Design, synthesis and biological activity of 6-substituted carbamoyl benzimidazoles as new nonpeptidic angiotensin II AT1 receptor antagonists

Homology modeling, binding site identification and docking study of human angiotensin II type I (Ang II-AT1) receptor

“…Ang II increases blood pressure by different mechanisms in these systems. In vascular smooth muscle it induces vasoconstriction, and in the adrenal cortex it acts on the zona glomerulosa and stimulates aldosterone biosynthesis and secretion; it also modulates fluid balance by affecting tubular sodium reabsorption, apart from constriction of both efferent arterioles and glomerular magnesium [5,6]. AT 1 receptor antagonism is an effective way to control pathogenesis of hypertension and heart failure.…”

Sulfonate-Grafted Metal–Organic Frameworks for Reductive Functionalization of CO2 to Benzimidazoles and N-Formamides

“…CO 2 has recently attracted growing concern as one of the greenhouse gases that is responsible for a series of environmental issues. Therefore, CO 2 transformation into high value-added chemicals has received extensive interest due to the renewable, abundant, economical, and nontoxic nature of CO 2 as the C1 resource. − Among various CO 2 -derived fine chemicals such as carbonate, formic acid, methanol, urea, carbamate, formamide, oxazolidinone, and benzimidazole, benzimidazole and its derivatives are pharmaceutically important N -containing heterocyclic compounds. − Benzimidazoles show an extensive range of pharmacological properties and biological activities with great significance in both industries and academia. − Traditionally, 1 H -benzo­[ d ]­imidazole ( 2a , R 1 = R 2 = H, Figure a) is prepared by condensation of 1,2-phenylenediamine ( 1a , R 1 = R 2 = H, Figure a) with carboxylic acid and its derivatives based on a Ladenburg ring closure method . However, a more environmentally friendly synthetic method for 2a via CO 2 functionalization with 1a is rarely reported due to the kinetic inertness and thermodynamic stability of CO 2 (Figure a).…”

Benzimidazole scaffolds as promising antiproliferative agents: a review

“…Especially, the benzimidazoles might be considered as auxiliary isosters of nucleotides having attached heterocyclic cores in their structures, cooperate effortlessly with biopolymers and have potential action for chemotherapeutic applications [6]. The benzimidazole moiety itself is an urgent pharmacophore in present day and has been used as privileged scaffolds to synthesize selective drugs of interest in numerous therapeutic areas including HIV-RT inhibitor [7], anticancer [8], antimicrobial [9], antihistamine [10], antihelmintic [11], antioxidant [12], antihypertensive [13], antiviral [14], anticoagulant [15] and antiulcer activity [16]. The marketed drugs having benzimidazole moiety (Fig.…”