18066-89-2Relevant articles and documents
Synthesis of Allocolchicine Conjugates with a Cetirizine Analog
Zotov,Shchegravina,Fedorov, A. Yu.
, p. 1498 - 1504 (2018)
Conjugates of allocolchicine and a cetirizine analog have been synthesized as potential anti-inflammatory and anti-allergic drugs.
Anti-inflammatory effects of two new methyl and morpholine derivatives of diphenhydramine on rats
Ahmadi, Abbas,Khalili, Mohsen,Hajikhani, Ramin,Safari, Narjes,Nahri-Niknafs, Babak
, p. 3532 - 3540 (2013/02/25)
Diphenhydramines are one of the first-generation histamine H1-receptor antagonists of the ethanolamine class that demonstrate many pharmacological properties including anti-inflammatory effects. In this research, bromo (II) and two new tolyl derivatives of I, (Di [p-tolyl] [dimethylaminoethoxy] methane, III) and (Di [p-tolyl] [2-morpholinoethoxy] methane, IV) were synthesized. Their acute and chronic anti-inflammatory activities were evaluated with the formalin and histamine-induced rat paw edema. The vascular permeability in formalin and histamine-induced paw edema, in xylene-induced ear edema, and in peritonitis after acetic acid application into peritoneal cavity were also measured and compared to II. Cotton pellet-induced granuloma model was selected for inducing chronic inflammations in rats. The newly synthesized analogs of diphenhydramine seemed effective to decrease acute inflammations. It was concluded that the prominent anti-phlogistic effects of the new drugs could be related to its reduction vascular permeability mechanism(s) or to its antagonistic effects on H1 histamine receptors. Springer Science+Business Media, LLC 2011.
Synthesis and anticonvulsant activity of some cinnamylpiperazine derivatives
Hu, Chuan,Sun, Zhi-Gang,Wei, Cheng-Xi,Quan, Zhe-Shan
, p. 661 - 664 (2011/11/29)
A series of cinnamylpiperazine derivatives was synthesized using different benzophenone as starting material. The structures of the compounds were proved by their IR, 1H-NMR spectroscopic data and mass spectra data. The anticonvulsant activities of these compounds were evaluated with maximal electroshock (MES) test and rotarod test with intraperitoneal injection on KunMing mice. Among all the flunarizine analogues, no one exhibited better anticonvulsant activity than flunarizine. Flunarizine (4i) exhibited anticonvulsant activity with ED50 of 38.1 mg/kg, TD50 of 164.3 mg/kg and PI of 4.3 through administration intraperitoneal, and with ED50 of 56.8 mg/kg, TD50 of 456.3 mg/kg and PI of 8.0 through oral administration.