2986-19-8Relevant articles and documents
Selenium-containing compounds and their use in treatment of neuro-degenerative diseases
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Paragraph 0089; 0097-0099, (2020/12/30)
The present invention relates to compounds of Formula I or pharmaceutically acceptable salts, solvates or pro-drugs thereof. The invention also relates to a preparation method of the compound or the pharmaceutically acceptable salt, solvate or prodrug thereof, a pharmaceutical composition containing the compound or the pharmaceutically acceptable salt, solvate or prodrug thereof and application ofthe compound or the pharmaceutically acceptable salt, solvate or prodrug thereof in preparation of drugs. The drugs are used for treating neuro-degenerative diseases.
Structure-Activity Relationship of Hetarylpropylguanidines Aiming at the Development of Selective Histamine Receptor Ligands?
Pockes, Steffen,Wifling, David,Buschauer, Armin,Elz, Sigurd
, p. 285 - 297 (2019/04/04)
New classes of alkylated hetarylpropylguanidines with different functionality and variation in spacer length were synthesized to determine their behavior at the four histamine receptor (H1R, H2R, H3R, H4R) subtypes. Alkylated guanidines with different terminal functional groups and varied basicity, like amine, guanidine and urea were developed, based on the lead structure SK&F 91486 (2). Furthermore, heteroatomic exchange at the guanidine structure of 2 led to simple analogues of the lead compound. Radioassays at all histamine receptor subtypes were accomplished, as well as organ bath studies at the guinea pig (gp) ileum (gpH1R) and right atrium (gpH2R). Ligands with terminal functionalization led to, partially, highly affine and potent structures (two digit nanomolar), which showed up a bad selectivity profile within the histamine receptor family. While the benzoylurea derivative 144 demonstrated a preference towards the human (h) H3R, S-methylisothiourea analogue 143 obtained high affinity at the hH4R (pKi=8.14) with moderate selectivity. The molecular basis of the latter finding was supported by computational studies.
Synthesis and cytotoxic activity of 2,5-disubstituted pyrimido[5,4-c] quinoline derivatives
Zhang, Fan,Zhai, Xin,Chen, Li Juan,Qi, Jian Guo,Cui, Bo,Gu, Yu Cheng,Gong, Ping
scheme or table, p. 1277 - 1280 (2012/01/06)
A series of 2,5-disubstituted pyrimido[5,4-c]quinoline derivatives were synthesized and their cytotoxic activity against H460, HT-29 and MDA-MB-231 cell lines was evaluated in vitro. It was found that most of the tested compounds especially compound 17, s