96225-46-6Relevant academic research and scientific papers
THIOPHENE DERIVATIVES FOR THE TREATMENT OF DISORDERS CAUSED BY IGE
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Page/Page column 187, (2020/01/11)
Thiophene derivatives of formula (I) and a pharmaceutically acceptable salt thereof are provided. These compounds have utility for the treatment or prevention of disorders caused by IgE, such as allergy, type 1 hypersensitivity or familiar sinus inflammation.
Design, synthesis, and evaluation of a novel dual fms-like tyrosine kinase 3/stem cell factor receptor (FLT3/c-KIT) inhibitor for the treatment of acute myelogenous leukemia
Davies, Robert J.,Pierce, Albert C.,Forster, Cornelia,Grey, Ron,Xu, Jinwang,Arnost, Michael,Choquette, Deborah,Galullo, Vincent,Tian, Shi-Kai,Henkel, Greg,Chen, Guanjing,Heidary, David K.,Ma, Joanne,Stuver-Moody, Cameron,Namchuk, Mark
supporting information; experimental part, p. 7184 - 7192 (2011/12/03)
A high-throughput screen of our compound archive revealed a novel class of dual FMS-like tyrosine kinase 3 (FLT3)/c-KIT inhibitors. With the help of molecular modeling, this class was rapidly optimized for both potency against FLT3 and FLT3/c-KIT and exce
α1-Adrenoceptor blocking activity of some ring-open analogues of prazosin
Boschi,Di Stilo,Fruttero,Medana,Sorba,Gasco
, p. 661 - 667 (2007/10/02)
Synthesis and structural characterization of some ring-open analogues of Prazosin containing either the guanidine substructure or urea-equivalent groups are described. The opening of the pyrimidine ring in Prazosin is very important as far as the affinity for α1-adrenoceptor is concerned. The pA2 values of the ring-open derivatives are 104-105 fold lower than that of the parent. It is probable that the affinity decrease principally reflects a negative influence of the conformational factors in the interaction with the α1-receptor. The derivative 5 containing the guanidine moiety, charged at physiological pH, is as active as the other derivatives containing the uncharged urea-equivalent groups. This behaviour indicates, in this class of compounds, the importance of H-bonding interactions with the receptor. When in the ring-open models the ethanediamino substructure is substituted for the piperazine ring additional decrease in activity occurs.
