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The present invention refers to novel heterocyclic compounds and organic light emitting device using the same number […] substrate. (by machine translation)

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The invention relates to thiazine derivatives of the formula STR1 wherein R1 is lower alkyl and R2 is the residue of an aromatic heterocycle containing 1 to 4 hetero atoms optionally substituted by one or two lower alkyl groups, or a phenyl or benzyl group optionally substituted by halogen, hydroxy, lower alkyl, trifluoromethyl, nitro or lower alkoxy, and pharmaceutically acceptable salts thereof. The compounds of formula I are useful for the control or prevention of inflammation, pains, rheumatics and thromboses.

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A number of 3-phenylpiperazinylethyl pyrimido<5,4-b>benzofuran-2,4-dione and pyrimido<5,4-b>benzothiophene-2,4-dione derivatives 5-15 were designed as bioisosters of the previously reported pyrimido<5,4-b>indole-2,4-diones and synthesized starting from the 3-amino-2-carboxybenzofuran and benzothiophene ethyl and methyl esters respectively.They were evaluated for their in vitro alpha1-adrenoceptor and 5HT1A-receptor affinities by radioligand receptor binding assays.All target compounds showed good to excellent affinities for the alpha1-adrenoceptor with Ki values in the subnanomolar range.Some compounds were also good ligands for the 5HT1A-receptor with Ki values in the nanomolar range. 3-<2-<4-(2-Methoxyphenyl)piperazin-1-yl>ethyl>-1-methyl pyrimido<5,4-b>benzothiophen-2,4-dione 15 was the most active derivative in displacing <3H>-8-OH-DPAT from rat hippocampal membranes.There is evidence suggesting that the N1 methyl group of the tricyclic moiety of the title compounds is probably able to undergo a Van der Walls interaction at the 5HT1A-receptor binding site but not at the alpha1-adrenoceptor active site. pyrimido<5,4-b>benzofurans / pyrimido<5,4-b>benzothiophenes / alpha1-adrenoceptor binding / 5HT1A-receptor binding

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In search of a uroselective agent that exhibits a high level of selectivity for the alpha(1A) receptor, a novel series of tricyclic hexahydrobenz[e]isoindoles was synthesized. A generic pharmacophoric model was developed requiring the presence of a basic amine core and a fused heterocyclic side chain separated by an alkyl chain. It was shown that the 6- OMe substitution with R, R stereochemistry of the ring junction of the benz[e]isoindole and a two-carbon spacer chain were optimal. In contrast to the highly specific requirements for the benz[e]isoindole portion and linker chain, a wide variety of tricyclic fused heterocyclic attachments were tolerated with retention of potency and selectivity. In vitro functional assays for the alpha1 adrenoceptor subtypes were used to further characterize these compounds, and in vivo models of vascular vs prostatic tone were used to assess uroselectivity.

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The palladium-catalyzed Matsuda-Heck and Suzuki-Miyaura cross-couplings of 2-methoxycarbonylthiophene-3-diazonium tetrafluoroborate 1 were performed to synthesize a series of thiophene derivatives functionalized in the beta-position. Good to excellent yields of the cross-coupling products were obtained using palladium acetate [Pd(OAc)2], a ligandless palladium catalyst, without a base, at room temperature, under aerobic conditions and with short reaction times. A diazotization and cross-coupling sequence can also be performed in a one-pot process avoiding the isolation of the thiophenediazonium salt derivative. In addition, 2-methoxycarbonylbenzo[b]thiophene-3-diazonium tetrafluoroborate 8 was also efficiently arylated by applying the same Suzuki-Miyaura optimized reaction conditions. Copyright

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35212-85-2, Chemical Research Letters, May 2021. Reactions catalyzed within inorganic and organic materials and at electrochemical interfaces commonly occur at high coverage, causing turnover rates to depend strongly on interfacial structure. In a article, 35212-85-2, molcular formula is C10H9NO2S, introducing its new discovery.

