenous agonist acetylcholine (ACh) but… read more here.
Keywords: agonist activity; muscarinic acetylcholine; allosteric modulators; synthesis pharmacological ... See more keywords
Synthesis and Pharmacological Evaluation of Triazolopyrimidinone Derivatives as Noncompetitive, Intracellular Antagonists for CC Chemokine Receptors 2 and 5
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DOI: 10.1021/acs.jmedchem.9b00742
Abstract: CC chemokine receptors 2 (CCR2) and 5 (CCR5) are involved in many inflammatory diseases; however, most CCR2 and CCR5 clinical candidates have been unsuccessful. (Pre)clinical evidence suggests that dual CCR2/CCR5 inhibition might be more effective… read more here.
Keywords: triazolopyrimidinone derivatives; pharmacological evaluation; synthesis pharmacological; chemokine receptors ... See more keywords
Synthesis and Pharmacological Activities of Pyrano[2,3-d]pyrimidine and Pyrano[2,3-d]pyrimidine-5-one Derivatives as New Fused Heterocyclic Systems
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DOI: 10.1155/2017/5373049
Abstract: Various fused oxazine such as 4-(4-methoxyphenyl)-3,7-dimethyl-1,4-dihydro-5H-pyrazolo [4′,3′:5,6]pyrano[2,3-d][ ]oxazin-5-one 2 has been prepared and utilized as a starting material for novel pyrazolopyranopyrimidinones 3, 5, 6, and 7a–c and pyrazolopyranopyrimidines 4, 9, 10, and 11 which are… read more here.
Keywords: pyrimidine pyrano; pharmacological activities; synthesis pharmacological; activities pyrano ... See more keywords