430464-44-1Relevant academic research and scientific papers
Mechanochromic Luminescence from Crystals Consisting of Intermolecular Hydrogen-Bonded Sheets
Nakamura, Takayoshi,Sagara, Yoshimitsu,Takahashi, Kiyonori,Tamaoki, Nobuyuki
supporting information, (2020/02/04)
Introduction of functional groups that can form intermolecular hydrogen bonds into highly-emissive luminophores is a promising way to induce mechanochromic luminescence. Herein, we report that a 9,10-bis(phenylethynyl)anthracene derivative featuring two amide groups forms green-emissive crystals based on two-dimensional hydrogen-bonded molecular sheets. Mechanical grinding changed the emission from green to yellow, owing to a transition from a crystalline to an amorphous phase. Infrared spectroscopy revealed that mechanical stimuli disrupted the linear hydrogen-bonding formation. A thermal treatment recovered the original green photoluminescence.
Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists part 1. The discovery of arylacetamides as viable replacements for the dihydropyrimidinone moiety of an HTS hit
Jiang, Yu,Chen, Chien-An,Lu, Kai,Daniewska, Irena,De Leon, John,Kong, Ron,Forray, Carlos,Li, Boshan,Hegde, Laxminarayan G.,Wolinsky, Toni D.,Craig, Douglas A.,Wetzel, John M.,Andersen, Kim,Marzabadi, Mohammad R.
, p. 3870 - 3882 (2008/02/09)
Melanin-concentrating hormone (MCH) is involved in the regulation of feeding, water balance, energy metabolism, general arousal and attention state, memory, cognitive functions, and psychiatric disorders. Herein, two new chemical series exemplified by N-[5-(1-{3-[2,2-bis-(4-fluoro-phenyl)-acetylamino]- propyl}-piperidin-4-yl)-2,4-difluoro-phenyl]-isobutyramide (SNAP 102739, 5m) and N-[3-(1-{3-[(S)-2-(4-fluorophenyl)-propionylamino]-propyl}-piperidin-4-yl)-4- methylphenyl]-isobutyramide ((S)-6b) are reported. These compounds were designed to improve the pharmacokinetic properties of the high-throughput screening lead compound 1 (SNAP 7941). The MCH1 receptor antagonists 5m and (S)-6b show reasonable pharmacokinetic profiles (rat bioavailability = 48 and 81%, respectively). Compounds 5m and (S)-6b demonstrated the inhibition of a centrally administered MCH-evoked drinking effect, and compound 5m exhibited oral in vivo efficacy in the rat social interaction model of anxiety, with a minimum effective dose = 0.3 mg/kg.
