23510-18-1Relevant articles and documents
Design, Synthesis and Preliminary Evaluation of Novel Imperatorin Derivatives as Vasorelaxant Agents
Li, Na,He, Jianyu,Zhan, Yingzhuan,Zhou, Nan,Zhang, Jie
experimental part, p. 18 - 23 (2012/01/11)
A series of novel imperatorin derivatives were synthesized from commercially available xanthotoxin. The in vitro pharmacological evaluation indicated that all of the compounds possessed potent vasodilatory activity. Among them, compounds (5b), (5d) and (5e) exhibited higher vasdilatory activity (with EC50 values of 0.68 μM, 0.59 μM and 0.49 μM, respectively) than imperatorin (EC50 = 1.12 μM). The program Volsurf was used to predict the derivatives' ADMErelevant descriptors. The results suggested that these novel compounds had a potential interest for the development of novel and potent vasorelaxant agents.
Diaryldiamines with dual inhibition of the histamine H3 receptor and the norepinephrine transporter and the efficacy of 4-(3-(methylamino)-1- phenylpropyl)-6-(2-(pyrrolidin-1-yl)ethoxy)naphthalen-1-ol in pain
Altenbach, Robert J.,Black, Lawrence A.,Strakhova, Marina I.,Manelli, Arlene M.,Carr, Tracy L.,Marsh, Kennan C.,Wetter, Jill M.,Wensink, Erica J.,Hsieh, Gin C.,Honore, Prisca,Garrison, Tiffany Runyan,Brioni, Jorge D.,Cowart, Marlon D.
supporting information; experimental part, p. 7869 - 7873 (2011/01/12)
A series of compounds was designed as dual inhibitors of the H3 receptor and the norepinephrine transporter. Compound 5 (rNET Ki = 14 nM; rH3R Ki = 37 nM) was found to be efficacious in a rat model of osteoarthritic pain.
6-Substituted 6H-dibenzo[c,h][2,6]naphthyridin-5-ones: Reversed lactam analogues of ARC-111 with potent topoisomerase I-targeting activity and cytotoxicity
Zhu, Shejin,Ruchelman, Alexander L.,Zhou, Nai,Liu, Angela,Liu, Leroy F.,LaVoie, Edmond J.
, p. 3131 - 3143 (2007/10/03)
6-Substituted 8,9-dimethoxy-2,3-methylenedioxy-6H-dibenzo[c,h][2,6] naphthyridin-5-ones were synthesized and evaluated for topoisomerase I-targeting activity and cytotoxicity. Several of these reversed lactam analogues of ARC-111 exhibited exceptional cyt