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
Discovery and Optimization of Triazolopyrimidinone Derivatives as Selective NLRP3 Inflammasome Inhibitors.
Sign Up to like & getrecommendations! Published in 2022 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.2c00242
Abstract: The NLRP3 inflammasome is a multiprotein complex that facilitates activation and release of the proinflammatory cytokines interleukin-1β (IL-1β) and IL-18 in response to infection or endogenous stimuli. It can be inappropriately activated by a range… read more here.
Keywords: triazolopyrimidinone derivatives; derivatives selective; optimization triazolopyrimidinone; discovery optimization ... See more keywords