G protein‐coupled receptor binding and pharmacological evaluation of indole‐derived thiourea compounds
Sign Up to like & getrecommendations! Published in 2019 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.201900218
Abstract: Four 2‐(1H‐indol‐3‐yl)ethylthiourea derivatives were prepared by condensation of 2‐(1H‐indol‐3‐yl)ethanamine with the corresponding aryl/alkylisothiocyanates in a medium‐polarity solvent. Their structures were confirmed by spectral techniques, and the molecular structure of 3 was determined by X‐ray crystal… read more here.
Keywords: binding pharmacological; pharmacological evaluation; protein coupled; coupled receptor ... See more keywords
Synthesis and Pharmacological Evaluation of Fluorinated Quinoxaline‐Based κ‐Opioid Receptor (KOR) Agonists Designed for PET Studies
Sign Up to like & getrecommendations! Published in 2020 at "Chemmedchem"
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
In silico design and pharmacological evaluation of conjugates of atenolol with modified saccharide for cardiovascular targeting
Sign Up to like & getrecommendations! Published in 2021 at "Glycoconjugate Journal"
DOI: 10.1007/s10719-021-09983-x
Abstract: Amongst a wide range of biological macromolecules, saccharides exhibit the potential to be specifically recognized by cell-surface receptors and hence can be utilized as ligands in targeted drug delivery. The current study aims to use… read more here.
Keywords: silico design; pharmacological evaluation; study; drug ... See more keywords
Synthesis, characterization, pharmacological evaluation and molecular docking studies of benzothiazole azo derivatives
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Molecular Structure"
DOI: 10.1016/j.molstruc.2020.128477
Abstract: Abstract A series of novel benzothiazole based azo dyes were synthesized and fully characterized by using different analytical techniques. The antioxidant activity of synthesized azo dyes was studied with the DPPH, hydrogen peroxide, metal chelating… read more here.
Keywords: characterization pharmacological; synthesized compounds; synthesized azo; pharmacological evaluation ... See more keywords
Pharmacological evaluation of clinically relevant concentrations of (2R,6R)-hydroxynorketamine
Sign Up to like & getrecommendations! Published in 2019 at "Neuropharmacology"
DOI: 10.1016/j.neuropharm.2019.04.019
Abstract: Ketamine is a rapid-onset antidepressant whose efficacy long outlasts its pharmacokinetics. Multiple studies suggest ketamine's antidepressant effects require increased α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR)-dependent currents, which have recently been exclusively attributed to its N-methyl-d-aspartate receptor-inactive metabolite… read more here.
Keywords: hnk concentrations; clinically antidepressant; ketamine; pharmacological evaluation ... See more keywords
Synthesis and Pharmacological Evaluation of New N-Sulfonylureas as NLRP3 Inflammasome Inhibitors: Identification of a Hit Compound to Treat Gout.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
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
Structural Modification and Pharmacological Evaluation of Substituted Quinoline-5,8-diones as Potent NSD2 Inhibitors.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01920
Abstract: The histone lysine methyltransferase NSD2 is overexpressed, translocated, or mutated in multiple types of cancers and has emerged as an attractive therapeutic target. However, the development of small-molecule NSD2 inhibitors is still in its infancy,… read more here.
Keywords: modification pharmacological; structural modification; nsd2 inhibitors; substituted quinoline ... See more keywords
Synthesis and Pharmacological Evaluation of Triazolopyrimidinone Derivatives as Noncompetitive, Intracellular Antagonists for CC Chemokine Receptors 2 and 5
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Medicinal Chemistry"
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
Characterization and Pharmacological Evaluation of Anti-Cellulite Herbal Product(s) Encapsulated in 3D-Fabricated Polymeric Microneedles
Sign Up to like & getrecommendations! Published in 2020 at "Scientific Reports"
DOI: 10.1038/s41598-020-63271-6
Abstract: Skin health is vital for a healthy body. Herbal remedies have long been used for skin care, and their global use has tremendously increased over the past three decades. Although cellulite is seen as a… read more here.
Keywords: cellulite herbal; characterization pharmacological; evaluation anti; pharmacological evaluation ... See more keywords
Synthesis, characterization, and pharmacological evaluation of thiourea derivatives
Sign Up to like & getrecommendations! Published in 2020 at "Open Chemistry"
DOI: 10.1515/chem-2020-0139
Abstract: Abstract Thioureas and their derivatives are organosulfur compounds having applications in numerous fields such as organic synthesis and pharmaceutical industries. Symmetric thiourea derivatives were synthesized by the reaction of various anilines with CS2. The synthesized… read more here.
Keywords: g6pase; characterization pharmacological; pharmacological evaluation; evaluation thiourea ... See more keywords
Design, Synthesis and Pharmacological Evaluation of Novel C2,C3-Quinoxaline Derivatives as Promising Anxiolytic Agents
Sign Up to like & getrecommendations! Published in 2022 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms232214401
Abstract: A new series of quinoxaline derivatives, 2a–4b, were synthesized and their anxiolytic potential was evaluated in vivo using elevated plus maze (EPM), open field (OF) and light-dark box (LDB) techniques. According to the results of… read more here.
Keywords: design synthesis; synthesis pharmacological; quinoxaline derivatives; evaluation novel ... See more keywords