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Molecules, Vol. 27, Pages 5488: The Effect of a New N-hetero Cycle Derivative on Behavior and Inflammation against the Background of Ischemic Stroke
Kiseleva Vadim V. Negrebetsky Yuri I. Baukov Ischemic stroke triggers a whole cascade of pathological changes in the brain, one of which is postischemic inflammation. Since in such cases thrombolytic therapy is often not possible, methods that modulate inflammation and affect microglia become particularly interesting. We synthesized 3-(2-oxo-4-phenylpyrrolidin-1-yl)propane-1-sulfonate calcium(II) (Compound 4) and studied its anti-inflammatory activity in in vitro and in vivo models of inflammation and ischemia. Macrophage cell line RAW 264.7 was treated with lipopolysaccharides (LPS) and Compound 4 at various dosa...
Source: Molecules - August 26, 2022 Category: Chemistry Authors: Denis A. Borozdenko Tatiana A. Shmigol Aiarpi A. Ezdoglian Darya I. Gonchar Natalia. Y. Karpechenko Dmitri N. Lyakhmun Anastasia D. Shagina Elvira A. Cherkashova Daria D. Namestnikova Ilya L. Gubskiy Anastasia A. Chernysheva Nina M. Kiseleva Vadim V. Negr Tags: Article Source Type: research

Vitamin D and its possible relationship to neuroprotection in COVID-19: evidence in the literature
Curr Top Med Chem. 2022 Apr 1. doi: 10.2174/1568026622666220401140737. Online ahead of print.ABSTRACTVitamin D is a hormone involved in the regulation of important biological processes such as signal transduction, immune response, metabolic regulation and also in the nervous and vascular systems. To date, coronavirus disease 2019 (COVID-19) infection does not have a specific treatment, however various drugs have been proposed, including those that attenuate the intense inflammatory response and recently the use of vitamin D, in clinical trials, as part of the treatment of COVID-19 has provided promising results. It has bee...
Source: Current Topics in Medicinal Chemistry - April 3, 2022 Category: Chemistry Authors: Saray Quintero-Fabi án Cindy Bandala Luz Adriana Pichardo-Mac ías Itzel Jatziri Contreras-Garc ía Sa úl Gómez-Manzo Beatriz Hern ández-Ochoa Jos é Arturo Martínez-Orozco Iv án Ignacio-Mejía Noem í Cárdenas-Rodríguez Source Type: research

Synthesis and evaluation of novel and potent protease activated receptor 4 (PAR4) antagonists based on a quinazolin-4(3H)-one scaffold
In this study, we explored the activity of quinazolin-4(3H)-one-based PAR4 antagonists, beginning with their IDT analogues. By repeated structural optimisation, we developed a series of highly selective PAR4 antagonists with nanomolar potency on human platelets. Of these, 13 and 30g, with an 8-benzo[d]thiazol-2-yl-substituted quinazolin-4(3H)-one structure, showed optimal activity (h. PAR4-AP PRP IC50 = 19.6 nM and 6.59 nM, respectively) on human platelets. Furthermore, 13 and 30g showed excellent selectivity for PAR4 versus PAR1 and other receptors (IC50s > 10 μM) on human platelets. And 13 and 30g were lack of cross-...
Source: European Journal of Medicinal Chemistry - August 14, 2021 Category: Chemistry Authors: Shangde Liu Duo Yuan Shanshan Li Roujie Xie Yi Kong Xiong Zhu Source Type: research