A series of acrylic acids and their structurally related compounds were evaluated for their binding affinity to four EP receptor subtypes (EP1-4). Starting from the initial hit 3, which was discovered in our in-house library, compounds 4 and 5 were identified as new chemical leads as candidates for further optimization towards a selective EP3 receptor antagonist. The identification process of these compounds and their pharmacokinetic profiles are presented.
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http://dx.doi.org/10.1016/j.bmc.2009.08.007 | DOI Listing |
ACS Macro Lett
January 2025
Key Laboratory of Materials Chemistry for Energy Conversion and Storage, Ministry of Education, Hubei Key Laboratory of Materials Chemistry and Service Failure, Hubei Engineering Research Center for Biomaterials and Medical Protective Materials, State Key Laboratory of Materials Processing and Die & Mould Technology, School of Chemistry and Chemical Engineering, Huazhong University of Science and Technology, Wuhan 430074, China.
As a special kind of supramolecular compound with many favorable properties, pillar[]arene-based supramolecular polymer networks (SPNs) show potential application in many fields. Although we have come a long way using pillar[]arene to prepare SPNs and construct a series of smart materials, it remains a challenge to enhance the mechanical strength of pillar[]arene-based SPNs. To address this issue, a new supramolecular regulation strategy was developed, which could precisely control the preparation of pillar[]arene-based SPN materials with excellent mechanical properties by adjusting the polymer network structures.
View Article and Find Full Text PDFNanomaterials (Basel)
December 2024
Leibniz-Institut für Polymerforschung Dresden e.V., Hohe Str. 6, 01069 Dresden, Germany.
Understanding the interplay between the molecular structure of the ionic liquid (IL) subunit, the resulting nanostructure and ion transport in polymerized ionic liquids (PILs) is necessary for the realization of high-performance solid-state electrolytes required in various advanced applications. Herein, we present a detailed structural characterization of a recently synthesized series of acrylate-based PIL homopolymers and networks with imidazolium cations and chloride anions with varying alkyl spacer and terminal group lengths designed for organic solid-state batteries based on X-ray scattering. The impact of the concentrations of both the crosslinker and added tetrabutylammonium chloride (TBACl) conducting salt on the structural characteristics is also investigated.
View Article and Find Full Text PDFAntibiotics (Basel)
December 2024
Medicinal Chemistry Laboratory, Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India.
The increasing prevalence of antimicrobial resistant highlights the urgent need for the new therapeutic agents. This study aimed to design and synthesize fused tricyclic benzimidazole-thiazinone derivatives (-) through a convenient method and evaluate their antimicrobial activity against various microorganisms. A series of fused tricyclic benzimidazole-thiazinone derivatives was rationally designed and synthesized in one pot by the reaction between trans substituted acrylic acids and 1-benzo[d]imidazole-2-thiol using coupling reagent TBTU (2-(1-benzotriazol-1-yl)-1,1,3,3-tetramethyluronium tetrafluoroborate).
View Article and Find Full Text PDFJ Am Chem Soc
January 2025
Tianjin Key Laboratory of Brine Chemical Engineering and Resource Eco-utilization, College of Chemical Engineering and Materials Science, Tianjin University of Science & Technology, Tianjin 300457, P. R. China.
Polymer nanoparticles with low curvature, especially two-dimensional (2D) soft materials, are rich in functions and outstanding properties and have received extensive attention. Crystallization-driven self-assembly (CDSA) of linear semicrystalline block copolymers is currently a common method of constructing 2D platelets of uniform size. Although accompanied by high controllability, this CDSA method usually and inevitably requires a longer aging time and lower assembly concentration, limiting the large-scale preparation of nanoaggregates.
View Article and Find Full Text PDFContact Dermatitis
December 2024
Department of Occupational and Environmental Dermatology, Lund University, Skåne University Hospital, Malmö, Sweden.
Background: There is a current fashion for the use of methacrylate-containing nail cosmetics that can induce allergic contact dermatitis. European Union (EU) legislation was introduced in 2021 that had the aim of preventing its development.
Objectives: To assess prevalence and exposures causing contact allergy to 2-hydroxyethyl methacrylate (HEMA) prior to and following implementation of the legislation.
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