Synthesis of new indole-2-carboxamide and 3-acetamide derivatives and evaluation their antioxidant properties

Ölgen, Süreyya; Bakar, F. Abu; Aydin, Sevim; Nebioğlu, Doğu; Nebioğlu, Serpil

doi:10.3109/14756366.2011.631183

Cited by 17 publications

(14 citation statements)

References 32 publications

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“…Therefore, special attention has also been given to acetamide medications because of their possible use as a therapeutic agent. Acetamide derivatives and their analogs representing a high potential of biological activities including anti-inflammatory [63], anti-oxidant [64], anti-cancer [65], anti-convulsant [66], anti-hypoxic and anti-microbial [67], antituberculosis agents [68] and anti-COVID-19 molecules [69]. In addition, several acetamide derivatives are used to improve some enzymes that inhibit HIV virus activity from replicating [70].…”

Section: An Overview Of Acetamide Derivatives As Possible Therapeutic Candidatesmentioning

confidence: 99%

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Recent investigations into synthesis and pharmacological activities of phenoxy acetamide and its derivatives (chalcone, indole and quinoline) as possible therapeutic candidates

2021

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Graphical abstract Medicinal chemistry can rightfully be regarded as a cornerstone in the public health of our modern society that combines chemistry and pharmacology with the aim of designing and developing new pharmaceutical compounds. For this purpose, many chemical techniques as well as new computational chemistry applications are used to study the utilization of drugs and their biological effects. In the biological interface, medicinal chemistry constitutes a group of interdisciplinary sciences, as well as controlling its organic, physical and computational pillars. Therefore, medicinal chemists working to design an integrated and developing system that portends an era of novel and safe tailored drugs either by synthesizing new pharmaceuticals or to improving the processes by which existing pharmaceuticals are made. It includes researching the effects of synthetic, semi-synthetic and natural biologically active substances based on molecular interactions in terms of molecular structure with triggered functional groups or the specific physicochemical properties. The present work focuses on the literature survey of chemical diversity of phenoxy acetamide and its derivatives (Chalcone, Indole and Quinoline) in the molecular framework in order to get complete information regarding pharmacologically interesting compounds of widely different composition. From a biological and industrial point of view, this literature review may provide an opportunity for the chemists to design new derivatives of phenoxy acetamide and its derivatives that proved to be the successful agent in view of safety and efficacy to enhance life quality.

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Section: An Overview Of Acetamide Derivatives As Possible Therapeutic Candidatesmentioning

confidence: 99%

“…Many chalcones also can be obtained via coupling reactions by using different reactants (63)(64)(65)(66)(67)(68)(69). Several reactions involved C-C and C-heteroatom covalent bond via oxidative addition transmetalation-reductive elimination, as illustrated in Scheme 12 [93].…”

Section: Introduction To Synthesis Of Chalcone and Its Derivativesmentioning

confidence: 99%

Recent investigations into synthesis and pharmacological activities of phenoxy acetamide and its derivatives (chalcone, indole and quinoline) as possible therapeutic candidates

2021

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“…The data obtained from the current investigation suggest that HTS08688 partially prevents the sudden decline in lenticular antioxidant enzyme activities that follow exposure of rat lenses to sodium selenite; this evasive effect was demonstrated morphologically by a decrease in the intensity of lenticular opacification. Recently, Ölgen et al demonstrated that acetamide derivatives exhibit antioxidant property; HTS08688 also possesses an acetamide moiety attached to its functional group. Hence, in the present study, maintenance of antioxidant defenses at near normal values in the HTS08688-treated group of rat lenses was possibly due to the presence of this acetamide group.…”

Section: Experimental Validationmentioning

confidence: 99%

Structure-Based Virtual Screening and Biological Evaluation of a Calpain Inhibitor for Prevention of Selenite-Induced Cataractogenesis in an in Vitro System

Muralidharan

Selvaraj

Sheu

et al. 2015

J. Chem. Inf. Model.

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Calpains belong to the family of calcium-dependent, structurally related intracellular cysteine proteases that exhibit significant functions in evolution of different types of cataracts in human as well as animal models. Application of calpain inhibitors generated through a virtual screening workflow may provide new avenues for the prevention of cataractogenesis. Hence, in the current study, compounds were first screened for potent calpain inhibitory activity by employing a structure-based approach, and the screening results were then validated through biological experiments in rat lenses. A hit compound, HTS08688, was obtained by structure-based virtual screening. A micromolar concentration of HTS08688 was found to prevent in vitro cataractogenesis in isolated Wistar rat lenses, while maintaining the antioxidant and calcium concentrations at near normal levels. Inhibition of superoxide anion generation, as observed through cytochemical localization studies, and maintenance of structural integrity, as demonstrated by histological analysis of lenticular tissue, also suggested that HTS08688 can ameliorate the cataractous condition induced by selenite in an in vitro rodent model. A cell proliferation assay was performed; the IC 50 value of the screened calpain inhibitor, HTS08688, against human lenticular epithelial cells-b3 was found to be 177 μM/mL. This combined theoretical and experimental approach has demonstrated a potent lead compound, HTS08688, that exhibits putative anticataractogenic activity by virtue of its potential to inhibit calpain.

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“…Quinoxaline and its moieties are an crucial class of nitrogen-containing heterocycle in medicinal chemistry [1], possess a wide [2,3] and diverse spectrum of pharmacological properties [4,5], such as antibiotic [6], anti-viral [7], anti-cancer [8], and antiin lammatory activities [1,9]. The quinoxaline core moiety is also associated with multiple applications in semiconductors [2,10], dyes [3], cavitands and dehydroannulenes [11].…”

Section: Introductionmentioning

confidence: 99%

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Injeti¹

2022

Fut J. Pharm & H. Sci

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Synthesis of new indole-2-carboxamide and 3-acetamide derivatives and evaluation their antioxidant properties

Cited by 17 publications

References 32 publications

Recent investigations into synthesis and pharmacological activities of phenoxy acetamide and its derivatives (chalcone, indole and quinoline) as possible therapeutic candidates

Recent investigations into synthesis and pharmacological activities of phenoxy acetamide and its derivatives (chalcone, indole and quinoline) as possible therapeutic candidates

Structure-Based Virtual Screening and Biological Evaluation of a Calpain Inhibitor for Prevention of Selenite-Induced Cataractogenesis in an in Vitro System

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