Next-Generation Diprovocims with Potent Human and Murine TLR1/TLR2 Agonist Activity That Activate the Innate and Adaptive Immune Response.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00419
Abstract: The diprovocims, a new class of toll-like receptor (TLR) agonists, bear no similarity to prior TLR agonists, act through a well-defined mechanism (TLR1/TLR2 agonist), exhibit exquisite structure-activity relationships, and display in vivo adjuvant activity. They… read more here.
Keywords: tlr2 agonist; tlr1 tlr2; agonist activity; murine ... 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.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
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
Catecholic Isoquinolines from Portulaca oleracea and Their Anti-inflammatory and β2-Adrenergic Receptor Agonist Activity.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of natural products"
DOI: 10.1021/acs.jnatprod.7b00762
Abstract: Isoquinoline alkaloids possess a wide range of structural features and pharmaceutical activities and are promising drug candidates. Ten water-soluble catecholic isoquinolines were isolated from the medicinal plant Portulaca oleracea, including three new (1-3) and seven… read more here.
Keywords: anti inflammatory; agonist activity; receptor agonist; catecholic isoquinolines ... See more keywords
Minimal Structural Changes Determine Full and Partial Nicotinic Receptor Agonist Activity for Nicotine Analogues
Sign Up to like & getrecommendations! Published in 2019 at "Molecules"
DOI: 10.3390/molecules24152684
Abstract: Neuronal α4β2 nicotinic acetylcholine receptors (nAChRs) are ligand-gated ion channels (LGIC) that have been implicated in nicotine addiction, reward, cognition, pain disorders, anxiety, and depression. Nicotine has been widely used as a template for the… read more here.
Keywords: minimal structural; nicotine; structural changes; agonist activity ... See more keywords