10.1021/jm000496v
The research focuses on the synthesis, structure-activity relationships (SARs), and pharmacokinetic profiles of nonpeptidic r-keto heterocycles as novel inhibitors of human chymase, a chymotrypsin-like serine protease with potential roles in cardiovascular diseases and inflammatory conditions. The study hypothesizes that a pyrimidinone scaffold combined with heterocycles as P1 carbonyl-activating groups can effectively inhibit chymase, leading to the design and synthesis of various 5-amino-6-oxo-1,6-dihydropyrimidine derivatives with different heterocycles. The compounds were evaluated for their in vitro inhibitory activity against human heart chymase and other proteases using spectrophotometric assays monitoring the release of p-nitroaniline from synthetic substrates. The most potent compound, 2r (Y-40079), was further subjected to pharmacokinetic studies in rats, assessing its absorption, bioavailability, and metabolic stability. The experiments involved various reactants such as acetone cyanohydrin, HCl, monoethanolamine, and palladium-carbon for synthesis, and employed techniques like NMR, MS, and elemental analysis for compound characterization. The inhibitory constants (Ki), association rate constants (kon), and dissociation constants (koff) were determined through progress curve analysis and nonlinear regression. The research aimed to develop a potent, selective, and metabolically stable nonpeptidic chymase inhibitor, which could serve as a therapeutic agent or a tool for understanding chymase-related pathophysiology.
10.1016/j.orgel.2021.106171
The research focuses on the development of a high-performance, non-doped, pure-blue electroluminescent device based on a bisphenanthroimidazole derivative with a twisted donor-acceptor structure. The study involves the design and synthesis of a compound named TPA-DPPI, which consists of bisphenanthroimidazole and triphenylamine units, exhibiting bipolar carrier transport properties. The experiments conducted include the synthesis of TPA-DPPI through a series of chemical reactions using reactants such as phenanthrene-9,10-dione, benzaldehyde, 4-nitroaniline, and ammonium acetate, followed by purification and characterization using techniques like 1H NMR, mass spectrometry, and elemental analysis. The compound's thermal properties were investigated using TGA and DSC, while its electrochemical properties were assessed through cyclic voltammetry. The molecular structure and electronic properties were analyzed using DFT calculations, and the optical properties were examined through UV–vis absorption and photoluminescence (PL) spectra. The performance of the non-doped OLED device was evaluated based on its electroluminescence, with key metrics including Commission International de l’Eclairage (CIE) coordinates, external quantum efficiency (EQE), and device stability. The research demonstrates that TPA-DPPI can achieve a high EQE of 5.20%, making it a promising candidate for non-doped pure-blue OLEDs.
10.1016/j.ica.2004.03.004
The study focuses on the synthesis, crystal structures, and molecular hyperpolarizabilities of a new Schiff base ligand (HL) derived from the condensation of 4-(diethylamino)salicylaldehyde with 4-nitroaniline, and its metal complexes with nickel(II), copper(II), and cobalt(II). The purpose of these chemicals is to investigate their quadratic nonlinear optical (NLO) properties, which are crucial for applications in fields like telecommunications and optical data storage. The Schiff base ligand and its metal complexes were analyzed for their crystal structures, thermal stability, and NLO responses, with the aim of understanding how the introduction of a metal center can enhance the NLO response and improve thermal stability. The study found that while the nickel(II) and copper(II) complexes were centrosymmetric and thus had vanishing hyperpolarizabilities, the cobalt(II) complex exhibited a pseudo-tetrahedral structure, leading to an enhancement of the NLO response and an increase in thermal stability.
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