62402-24-8Relevant articles and documents
An inorganic helix [Mn(IPG)(MeOH)](n)[PF6](n): Structural and magnetic properties of a syn-anti carboxylate-bridged manganese(II) chain involving a tetradentate ligand
Policar, Clotilde,Lambert, Francois,Cesario, Michele,Morgenstern-Badarau, Irene
, p. 2201 - 2207 (1999)
The crystal structure of an infinite inorganic chain consisting of Mn(II) and an N-centered tripodal ligand N,N-(2-pyridylmethyl)[(1- methylimidazol-2-yl)-methyl]glycinate is presented. It exhibits a chiral helical structure with a pitch of two monomeric units (each monomeric unit containing one Mn atom). Each manganese is connected to its neighbor through a carboxylate bridge in a syn-antigeometry. Around each manganese center, two carboxylates bind in a cis geometry. This peculiar bridging geometry (syn- anti cis) provides a broken-line chain, running in a zig-zag manner along the b axis of the P21 space group. The magnetic properties have been investigated. They show a pseudo-2D magnetic structure, with one major pathway along the chain and an inter-chain minor one. The intrachain coupling is a weak antiferromagnetic interaction (J/k = -0.25). This low value is entirely consistent with the geometry of the bridge. The interchain coupling is a weaker antiferromagnetic coupling (J'/k = -0.11) and could be mediated through π-π interactions between pyridine and imidazole from two adjacent helixes.
Discovery of a First-In-Class Small Molecule Antagonist against the Adrenomedullin-2 Receptor: Structure-Activity Relationships and Optimization
Zirimwabagabo, Jean-Olivier,Jailani, Ameera B. A.,Avgoustou, Paris,Tozer, Matthew J.,Gibson, Karl R.,Glossop, Paul A.,Mills, James E. J.,Porter, Roderick A.,Blaney, Paul,Wang, Ning,Skerry, Timothy M.,Richards, Gareth O.,Harrity, Joseph P. A.
, p. 3299 - 3319 (2021/04/06)
Class B G-protein-coupled receptors (GPCRs) remain an underexploited target for drug development. The calcitonin receptor (CTR) family is particularly challenging, as its receptors are heteromers comprising two distinct components: The calcitonin receptor-like receptor (CLR) or calcitonin receptor (CTR) together with one of three accessory proteins known as receptor activity-modifying proteins (RAMPs). CLR/RAMP1 forms a CGRP receptor, CLR/RAMP2 forms an adrenomedullin-1 (AM1) receptor, and CLR/RAMP3 forms an adrenomedullin-2 (AM2) receptor. The CTR/RAMP complexes form three distinct amylin receptors. While the selective blockade of AM2 receptors would be therapeutically valuable, inhibition of AM1 receptors would cause clinically unacceptable increased blood pressure. We report here a systematic study of structure-activity relationships that has led to the development of first-in-class AM2 receptor antagonists. These compounds exhibit therapeutically valuable properties with 1000-fold selectivity over the AM1 receptor. These results highlight the therapeutic potential of AM2 antagonists.
Unsymmetrical dizinc complexes as models for the active sites of phosphohydrolases
Jarenmark, Martin,Csapo, Edit,Singh, Jyoti,Woeckel, Simone,Farkas, Etelka,Meyer, Franc,Haukka, Matti,Nordlander, Ebbe
scheme or table, p. 8183 - 8194 (2011/01/07)
The unsymmetrical dinucleating ligand 2-(N-isopropyl-N-((2-pyridyl)methyl) aminomethyl)-6-(N-(carboxylmethyl)-N-((2-pyridyl)methyl)aminomethyl) -4-methylphenol (IPCPMP or L) has been synthesized to model the active site environment of dinuclear metallohydrolases. It has been isolated as the hexafluorophosphate salt H4IPCPMP(PF6)2· 2H2O (H4L), which has been structurally characterized, and has been used to form two different Zn(ii) complexes, [{Zn2(IPCPMP) (OAc)}2][PF6]2 (2) and [{Zn2(IPCPMP) (Piv)}2][PF6]2 (3) (OAc = acetate; Piv = pivalate). The crystal structures of 2 and 3 show that they consist of tetranuclear complexes with very similar structures. Infrared spectroscopy and mass spectrometry indicate that the tetranuclear complexes dissociate into dinuclear complexes in solution. Potentiometric studies of the Zn(ii):IPCPMP system in aqueous solution reveal that a mononuclear complex is surprisingly stable at low pH, even at a 2:1 Zn(ii):L ratio, but a dinuclear complex dominates at high pH and transforms into a dihydroxido complex by a cooperative deprotonation of two, probably terminally coordinated, water molecules. A kinetic investigation indicates that one of these hydroxides is the active nucleophile in the hydrolysis of bis(2,4-dinitrophenyl)phosphate (BDNPP) enhanced by complex 2, and mechanistic proposals are presented for this reaction as well as the previously reported transesterification of 2-hydroxypropyl p-nitrophenyl phosphate (HPNP) promoted by Zn(ii) complexes of IPCPMP.
