1008-76-0 Dopamine/serotonin receptor ligands. 10: SAR studies on azecine-type dopamine receptor ligands by functional

On the basis of the benz[d]indolo[2,3-g]azecine derivative 1 (LE300), structure-activity relations were investigated in order to identify the pharmacophore in this new class of ligands. Various structural modifications were performed and the inhibitory activities at human cloned D1, D2L, and D5 receptors were measured by using a simple fluorescence microplate reader based calcium assay. Subsequently, the affinities of active compounds were estimated by radioligand binding experiments, Deleting one of the aromatic rings as well as replacing it by a phenyl moiety abolishes the inhibitory activities almost completely. Contraction of the 10-membered central ring decreases them significantly. The replacement of indole by thiophene or N-methylpyrrole reduces the inhibitory activity, whereas replacing the indole by benzene increases it. Finally, the hydroxylated dibenz[d,g]azecine derivative 11d (LE404) was found to be more active than the lead 1 in the functional calcium assay as well as in radioligand displacement experiments. https://www.lookchem.com/CASDataBase_1008-76-0.htm

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1023-17-2 Syntheses, structures, and catalytic activity in Friedel–Crafts acylations of substituted tetramethylcyclopentadienyl molybdenum carbonyl complexes

Reactions of the substituted tetramethylcyclopentadienes [C 5 HMe 4 R] [R?=? t Bu, Ph, CH 2 CH 2 C(CH 3 ) 3 ] with Mo(CO) 3 (CH 3 CN) 3 in refluxing xylene gave a series of dinuclear molybdenum carbonyl complexes [(η 5 -C 5 Me 4 R)Mo(CO) 3 ] 2 [R?=? t Bu (1), Ph (2), CH 2 CH 2 C(CH 3 ) 3 (3)], [(η 5 -C 5 Me t Bu)Mo(μ-CO) 2 ] 2 (4)], and [(η 5 -C 5 Me 4 ) t Bu] 2 Mo 2 O 4 (μ-O) (5)], respectively. Complexes 1–5 were characterized by elemental analysis, IR, 1 H NMR, and 13 C NMR spectroscopy. In addition, their crystal structures were determined by X-ray crystal diffraction analysis. The catalytic activities of complexes 1–3 in Friedel–Crafts acylation in the presence of o-chloranil has also been investigated; the reactions were achieved under mild conditions to give the corresponding products in moderate yields. https://www.lookchem.com/CASDataBase_1023-17-2.htm
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7440-47-3 Influence of pulse plating on the crystal structure and orientation of chromium

Chromium deposits with various structures and orientations were prepared by pulse plating from a sulfate-catalyzed chromic acid solution and without formic acid addition. The influences of the puls duration, off-time, curent density, formic acid concentration, and plating time on the structure and orientation were studied by X-Ray diffraction and transmition electron microcsopy. https://www.lookchem.com/CASDataBase_7440-47-3.htm
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101219-73-2 Influences of electronic effects and anions on the enantioselectivity in the oxazaborolidine-catalyzed asymmetric borane reduction of ketones

The influence of electronic effects on the enantioselectivity of the oxazaborolidine-catalyzed asymmetric borane reduction of ketones has been observed and investigated with use of parasubstituted acetophenones and propiophenones with a variety of functional groups and B-unsubstituted and B-methoxyoxazaborolidines derived from (S)-2-(diphenylhydroxymethyl)-pyrrolidine with borane and trimethyl borate as catalysts in toluene and THF. The results indicate that Hammett linear free energy electronic effects on the enantioselectivity in the asymmetric reduction were observed and rationalized. Tuning electronic effects of the catalyst can improve the enantioselectivity in the reduction. Another interesting finding to be noted is that anions heavily affect the enantioselectivity, especially for the B-methoxy catalyst, because of their coordination with the boron atom in the catalysts. https://www.lookchem.com/CASDataBase_101219-73-2.htm
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