133051-88-4Relevant 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.
Synthesis and selective cytotoxicity of novel biphenyl-based tetrazole derivatives
Malani, Mahesh H.,Dholakiya, Bharatkumar Z.,Ibrahim, Ahmed S.,Badria, Farid A.
, p. 4427 - 4435 (2015/04/22)
Cancer today represents a significant public health problem worldwide, and the challenge is to produce cost-effective drugs. Recently, biphenyl compounds as well as tetrazole derivatives is known for their potential nonselective anticancer activities. In search of novel selective anticancer agents, a series of newly hybrid molecules was designed and synthesized by combining the structural features of biphenyl and tetrazole moieties. The structures of newly synthesized compounds were characterized using spectroscopic techniques (FT-IR, 1H NMR, 13C NMR, and HMBC). Cytotoxic evaluations of these novels compound on human cancer cell lines showed a significant anticancer activity against more than one tested cell lines. Compounds 5n, 5j, and 5o proved to exhibit the strongest and selective cytotoxic effect on HepG2 and MCF-7 lines. Taken together, this study has led to the development of promising leads for cancer therapy.
An efficient synthesis of a rationally designed 1,5 disubstituted imidazole AT1 Angiotensin II receptor antagonist: Reorientation of imidazole pharmacophore groups in losartan reserves high receptor affinity and confirms docking studies
Agelis, George,Roumelioti, Panagiota,Resvani, Amalia,Durdagi, Serdar,Androutsou, Maria-Eleni,Kelaidonis, Konstantinos,Vlahakos, Demetrios,Mavromoustakos, Thomas,Matsoukas, John
, p. 749 - 758 (2011/04/16)
A new 1,5 disubstituted imidazole AT1 Angiotensin II (AII) receptor antagonist related to losartan with reversion of butyl and hydroxymethyl groups at the 2-, 5-positions of the imidazole ring was synthesized and evaluated for its antagonist activity (V8). In vitro results indicated that the reorientation of butyl and hydroxymethyl groups on the imidazole template of losartan retained high binding affinity to the AT 1 receptor concluding that the spacing of the substituents at the 2,5- positions is of primary importance. The docking studies are confirmed by binding assay results which clearly show a comparable binding score of the designed compound V8 with that of the prototype losartan. An efficient, regioselective and cost effective synthesis renders the new compound as an attractive candidate for advanced toxicological evaluation and a drug against hypertension.
