73278-98-5Relevant articles and documents
H2-Antihistaminics, XXXIII: Synthesis and H2-antagonistic activity of heteroaromatic (Thio)carboxamides and triazole(thi)one-derivatives of piperidinomethylphenoxypropylamine
Wegner,Kramer,Schunack
, p. 108 - 114 (1987)
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A preparation method for rosacea acetate hydrochloride
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Paragraph 0105; 0109, (2021/12/07)
The present invention relates to the field of pharmaceutical preparation technology, in particular to a method for preparing rosatidine acetate hydrochloride. The present invention adopts m-hydroxybenzoic acid as a starting material, a wide range of sources, inexpensive, and it can be prepared by oxidation of m-hydroxytoluene, without involving a toxicity warning structure and nitrosamine impurities; at the same time, in this preparation process only involves a genotoxic warning structure substance, reducing the risk of medication of subsequent drugs.
Hexacyclododecylamines with sigma-1 receptor affinity and calcium channel modulating ability
Joubert, Jacques,Strydom, Natasha,Geldenhuys, Werner J.,Greyling, Yolande,Dyk, Sandra V.,Malan, Sarel F.
, p. 29 - 39 (2019/05/24)
Recent research points to the Sigma Receptor (σR) as a possible neuromodulatory system with multi-functional action and σ1Rs have been suggested as a drug target for a number of CNS conditions. Hexacyclododecylamines have shown σ1R activity and provide an advantageous scaffold for drug design that can improve the blood-brain barrier permeability of privileged structures. A series of oxa-and aza-hexaxcyclododecylamines were synthesised and evaluated for sigma-1 receptor activity and voltage-gated calcium channel blocking ability to determine the effect of inclusion of amine containing heterocycles. The compounds had promising σ1R activities (Ki = 0.067 – 11.86 μM) with the aza-hexacyclododecylamines 12, 24 and 27 showing some of the highest affinities (Ki = 0.067 μM, 0.215 μM and 0.496 μM respectively). This confirms, as observed in previous studies, that the aza compounds are more favourable for σ1R binding than their oxa counterparts. The addition of the amine heterocycle showed affinities similar to that of related structures with only two lipophilic binding regions. This indicates that the inclusion of an amine heterocycle into these structures is a viable option in the design of new σ1R ligands. Significant voltage-gated calcium channel blocking ability was also observed for 12, 24 and 27, suggesting a link between σ1R activity and intracellular calcium levels.