Synthesis, Characterization and Biological Evaluation of Benzimidazole and Benzindazole Derivatives as Anti-hypertensive Agents | ||||
Egyptian Journal of Chemistry | ||||
Article 42, Volume 64, Issue 7, July 2021, Page 3659-3664 PDF (532.78 K) | ||||
Document Type: Original Article | ||||
DOI: 10.21608/ejchem.2021.79840.3931 | ||||
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Authors | ||||
Silky Sethy1; Sudip Kumar Mandal 2; Ewies Fawzy Ewies 3; Neerupma Dhiman 4; Arun Garg1 | ||||
1SMAS, KR Mangalam University, Gurugram, Haryana | ||||
2Dr. B. C. Roy College of Pharmacy and A.H.S., Durgapur-713206, West Bengal, India | ||||
3Organometallic and Organometalloid Chemistry, Chemical Industries Division, National Research Centre | ||||
4Amity Institute of Pharmacy, Amity University, Noida, Uttar Pradesh-201303, India | ||||
Abstract | ||||
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. | ||||
Keywords | ||||
Hypertension; Synthesis; Characterization; Non-peptide AT1 Receptor Antagonist; Renin-Angiotensin System | ||||
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