91181-95-2Relevant academic research and scientific papers
Discovery of novel and ligand-efficient inhibitors of plasmodium falciparum and plasmodium vivax N-myristoyltransferase
Rackham, Mark D.,Brannigan, James A.,Moss, David K.,Yu, Zhiyong,Wilkinson, Anthony J.,Holder, Anthony A.,Tate, Edward W.,Leatherbarrow, Robin J.
supporting information, p. 371 - 375 (2013/02/23)
N-Myristoyltransferase (NMT) is an attractive antiprotozoan drug target. A lead-hopping approach was utilized in the design and synthesis of novel benzo[b]thiophene-containing inhibitors of Plasmodium falciparum (Pf) and Plasmodium vivax (Pv) NMT. These inhibitors are selective against Homo sapiens NMT1 (HsNMT), have excellent ligand efficiency (LE), and display antiparasitic activity in vitro. The binding mode of this series was determined by crystallography and shows a novel binding mode for the benzothiophene ring.
NOVEL COMPOUNDS AND THEIR USE IN THERAPY
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Page/Page column 67-68, (2013/06/27)
The invention provides compounds which inhibit N-myristoyltransferase and are selective for protozoal N-myristoyltransferase and, consequently suitable to treat microbial infections, including viral and fungal infections, and protozoan infections such as malaria, leishmaniasis and sleeping sickness.
Synthesis of benzofuran analogs of fenamates as non steroidal antiinflammatory agents
Mane, Balasaheb Y.,Agasimundin,Shivakumar
scheme or table, p. 264 - 269 (2010/11/04)
A series of benzofuran analogs of anthranilic acid derivatives are synthesized. All the new compounds have been characterized by spectral data and elemental analyses and screened for antiinflammatory activity. Compounds 3e, 4e, 4g and 5g are found to poss
APPLICATION OF MAGNESIUM ALKOXIDES TO SYNTHESES OF BENZOHETEROCYCLIC COMPOUNDS
Svoboda, Jiri,Nic, Miloslav,Palecek, Jaroslav
, p. 592 - 599 (2007/10/02)
The Dieckmann condensations of methyl -X-acetates Ia-Ih (X = O, S, SO2, NH, NCH3) initiated by action of magnesium methoxide, ethoxide, isopropoxide and other basic reagents have been studied under various conditions.Whereas magnesium methoxide has comparable efficiency as sodium methoxide and potassium tert-butoxide in syntheses of benzoheterocyclic compounds IIa-IIh, magnesium ethoxide gives the ethyl ester IIb in a medium yield, and magnesium isopropoxide is quite inefficient in the condensation reaction.The alkylation of the esters IIa, IId, and IIg with methyl chloroaetate in the presence of sodium hydride in dimethylformamide gives the diesters IIi-IIk which on action by potassium tert-butoxide undergo the cyclization reaction to give esters III.