The present invention refers to novel heterocyclic compound and organic light emitting number including […] substrate. (by machine translation)

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Synthetic Route of 35212-85-2, Chemical Research Letters, May 2021. The transformation of simple hydrocarbons into more complex and valuable products via catalytic C–H bond functionalisation has revolutionised modern synthetic chemistry. In a article, 35212-85-2, molcular formula is C10H9NO2S, introducing its new discovery.

Acylic n-hydroxy imides and their use in pharmaceutical compositions and in the inhibition of flap endonuclease are disclosed

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The synthesis of a new family of benzyl derivatives of 2,1,3-benzo- and benzothieno[3,2-a]-thiadiazine 2,2-dioxides was achieved. The biological data revealed the first heterocyclic family of compounds with PDE 7 inhibitory properties appearing to be a new objective for the treatment of T-cell- dependent disorders. The IC50 values or percent inhibition values of the compounds against PDE 7 were calculated by testing them against human recombinant PDE 7 expressed in S. cerevisiae. In this expression system the only cyclic nucleotide hydrolyzing activity present in cell extracts corresponded to human PDE 7. Isoenzyme selectivity PDE 7 versus PDE 4 and PDE 3 was also measured. Considering simultaneously inhibition of the three different isoenzymes, monobenzyl derivatives 15 and 23 showed interesting PDE 7 potency (around 10 muM); although not statistically significant, a trend toward selectivity with respect to PDE 3 and PDE 4 was obtained. Benzothiadiazine 16, although less potent at PDE 7 (IC50 = 25 muM), also showed a trend of selectivity toward PDE 3 and PDE 4. These compounds are considered the best leads for further optimization.

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New Advances in Chemical Research in 2021. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction by binding to a specific portion of an enzyme and thus slowing or preventing a reaction from occurring. Computed Properties of C10H9NO2S, In an article, mentioned the application of 35212-85-2, Name is Methyl 3-aminobenzo[b]thiophene-2-carboxylate, molecular formula is C10H9NO2S

Several novel 3-(aryl)benzothieno[2,3-c]pyran-1-ones (tricyclic lactones) were prepared either by a tandem one-pot Sonogashira coupling and intramolecular cyclization, reacting the 3-bromobenzo[b]thiophene-2-carboxylic acid with arylacetylenes, or by Sonogashira coupling of the methyl 3-bromobenzo[b]thiophene-2-carboxylate or the methyl 3-bromo-6-methoxybenzo[b]thiophene-2-carboxylate with arylacetylenes followed by an electrophilic intramolecular cyclization using iodine or TFA in two separate steps. The Sonogashira products and the tricyclic lactones obtained were evaluated for their capacity to inhibit the in vitro growth of three human tumor cell lines, MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer) and SF-268 (CNS cancer). Most of the compounds showed a high growth inhibitory effect on all the tested cell lines, with GI50 values in the muM range. A structure-activity relationship was established for the Sonogashira products and for the tricyclic lactones, namely related to the presence and position of substituents (OMe and/or F) in the benzothiophene moiety or in the phenyl ring.

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The present paper describes the synthesis and the binding properties for the serotonergic 5-HT7 and 5-HT1A receptors of three new series (A?C) of (benzo)thienopyrimidinone derivatives. All series exhibit a basic moiety at the 2-position of the heterocyclic scaffold such as N,N-dialkylaminoalkylthio chain in series A and phenylpiperazine, benzylpiperazine, or benzylpiperidine alkyl chain in series B and C. Compounds endowed with the best binding properties at 5-HT7R belong to the B and C types. In particular, derivatives B2 and C1 (RSC4) exhibit notable affinity for 5-HT7R (Ki = 9.08 and 0.85 nM, respectively) and selectivity over the 5-HT1AR (254- and 48-fold, respectively). The structure-affinity relationships for these three new classes of 5-HT7R ligands are discussed and, in order to rationalize and deeply investigate the observed results, molecular modeling studies were performed. In particular, the binding poses of the synthesized compounds were studied by docking them in the two receptor proteins suitably built by homology modeling. The calculated binding energies resulted in an excellent agreement with the experimental measured Ki, further validating the quality of the models.

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Benzothiophene – Wikipedia,
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