217170-70-2Relevant academic research and scientific papers
Design, Synthesis and Antimalarial Activity of Some New minoalcoholpyrrolo[ 1,2-A]quinoxaline Derivatives
Guillon, Jean,Moreau, Stéphane,Ronga, Luisa,Basmacyian, Louise,Cohen, Anita,Rubio, Sandra,Bentzinger, Guillaume,Savrimoutou, Solène,Azas, Nadine,Mullié, Catherine,Sonnet, Pascal
, p. 932 - 942 (2016/11/02)
Following our search for antimalarial compounds, novel series of piperazinylalcohol pyrrolo 1,2-A]quinoxaline derivatives 1-2 were synthesized from 2-nitroaniline or 2-Amino-3 nitrophenol and tested for in vitro activity upon the intraerythrocytic stage of W2 and 3D7 Plasmodiu falciparum strains. Biological results showed good antimalarial activity with IC50 ranging fro 0.3 to 21.1 M. In attempting to investigate the large broad-spectrum antiprotozoal activities of thes pyrrolo[1,2-A]quinoxaline derivatives, their properties toward the promastigote form of Leishmani donovani were also investigated and revealed their selective antiplasmodial profile. In parallel, the i vitro cytotoxicity of these molecules was assessed on the human HepG2 cell line. Structure-Activit relationships of these new synthetic compounds are here discussed.
Design, synthesis, and structure-activity relationships of phthalimide- phenylpiperazines: A novel series of potent and selective {1a)-adrenergic receptor antagonists
Kuo, Gee-Hong,Prouty, Catherine,Murray, William V.,Pulito, Virginia,Jolliffe, Linda,Cheung, Peter,Varga, Sally,Evangelisto, Mary,Wang, Jian
, p. 2183 - 2195 (2007/10/03)
Beginning from the screening hit and literature α1-adrenergic compounds, a hybridized basic skeleton A was proposed as the pharmacophore for potent and selective α(1a)-AR antagonists. Introduction of a hydroxy group to increase the flexibility
Design, synthesis and biological evaluation of pyridine-phenylpiperazines: A novel series of potent and selective α(1a)-adrenergic receptor antagonist
Kuo, Gee-Hong,Prouty, Catherine,Murray, William V.,Pulito, Virginia,Jolliffe, Linda,Cheung, Peter,Varga, Sally,Evangelisto, Mary,Shaw, Charles
, p. 2263 - 2275 (2007/10/03)
Beginning from the screening hit and literature α1-adrenergic compounds, a hybridized basic skeleton A was proposed as the pharmacophore for potent and selective α(1a)-AR antagonists. Introduction of a hydroxy group to increase the flexibility
Studies on quinazolines IX:1 Fluorination versus 1,2-migration in the reaction of 1,3-bifunctionalized amino-2-propanol with DAST
Chern, Ji-Wang,Chang, Jun-Yi,Usifoh, Cyril O.,Gutsait, Alexander
, p. 8483 - 8486 (2007/10/03)
Treatment of 1-phthaloylamino-3-[4-(2-methoxyphenyl)piperazin-1-yl]- propanol (7) with DAST induced 1,2-migration via a proposed spiro-aziridinium intermediate to give N-[2-fluoro-3-[4-(2-methoxyphenyl)piperazin-1- yl]propyl]-phthalimide (11a) in 13% yield and N-12-fluoromethyl-2-[4-(2- methoxyphenyl)-piperazin-1-yl]ethyl]phthalimide (11b) in 73% yield.
