16035-97-5Relevant academic research and scientific papers
A new synthesis of 8-hydroxy-2-di-n-propylamino-tetralin (8-OH-DPAT)
Langlois,Gaudy
, p. 1723 - 1734 (1992)
A new synthesis method for 8-OH-DPAT, a specific agonist at the 5-HT(1A) serotonin receptor, is described. It employs the Curtius degradation of a tetralin carboxylic acid easily prepared from (2-methoxy benzyl) succinic acid by Friedel-Craft cyclisation.
Benzoxaborole antimalarial agents. Part 2: Discovery of fluoro-substituted 7-(2-carboxyethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles
Zhang, Yong-Kang,Plattner, Jacob J.,Freund, Yvonne R.,Easom, Eric E.,Zhou, Yasheen,Ye, Long,Zhou, Huchen,Waterson, David,Gamo, Francisco-Javier,Sanz, Laura M.,Ge, Min,Li, Zhiya,Li, Lingchao,Wang, Hailong,Cui, Han
, p. 1299 - 1307 (2012/03/26)
A series of new boron-containing benzoxaborole compounds was designed and synthesized for a continuing structure-activity relationship (SAR) investigation to assess the antimalarial activity changes derived from side-chain structural variation, substituent modification on the benzene ring and removal of boron from five-membered oxaborole ring. This SAR study demonstrated that boron is required for the antimalarial activity, and discovered that three fluoro-substituted 7-(2-carboxyethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles (9, 14 and 20) have excellent potencies (IC50 0.026-0.209 μM) against Plasmodium falciparum.
