791809-44-4Relevant academic research and scientific papers
12-Tungstophosphoric acid supported on nano silica from rice husk ash as an efficient catalyst for direct benzylation of 1,3-dicarbonyl compounds in solvent-free condition
Rafiee, Ezzat,Khodayari, Maryam,Shahebrahimi, Shabnam,Joshaghani, Mohammad
, p. 204 - 209 (2011)
Nano silica has been prepared from rice husk, which is an agricultural waste, with high surface area and in amorphous form. 12-Tungstophosphoric acid, H3PW12O40 (PW) has been supported on this silica to produce nano silica supported PW (NPW/SiO2) as a nano catalyst. Characterization of this catalyst has been investigated by TEM, FTIR, and ICP, also, acidic properties have been studied by potentiometric titration method. 40% NPW/SiO2 has been used as a high effective catalyst for benzylation of 1,3-dicarbonyl compounds with benzylic alcohols. The present methodology offers a clean, practical, simple, mild, environmentally friendly, green and time-saving method under solvent free condition. Also, the catalyst is a good candidate for large-scale in direct benzylation of 1,3-dicarbonyl compounds.
Lead optimization of a pyrrole-based dihydroorotate dehydrogenase inhibitor series for the treatment of malaria
Kokkonda, Sreekanth,Deng, Xiaoyi,White, Karen L.,El Mazouni, Farah,White, John,Shackleford, David M.,Katneni, Kasiram,Chiu, Francis C. K.,Barker, Helena,Mclaren, Jenna,Crighton, Elly,Chen, Gong,Angulo-Barturen, Inigo,Jimenez-Diaz, Maria Belen,Ferrer, Santiago,Huertas-Valentin, Leticia,Martinez-Martinez, Maria Santos,Lafuente-Monasterio, Maria Jose,Chittimalla, Rajesh,Shahi, Shatrughan P.,Wittlin, Sergio,Waterson, David,Burrows, Jeremy N.,Matthews, Dave,Tomchick, Diana,Rathod, Pradipsinh K.,Palmer, Michael J.,Charman, Susan A.,Phillips, Margaret A.
, p. 4929 - 4956 (2020/06/08)
Malaria puts at risk nearly half the world's population and causes high mortality in sub-Saharan Africa, while drug resistance threatens current therapies. The pyrimidine biosynthetic enzyme dihydroorotate dehydrogenase (DHODH) is a validated target for malaria treatment based on our finding that triazolopyrimidine DSM265 (1) showed efficacy in clinical studies. Herein, we describe optimization of a pyrrole-based series identified using a target-based DHODH screen. Compounds with nanomolar potency versus Plasmodium DHODH and Plasmodium parasites were identified with good pharmacological properties. X-ray studies showed that the pyrroles bind an alternative enzyme conformation from 1 leading to improved species selectivity versus mammalian enzymes and equivalent activity on Plasmodium falciparum and Plasmodium vivax DHODH. The best lead DSM502 (37) showed in vivo efficacy at similar levels of blood exposure to 1, although metabolic stability was reduced. Overall, the pyrrole-based DHODH inhibitors provide an attractive alternative scaffold for the development of new antimalarial compounds.
PYRAZOLO [1,5-A] PYRIMIDINE ANALOGS FOR USE AS INHIBITORS OF STEAROYL-COA DESATURASE (SCD) ACTIVITY
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Page/Page column 34, (2010/11/29)
The present invention relates to compounds of the formula (I): including pharmaceutically acceptable salts, solvates, hydrates, geometrical isomers, tautomers, optical isomers, and N-oxides thereof, said compounds being useful as inhibitors of stearoyl-CoA desaturase (SCD). The invention further relates to the use of compounds of the formula (I) for treatment of medical conditions in which the modulation of SCD activity is beneficial, such as cardiovascular diseases, obesity, non- insulin-dependent diabetes mellitus, hypertension, neurological diseases, immune disorders, cancer, essential fatty acid deficiency, acne, psoriasis, rosacea or other skin conditions.
