100523-84-0Relevant articles and documents
Synthesis, Nicotinic Acetylcholine Receptor Binding, and in Vitro and in Vivo Pharmacological Properties of 2′-Fluoro-(substituted thiophenyl)deschloroepibatidine Analogues
Ondachi, Pauline W.,Castro, Ana H.,Sherman, Benjamin,Luetje, Charles W.,Damaj, M. Imad,Mascarella, S. Wayne,Navarro, Hernán A.,Carroll
, p. 115 - 127 (2017)
The synthesis, nAChR in vitro and in vivo pharmacological properties of 2′-fluoro-3′-(substituted thiophenyl)deschloroepibatidine analogues (5a-f, 6a-d, and 7a-c) are presented herein. All had subnanomolar affinity at α4β2*-nAChRs. Contrary to lead structure epibatidine, a potent nAChR agonist, all were potent α4β2- and α3β4-AChR antagonists in an in vitro functional assay. In vivo, the compounds were also nAChR antagonists with various degrees of agonist activity. Compounds 5e, 5f, 6a, 6c, 6d, and 7c had no agonist effects in the tail-flick, hot-plate, hypothermia, or spontaneous activity tests, whereas 5a-d, 7a and 7b did not have agonist activity in the tail-flick and hot-plate tests but, like varenicline, were agonists in the hypothermia and spontaneous activity tests. Compound 6b had agonist activity in all four in vivo tests. All the compounds were antagonists of nicotine-induced antinociception in the tail-flick test, and all except 5c, 5d, 5f, and 6b were antagonists of nicotine-induced antinociception in the hot-plate test. Compound 7c, which had a Ki = 0.86 nM in the binding assay similar potency at α4β2/α3β4 with selectivity relative to α7 nAChRs, had an AD50 value of 0.001 μg/kg in the tail-flick test with no agonist activity in the in vitro or in vivo test had one of the more interesting profiles.
Thermal behaviour of dicarboxylic ester bithiophene polymers exhibiting a high open-circuit voltage
Heuvel, Ruurd,Colberts, Fallon J.M.,Wienk, Martijn M.,Janssen, René A.J.
, p. 3731 - 3742 (2018)
Nine different polythiophene derivatives based on dialkyl-(2,2′-bithiophene-5,5′-diyl)-4,4′-dicarboxylate (DCB) alternating with thiophene (T), bithiophene (2T) or thienothiophene (TT) as co-monomer have been synthesized to study the effect of the polymer backbone and side chain length on the thermal properties, the tendency to aggregate, and the photovoltaic performance. Polymers incorporating DCB and 2T show increased crystallinity and a large effect of the side chain length on the morphology of the photoactive layer blends. Thermal annealing increases the crystallinity of the polymers and enhances the long-wavelength light absorption. The concomitant increase in polymer fibre width, however, deteriorates the photovoltaic performance. The best devices were made using the PDCB-2T polymer with 2-butyloctyl side chains providing a power conversion efficiency of 5.18%. The PDCB-T polymer with 2-ethylhexyl substituents shows a comparable efficiency (5.08%), but with a significantly higher open-circuit voltage due to deeper frontier orbitals levels.
Substituted thiophene compound Preparation method and application thereof (by machine translation)
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Paragraph 0120-0122, (2021/01/11)
The invention relates to a thiophene compound represented by general formula I, a pharmaceutically acceptable salt thereof, a preparation method thereof, a pharmaceutical composition containing the thiophene compound and application thereof. The thiophene compound and a pharmaceutically acceptable salt thereof are taken as a novel estrogen-related receptor α (ERR RR) inverse agonist. These compounds can be used to treat diseases associated with ERR and ERR RR, such as cancer, osteoporosis, diabetes, anti-aging, slimming, and the like. After further optimization and screening, the drug is expected to be developed into novel drugs for preventing and treating tumors or other ERR RR related diseases. (by machine translation)
