Title : Non-peptide angiotensin II receptor antagonists. 1. Design, synthesis, and biological activity of N-substituted indoles and dihydroindoles.

Pub. Date : 1993 Dec 24

PMID : 8277505






4 Functional Relationships(s)
Download
Sentence
Compound Name
Protein Name
Organism
1 Replacement of the terminal carboxyl (COOH) of 14a with the bioisostere tetrazole in 16 (AT1 IC50 = 5 nM, AT2 IC50 = 130 nM) not only improved the AT1 potency by 4-fold but also resulted in a 50-fold increase in AT2 activity. 1H-tetrazole angiotensin II receptor, type 1a Rattus norvegicus
2 Replacement of the terminal carboxyl (COOH) of 14a with the bioisostere tetrazole in 16 (AT1 IC50 = 5 nM, AT2 IC50 = 130 nM) not only improved the AT1 potency by 4-fold but also resulted in a 50-fold increase in AT2 activity. 1H-tetrazole angiotensin II receptor, type 1a Rattus norvegicus
3 Tetrazole 34 was identified as the most potent (AT1 IC50 = 18 nM) AT1 receptor antagonist in a structurally distinct series of compounds derived from N-alkylation of dihydroindole 25. 1H-tetrazole angiotensin II receptor, type 1a Rattus norvegicus
4 Tetrazole 34 was identified as the most potent (AT1 IC50 = 18 nM) AT1 receptor antagonist in a structurally distinct series of compounds derived from N-alkylation of dihydroindole 25. 1H-tetrazole angiotensin II receptor, type 1a Rattus norvegicus