133311-45-2Relevant academic research and scientific papers
Discovery of 1-aryloxyethyl piperazine derivatives as Kv1.5 potassium channel inhibitors (part I)
Guo, Xiaoke,Ma, Xianglei,Yang, Qian,Xu, Jing,Huang, Lu,Jia, Jianmin,Shan, Jiaojiao,Liu, Li,Chen, Weilin,Chu, Hongxi,Wei, Jinlian,Zhang, Xiaojin,Sun, Haopeng,Tang, Yiqun,You, Qidong
supporting information, p. 89 - 94 (2014/06/09)
Kv1.5 potassium channel is an efficacious and safe therapeutic target for the treatment of atrial fibrillation (AF), the most common arrhythmia that threatens human. Herein, by modifying the hit compound 7k from an in-house database, 48 derivatives were synthesized for the assay of their Kv1.5 inhibitory effects by whole cell patch clamp technique. Six compounds which showed better potency than the positive compound dronedarone were selected for the next evaluation of their drug-like properties. Compound 8 exhibited balanced solubility and permeability. It also showed acceptable pharmacodynamics profile with very low acute toxicity. Taking all these data into account, compound 8 can serve as a promising lead for the development of novel therapeutic agent for the treatment of AF.
Antipicornaviral pyridazinamines
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, (2008/06/13)
Piperidinyl, pyrrolidinyl, azepinyl and piperazinyl pyridazines of formula STR1 wherein one or two carbon atoms of the STR2 moiety may be substituted with C1-4 alkyl, C1-4 alkyloxy or two carbon atoms of the CH2 groups of said moiety may be bridged with a C2-4 alkanediyl radical; X represents CH or N; R1 represents hydrogen, C1-4 alkyl, halo, hydroxy, trifluoromethyl, cyano, C1-4 alkyloxy, C1-4 alkylthio, C1-4 alkylsulfinyl, C1-4 alkylsulfonyl, C1-4 alkyloxycarbonyl, C1-4 alkylcarbonyl or aryl; R2 and R3 each independently represent hydrogen or C1-4 alkyl; Alk represents C1-4 alkanediyl; R4 and R5 each independently represent hydrogen, C1-4 alkyl or halo; and Het represents STR3 the addition salts and stereochemically isomeric forms thereof, said compounds having antipicornaviral activity. Pharmaceutical compositions containing these compounds as active ingredient, and a method of preparing said compounds and pharmaceutical compositions.
