736977-34-7Relevant articles and documents
Structure-Function Evaluation of Imidazopyridine Derivatives Selective for δ-Subunit-Containing γ-Aminobutyric Acid Type A (GABAA) Receptors
Yakoub, Kirsten,Jung, Sascha,Sattler, Christian,Damerow, Helen,Weber, Judith,Kretzschmann, Annika,Cankaya, Aylin S.,Piel, Markus,R?sch, Frank,Haugaard, Anne S.,Fr?lund, Bente,Schirmeister, Tanja,Lüddens, Hartmut
, p. 1951 - 1968 (2018/03/21)
δ-Selective compounds 1 and 2 (DS1, compound 22; DS2, compound 16) were introduced as functionally selective modulators of δ-containing GABA type A receptors (GABAAR). In our hands, [3H]EBOB-binding experiments with recombinant GABAAR and compound 22 showed no proof of δ-selectivity, although there was a minimally higher preference for the α4β3δ and α6β2/3δ receptors with respect to potency. In order to delineate the structural determinants of δ preferences, we synthesized 25 derivatives of DS1 and DS2, and investigated their structure-activity relationships (SAR). Four of our derivatives showed selectivity for α6β3δ receptors (29, 38, 39, and 41). For all of them, the major factors that distinguished them from compound 22 were variations at the para-positions of their benzamide groups. However, two compounds (29 and 39), when tested in the presence of GABA, revealed effects at several additional GABAAR. The newly synthesized compounds will still serve as useful tools to investigate α6β3δ receptors.
Method for synthesizing minodronate intermediate
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Paragraph 0038-0039, (2018/02/04)
The invention belongs to the field of chemical synthesis, relates to a chemical synthesis technology, in particular to a preparation method of a minodronate intermediate, and provides a method or effectively synthesizing a minodronate intermediate through three-component cascade reaction. The method comprises the steps that compounds II and III are condensed into a compound V at first under the acid catalysis effect, the compound V and a compound IV react to obtain a cyclization compound I, and the compound I is further converted into minodronate according to the mature technology path. The method is short in steps, mild in condition, capable of achieving atom economy, environmentally friendly, high in yield, low in cost and suitable for industrial production.
Novel one-pot pseudo four component reaction: Expeditious synthesis of functionalized imidazo[1,2-a]pyridines
Sanaeishoar, Haleh,Nazarpour, Roya,Mohave, Fouad
, p. 68571 - 68578 (2015/09/01)
A new and efficient one-pot synthesis of imidazo[1,2-a]pyridines has been described. In this approach the installation of C-3 imine substituent on the imidazopyridine framework was developed. Corresponding products were prepared in mild conditions by reac
