110503-79-2Relevant academic research and scientific papers
Synthetic pores with sticky π-clamps
Tanaka, Hiroyuki,Bollot, Guillaume,Mareda, Jiri,Litvinchuk, Svetlana,Tran, Duy-Hien,Sakai, Naomi,Matile, Stefan
, p. 1369 - 1380 (2007)
In this report, we describe design, synthesis, evaluation and molecular dynamics simulations of synthetic multifunctional pores with π-acidic naphthalenediimide clamps. Experimental evidence is provided for the formation of unstable but inert, heterogeneo
A pH-sensitive Macromolecular Prodrug as TLR7/8 Targeting Immune Response Modifier
Aichhorn, Stefan,Linhardt, Anne,Halfmann, Angela,Nadlinger, Markus,Kirchberger, Stefanie,Stadler, Manuela,Dillinger, Barbara,Distel, Martin,Dohnal, Alexander,Teasdale, Ian,Sch?fberger, Wolfgang
, p. 17721 - 17726 (2017)
The chemical synthesis and biological activity of novel functionalized imidazoquinoline derivatives (ImQ) to generate Toll-like receptor (TLR) 7/8 specific prodrugs are presented. In vivo activity of ImQs to induce inflammation was confirmed in zebrafish
Interest of new alkylsulfonylhydrazide-type compound in the treatment of alcohol use disorders
Jeanblanc, Jér?me,Bourguet, Erika,Sketriené, Diana,Gonzalez, Céline,Moroy, Gautier,Legastelois, Rémi,Létévé, Mathieu,Trussardi-Régnier, Aurélie,Naassila, Micka?l
, p. 1835 - 1844 (2018)
Rationale: Recent preclinical research suggested that histone deacetylase inhibitors (HDACIs) and specifically class I HDAC selective inhibitors might be useful to treat alcohol use disorders (AUDs). Objective: The objective of this study was to find a new inhibitor of the HDAC-1 isoenzyme and to test its efficacy in an animal model of AUDs. Methods: In the present study, we prepared new derivatives bearing sulfonylhydrazide-type zinc-binding group (ZBG) and evaluated these compounds in vitro on HDAC-1 isoenzyme. The most promising compound was tested on ethanol operant self-administration and relapse in rats. Results: We showed that the alkylsulfonylhydrazide-type compound (ASH) reduced by more than 55% the total amount of ethanol consumed after one intracerebroventricular microinjection, while no effect was observed on motivation of the animals to consume ethanol. In addition, one ASH injection in the central amygdala reduced relapse. Conclusions: Our study demonstrated that a new compound designed to target HDAC-1 is effective in reducing ethanol intake and relapse in rats and further confirm the interest of pursuing research to study the exact mechanism by which such inhibitor may be useful to treat AUDs.
Oxadiazole-Based Cell Permeable Macrocyclic Transition State Inhibitors of Norovirus 3CL Protease
Damalanka, Vishnu C.,Kim, Yunjeong,Alliston, Kevin R.,Weerawarna, Pathum M.,Galasiti Kankanamalage, Anushka C.,Lushington, Gerald H.,Mehzabeen, Nurjahan,Battaile, Kevin P.,Lovell, Scott,Chang, Kyeong-Ok,Groutas, William C.
, p. 1899 - 1913 (2016/03/22)
Human noroviruses are the primary causative agents of acute gastroenteritis and a pressing public health burden worldwide. There are currently no vaccines or small molecule therapeutics available for the treatment or prophylaxis of norovirus infections. Norovirus 3CL protease plays a vital role in viral replication by generating structural and nonstructural proteins via the cleavage of the viral polyprotein. Thus, molecules that inhibit the viral protease may have potential therapeutic value. We describe herein the structure-based design, synthesis, and in vitro and cell-based evaluation of the first class of oxadiazole-based, permeable macrocyclic inhibitors of norovirus 3CL protease.
