The article 《Rational design of new multitarget histamine H3 receptor ligands as potential candidates for treatment of Alzheimer′s disease》 also mentions many details about this compound(111-24-0)Quality Control of 1,5-Dibromopentane, you can pay attention to it or contacet with the author([email protected]) to get more information.
Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 111-24-0, is researched, SMILESS is BrCCCCCBr, Molecular C5H10Br2Journal, Article, European Journal of Medicinal Chemistry called Rational design of new multitarget histamine H3 receptor ligands as potential candidates for treatment of Alzheimer′s disease, Author is Lazewska, Dorota; Bajda, Marek; Kaleta, Maria; Zareba, Paula; Doroz-Plonka, Agata; Siwek, Agata; Alachkar, Alaa; Mogilski, Szczepan; Saad, Ali; Kuder, Kamil; Olejarz-Maciej, Agnieszka; Godyn, Justyna; Stary, Dorota; Sudol, Sylwia; Wiecek, Malgorzata; Latacz, Gniewomir; Walczak, Maria; Handzlik, Jadwiga; Sadek, Bassem; Malawska, Barbara; Kiec-Kononowicz, Katarzyna, the main research direction is xanthone derivative preparation H3 receptor ligand Alzheimer’s; Alzheimer’s disease; Cholinesterase inhibitors; Histamine H(3) receptor; Monoamine oxidase inhibitors; Multitarget-directed ligands; Xanthone derivatives.Quality Control of 1,5-Dibromopentane.
Design and development of multitarget-directed ligands (MTDLs) has become a very important approach in the search of new therapies for Alzheimer′s disease (AD). In our present research, a number of xanthone derivatives were first designed using a pharmacophore model for histamine H3 receptor (H3R) antagonists/inverse agonists, and virtual docking was then performed for the enzyme acetylcholinesterase. Next, 23 compounds were synthesized and evaluated in vitro for human H3R (hH3R) affinity and inhibitory activity on cholinesterases. Most of the target compounds showed hH3R affinities in nanomolar range and exhibited cholinesterase inhibitory activity with IC50 values in submicromolar range. Furthermore, the inhibitory effects of monoamine oxidases (MAO) A and B were investigated. The results showed low micromolar and selective human MAO B (hMAO B) inhibition. Two azepane derivatives, namely 23 (2-(5-(azepan-1-yl)pentyloxy)-9H-xanthen-9-one) and 25 (2-(5-(azepan-1-yl)pentyloxy)-7-chloro-9H-xanthen-9-one), were especially very promising and showed high affinity for hH3R (Ki = 170 nM and 100 nM resp.) and high inhibitory activity for acetylcholinesterase (IC50 = 180 nM and 136 nM resp.). Moreover, these compounds showed moderate inhibitory activity for butyrylcholinesterase (IC50 = 880 nM and 394 nM resp.) and hMAO B (IC50 = 775 nM and 897 nM resp.). Furthermore, mol. docking studies were performed for hH3R, human cholinesterases and hMAO B to describe the mode of interactions with these biol. targets. Next, the two most promising compounds 23 and 25 were selected for in vivo studies. The results showed significant memory-enhancing effect of compound 23 in dizocilpine-induced amnesia in rats in two tests: step-through inhibitory avoidance paradigm (SIAP) and transfer latency paradigm time (TLPT). In addition, favorable analgesic effects of compound 23 were observed in neuropathic pain models. Therefore, compound 23 is a particularly promising structure for further design of new MTDLs for AD.
The article 《Rational design of new multitarget histamine H3 receptor ligands as potential candidates for treatment of Alzheimer′s disease》 also mentions many details about this compound(111-24-0)Quality Control of 1,5-Dibromopentane, you can pay attention to it or contacet with the author([email protected]) to get more information.
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