126866-16-8Relevant articles and documents
Vicinal diaryl azole-based urea derivatives as potential cholesterol lowering agents acting through inhibition of SOAT enzymes
Pal, Palash,Gandhi, Hardik P.,Kanhed, Ashish M.,Patel, Nirali R.,Mankadia, Niraj N.,Baldha, Satish N.,Barmade, Mahesh A.,Murumkar, Prashant R.,Yadav, Mange Ram
, p. 107 - 123 (2017/03/02)
A novel series of vicinal diaryl azole-urea derivatives were synthesized and evaluated for their potential to inhibit SOAT enzyme. Among the reported compounds, compound (12d) emerged as the most potent compound with an IC50value of 2.43?μM. In polaxamer-407 induced lipoprotein lipase inhibition model, compound (12d) reduced triglyceride turnover in?vivo. Compound (12d) also showed dose-dependent prevention of serum total cholesterol and prevention of LDL-C elevation at a dose of 30?mg/kg. Furthermore, compound (12d) showed potential to stop falling levels of serum HDL-C dose-dependently and improved the atherogenic index. Effect of 12d on body weight, plaque formation and development of atherogenic lesions were studied. Toxicological study of compound (12d) indicated that at a dose of 2000?mg/kg, 12d was devoid of any signs of toxicity or mortality.
Synthesis of novel substituted diaryl-1,4-diazepines
Ramajayam,Giridhar, Rajani,Yadav
, p. 901 - 906 (2008/02/12)
In this paper a convenient route to new 2,3-diaryl-substituted 1,4-diazepines is described through cyclization of ethanedione derivatives and 1,3-propanediamine. The ethanedione derivatives required were synthesized by microwave-assisted oxidation from ethanones.