Synthesis of N‐Alkyl‐Carbazole Derivatives as 5‐HT₇R Antagonists

Abstract

We designed and synthesized a series of N-alkyl-carbazoles with different alkyl chains and amine moieties, and biological evaluation was performed to discover novel 5-HT 7 R antagonists. Among 27 synthesized compounds, 20, 21, 23, and 24 showed excellent binding affinities to 5-HT 7 R (K i = 65, 64, 55, and 31 nM, respectively), and good selectivity profiles over other serotonin receptors. In functional assays, those compounds showed weak antagonistic activities against 5-HT 7 R. In particular, the compound 24, 2-(4-(5-(9H-carbazol-9-yl)pentyl)piperazin-1-yl)phenol, could be considered as a potent and selective 5-HT 7 R ligand with weak antagonistic effect. From the molecular docking study, the aromatic hydroxyl group in 24 was shown to play an important role in binding to 5-HT 7 R through a hydrogen bonding interaction with Asp142 in the ligand binding pocket of 5-HT 7 R.

Hexagonal Cylinder Mesoporous Sorbent for Separation of Uranium Ions from Nitrate Media

“…4a demonstrates that the point of zero charge (PZC) is around pH 1.1. The shift in the PZC to a lower pH, relative to the PZC of pure silica (pH 2–3) 27, confirms the success of DPTS immobilization into silica mesopores. Fig.…”

Selective Recovery of Silver(I) Ions from E‐Waste using Cubically Multithiolated Cage Mesoporous Monoliths

“…Figure A shows that the point of zero charge (pzc) is around pH 3.3. The shift in the pzc to a higher pH, relative to the pzc of pure HOM carriers (pH 2) indicates the immobilization of the chelating moiety (ATZT) in the HOM–Si surface and possibly arises from the decrease of the negative charge generated from the silanol dissociation in the silica surface. Below the pzc of MOH–Si–NS, the N sites of the mesoporous sorbent become protonated (NH + ), and the particle surface charge becomes positive and increases as the pH decreases .…”

Silica‐Microencapsulated Orange Oil for Sustainable Pest Control

“…A rule of thumb based on the Derjaguin, Landau, Verwey, and Overbeek theory suggests that values of ζ equal to or larger than ±30 mV are enough to promote stable water suspensions. [ 20 ] In light of practical applications, it is also relevant herein to notice that for amorphous silica, namely for glassy particles such as those comprising the SiliOrange material, the ζ potential rapidly decreases toward more negative values when increasing pH, [ 21,20 ] thus enabling the use of these microcapsules in aqueous systems of widely different pH.…”