246240-16-4Relevant articles and documents
Design, synthesis and biological evaluation of novel inosine 5′-monophosphate dehydrogenase (IMPDH) inhibitors
Dunkern, Torsten,Chavan, Sunil,Bankar, Digambar,Patil, Anuja,Kulkarni, Pritee,Kharkar, Prashant S.,Prabhu, Arati,Goebel, Heike,Rolser, Edith,Burckhard-Boer, Waltraud,Arumugam, Premkumar,Makhija, Mahindra T.
, p. 408 - 419 (2014/06/09)
This study is based on our attempts to further explore the structure-activity relationship (SAR) of VX-148 (3) in an attempt to identify inosine 5′-mono-phosphate dehydrogenase (IMPDH) inhibitors superior to mycophenolic acid. A five-point pharmacophore developed using structurally diverse, known IMPDH inhibitors guided further design of novel analogs of 3. Several conventional as well as novel medicinal chemistry strategies were tried. The combined structure- and ligand-based approaches culminated in a few analogs with either retained or slightly higher potency. The compounds which retained the potency were also checked for their ability to inhibit human peripheral blood mononuclear cells proliferation. This study illuminates the stringent structural requirements and strict SAR for IMPDH II inhibition.
A mild and efficient method for preparation of azides from alcohols using acidic ionic liquid [H-NMP]HSO4
Hajipour, Abdol R.,Rajaei, Asiyeh,Ruoho, Arnold E.
supporting information; experimental part, p. 708 - 711 (2011/03/17)
We report here an efficient method for the synthesis and characterization of [H-NMP]HSO4 and its application as an efficient catalyst and solvent for preparation of azides from corresponding alcohols under mild conditions. This processor showed
