19676-63-2Relevant academic research and scientific papers
Synthesis, antiepileptic effects, and structure-activity relationships of α-asarone derivatives: In vitro and in vivo neuroprotective effect of selected derivatives
Zhang, Jian,Mu, Keman,Yang, Peng,Feng, Xinqian,Zhang, Di,Fan, Xiangyu,Wang, Qiantao,Mao, Shengjun
, (2021/08/03)
In the present study, we compared the antiepileptic effects of α-asarone derivatives to explore their structure-activity relationships using the PTZ-induced seizure model. Our research revealed that electron-donating methoxy groups in the 3,4,5-position on phenyl ring increased antiepileptic potency but the placement of other groups at different positions decreased activity. Besides, in allyl moiety, the optimal activity was reached with either an allyl or a 1-butenyl group in conjugation with the benzene ring. The compounds 5 and 19 exerted better neuroprotective effects against epilepsy in vitro (cell) and in vivo (mouse) models. This study provides valuable data for further exploration and application of these compounds as potential anti-seizure medicines.
Carboxylated, heteroaryl-substituted chalcones as inhibitors of vascular cell adhesion molecule-1 expression for use in chronic inflammatory diseases
Meng, Charles Q.,Ni, Liming,Worsencroft, Kimberly J.,Ye, Zhihong,Weingarten, M. David,Simpson, Jacob E.,Skudlarek, Jason W.,Marino, Elaine M.,Suen, Ki-Ling,Kunsch, Charles,Souder, Amy,Howard, Randy B.,Sundell, Cynthia L.,Wasserman, Martin A.,Sikorski, James A.
, p. 1304 - 1315 (2008/02/02)
Starting from a simple chalcone template, structure-activity relationship (SAR) studies led to a series of carboxylated, heteroaryl-substituted chalcone derivatives as novel, potent inhibitors of vascular cell adhesion molecule-1 (VCAM-1) expression. Corr
SUBSTITUTED BENZYLAMINOQUINUCLIDINES AS SUBSTANCE P ANTAGONISTS
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, (2008/06/13)
Compounds useful in the treatment of inflammatory disorders, central nervous system disorders and other disorders of the formula I STR1 and the pharmaceutically-acceptable salts thereof, wherein Ar. sup.1 and Ar 2 are each independently aryl or substituted aryl; R 1 is alkyl having from 1 to 6 carbon atoms;R 2 is hydrogen or alkyl having from 1 to 6 carbon atoms;and either X and Y are taken separately and they are each, independently, hydrogen, dialkylphosphoryl having 2 to carbon atoms, alkyl having from 1 to 6 carbon atoms, alkenyl having from 2 to 6 carbon atoms or alkynyl having from 2 to 6 carbon atoms; or X and Y are taken together and they represent a hydrocarbon chain having 3, 4, or 5 carbon atoms, optionally containing up to 2 double bonds and optionally having 1 or 2 substituents selected from oxo, hydroxy and alkyl having from 1 to 6 carbon atoms; or Y is methoxy when X is ethyl; provided that when X and Y are taken together they are attached to adjacent carbon atoms; and provided that if either X or Y is hydrogen, then the other one must be alkenyl or alkynyl; and provided that when Y is methoxy and X is ethyl, then Y is at the 4-position and X is at the 5-position, Ar 1 or Ar 2 must each be phenyl, R. sup.1 is methyl and R 2 is hydrogen.
Vilsmeier-Haack Reaction on Methoxyallylbenzenes
Narasimhan, N. S.,Mukhopadhyay, T.,Kusurkar, S. S.
, p. 546 - 548 (2007/10/02)
Vilsmeier-Haack reaction on various methoxyallylbenzenes yields the naphthaldehydes (2, 11, 14, 17, 20, 21) when ortho-position to the allyl group is activated.In other cases only nuclear formylated products are obtained.The product analysis suggests that nuclear formylation is probably the first step in these reactions.
