Abstract
A series of 4′-[(benzimidazole-1-yl)methyl]biphenyl-2-sulfonamide derivatives (Ia-Il) were synthesized and biologically evaluated. It was found that Ig, the most active compound, antagonized both Ang II AT1 and endothelin ETA receptors (AT1 IC50 = 8.5, ETA IC50 = 8.9 nM), and was more potent than losartan in RHRs with no significant effect on heart rate. The preliminary structure-activity relationships were also discussed in the present paper.
Original language | English |
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Pages (from-to) | 4661-4667 |
Number of pages | 7 |
Journal | Bioorganic and Medicinal Chemistry |
Volume | 20 |
Issue number | 15 |
DOIs | |
State | Published - Aug 1 2012 |
Bibliographical note
Funding Information:This study was financially supported by grant from ‘Eleventh Five-Year’ Major Innovation Projects for New Drug Candidates (No. 2009ZX09102-036), Jiangsu Provincial Science Fund (No. BK2008344) and Project for Research and Innovation of Graduates in Colleges and Universities of Jiangsu Province (CXZZ11-0798).
Funding
This study was financially supported by grant from ‘Eleventh Five-Year’ Major Innovation Projects for New Drug Candidates (No. 2009ZX09102-036), Jiangsu Provincial Science Fund (No. BK2008344) and Project for Research and Innovation of Graduates in Colleges and Universities of Jiangsu Province (CXZZ11-0798).
Funders | Funder number |
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Jiangsu Provincial Science Fund |
Keywords
- AT receptor
- Antihypertensive activity
- DARAs
- ET receptor
- Structure-activity relationships
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry