N-Phenyl indole derivatives as AT1 antagonists with anti-hypertension activities: Design, synthesis and biological evaluation

Recent Progress Concerning the N-Arylation of Indoles

“…The acute toxicity of compound F5-2b was determined by LD 50 as 1551.71 mg/kg. Other indole derivatives have been prepared by the same group and studied as angiotensin II receptor 1 antagonists [ 167 , 168 , 169 , 170 ]. The examples given in Figure 5 show that a common feature of these compounds is the presence of an ortho -substituted phenyl ring with a carboxylic acid F5-3 [ 167 , 168 , 170 ] or 1,2,4-oxadiazole F5-4 [ 169 ] scaffold at position 1 of the indole unit.…”

“…Other indole derivatives have been prepared by the same group and studied as angiotensin II receptor 1 antagonists [ 167 , 168 , 169 , 170 ]. The examples given in Figure 5 show that a common feature of these compounds is the presence of an ortho -substituted phenyl ring with a carboxylic acid F5-3 [ 167 , 168 , 170 ] or 1,2,4-oxadiazole F5-4 [ 169 ] scaffold at position 1 of the indole unit. Similarly, the introduction of phenyl substituents was accomplished via nucleophilic aromatic substitution in refluxing DMF.…”

Synthesis of Antimicrobial Benzimidazole–Pyrazole Compounds and Their Biological Activities

“…Among the heterocyclic compounds known in the literature for their antimicrobial activities are those with benzimidazole ring and those with pyrazole ring, aromatic compounds with a very wide range of medicinal properties. Benzimidazole derivatives developed a considerable interest in medical domain due to their therapeutic action as antitumor [ 4 , 5 , 6 , 7 ], antimicrobial [ 8 , 9 , 10 , 11 , 12 , 13 , 14 ], antihelmintic [ 15 ], antihistaminic [ 16 , 17 ], proton pump inhibitors [ 16 , 18 ], anti-inflammatory [ 19 , 20 ] and anti-hypertensive [ 21 ] drugs. Astemizole-related compounds demonstrated anti-prion activity for the treatment of Creutzfeldt–Jakob disease, while albendazole compounds are currently used as medication for the treatment of a variety of parasitic worm infestations.…”

Synthesis of benzimidazole based hydrazones as non‐sugar based α‐glucosidase inhibitors: Structure activity relation and molecular docking

“…In drug discovery process (Yoon et al, 2014), the imidazole and benzimidazole nucleus, respectively, are key pharmacophores, as they are frequently confronted in those drugs that depict a variety of pharmacological activities including antiulcer (Torres et al, 2015), antihypertensive (Zhu et al, 2016), antiviral (Pan et al, 2015), antifungal (Patel et al, 2012), anticancer (Akhtar et al, 2017), anthelmintic (Mavrova et al, 2006), antibacterial (Patel et al, 2012), cytotoxicity (Akhtar et al, 2017), antimicrobial (Patel et al, 2012), anti‐inflammatory (Gaba et al, 2014), antitumor (Wu et al, 2016), histamine‐H3 antagonist (Venable et al, 2005), antioxidant (Sam Daniel Prabu et al, 2019), gastro protective (Loriga et al, 1992), DNA binding (Zhang et al, 2016 ) , and Alzheimer disease (Gulcan et al, 2019). In these days, one of the most well‐known yet critical metabolic disorder is diabetes mellitus (DM) affecting more than 400 million people (Khursheed et al, 2019), distinguished by inflated blood‐glucose levels along with variations in carbohydrate, lipid and protein metabolism (Shobana et al, 2009).…”