57598-33-1Relevant articles and documents
Synthesis, characterization and biological evaluation of benzimidazole and benzindazole derivatives as anti-hypertensive agents
Silky, Sethy,Mandal, Sudip Kumar,Ewies, Ewies Fawzy,Neerupma, Dhiman,Arun, Garg
, p. 3659 - 3664 (2021/07/10)
A substituted benzimidazole and benzindazole derivatives had been synthesized having antihypertensive activity through antagonizing the angiotensin II (Ang II) receptors. The in vivo antihypertensive activity of the compounds was done with acute renal hypertension model. Two compounds TG 1 and TG 3 were found to have antihypertensive activity comparable to Telmisartan which is a prototype for Angiotensin II receptor antagonists class of drugs.In an antihypertensive study the compounds TG 1, TG 2 and TG 3 had systolic blood pressures of 147.2 mm/Hg, 168.2 mm/Hg, and 126.3 mm/Hg, respectively. This systolic blood pressure was lower than the disease control vehicle-treated rodents, which had a systolic blood pressure of 167.2 mm/Hg. The diastolic blood pressure was 119.7 mm/Hg, 124.7 mm/Hg and 88.83 mm/Hg, respectively and that of the disease control vehicle-treated rodents was 122.3 mm/Hg. TG 3 had comparable decrease in the MABP to Telmisartan. These encouraging results make compound TG 3 effective anti-hypertensive drug candidate and worthy of further investigation.
Improved synthesis of valsartan via nucleophilic aromatic substitution on aryloxazoline
Ghosh, Samir,Kumar, A. Sanjeev,Soundararajan,Mehta
body text, p. 3880 - 3887 (2009/12/24)
A highly efficient approach to the synthesis of the angiotensin II receptor antagonist valsartan (Diovan), one of the most important agents used in antihypertensive therapy today is described. The formation of the aryl-aryl bond represents the key step of its synthesis, which has been done by simple nucleophelic aromatic substitution on aryloxazoline with good yield and purity. Copyright Taylor & Francis Group, LLC.
Synthesis and X-ray crystal structure of 1,4-dihydro-2,6-dimethyl-4-(2'-isopropylphenyl)-3,5-pyridine-dicarboxy lic acid dimethyl ester: A nifedipine analogue
Palmer, Robert B.,Andersen, Niels H.
, p. 2173 - 2176 (2007/10/03)
We report the synthesis and X-ray crystal structure of 1,4-dihydro-2,6-dimethyl-4-(2'-isopropylphenyl)-3,5-pyridine-dicarboxy lic acid dimethyl ester (4), an analogue of the 1,4-dihydropyridine calcium channel antagonist, nifedipine. Solution state NOE data indicate the presence of both rotameric forms. The solid state shows exclusively one rotamer of 4 (that in which the 2'-isopropyl substituents is syn with C4H, which is also the major solution state rotamer). The 3,5-methyl esters adopt an ap/sp orientation with respect to the dihydropyridine double bonds in the solid state.
