Synthesis and Antimicrobial Activities of Benzothiophene Derivatives

Aganagowda, Gadada; Thamyongkit, Patchanita; Petsom, Amorn

doi:10.4067/s0717-97072012000100019

Cited by 14 publications

(9 citation statements)

References 9 publications

(11 reference statements)

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“…In addition, chalcones serve as intermediates for the synthesis of corresponding pyrazolines by undergo a subsequent cyclization reaction with hydrazine hydrate, which are found to have extensive pharmaceutical applications. [51][52][53] So, N-(3-(2-hydroxyphenyl)acryloyl)phthalimide 1 was treated with hydrazine hydrate in ethanol to afford N-(5-(2-hydroxyphenyl)-4,5-dihydro-1H-pyrazol-3-yl)phthalimide (HPZPHT) 2 in 80 % yield.…”

Section: Resultsmentioning

confidence: 99%

Synthesis, radioiodination and biological evaluation of a novel phthalimide derivative

Motaleb

Abdel-Ghaney

Abdel‐Bary

et al. 2015

J Radioanal Nucl Chem

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Biologically active novel phthalimide derivative, N-(5-(2-hydroxyphenyl)-4,5-dihydro-1H-pyrazol-3-yl)phthalimide (HPZPHT), was synthesized in excellent yield and characterized by IR, mass and 1 H NMR spectroscopy. It was radiolabeled with iodine-131 by direct electrophilic substitution reaction and radiochemical yield was determined by using different chromatographic techniques (HPLRC, paper chromatography and paper electrophoresis). 131 I-HPZPHT has high radiolabeling yield (98.00 ± 2.00 %), stability, solid tumor uptake and T/NT ratio (5.17 ± 0.03 at 30 min. post-injection) compared with many new tracers which have been developed in recent years. This study encourages the possible use of this tracer as a potential imaging and/or therapeutic agent for cancer.

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Section: Resultsmentioning

confidence: 99%

Synthesis, radioiodination and biological evaluation of a novel phthalimide derivative

Motaleb

Abdel-Ghaney

Abdel‐Bary

et al. 2015

J Radioanal Nucl Chem

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“…Earlier classes of antibacterial compounds have been bisindoles with an indole scaffold and benzothiophenes with a benzothiophene scaffold for that low to moderate antimicrobial activities have been reported (Figure 1) [18,19]. We found novel antibacterial compound (sub)classes in a simple one-pot reaction with structurally varied substitution patterns within the molecular scaffold, and combined them with substituted indole residues at respective positions of the scaffold.…”

Section: Introductionmentioning

confidence: 89%

Section: Introductionmentioning

confidence: 99%

Novel Effective Fluorinated Benzothiophene-Indole Hybrid Antibacterials against S. aureus and MRSA Strains

Seethaler

Hertlein²,

Hopke³

et al. 2022

Pharmaceuticals

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Increasing antibacterial drug resistance threatens global health, unfortunately, however, efforts to find novel antibacterial agents have been scaled back by the pharmaceutical industry due to concerns about a poor return on investment. Nevertheless, there is an urgent need to find novel antibacterial compounds to combat antibacterial drug resistance. The synthesis of novel drugs from natural sources is mostly cost-intensive due to those drugs’ complicated structures. Therefore, it is necessary to find novel antibacterials by simple synthesis to become more attractive for industrial production. We succeeded in the discovery of four antibacterial compound (sub)classes accessible in a simple one-pot reaction based on fluorinated benzothiophene-indole hybrids. They have been evaluated against various S. aureus and MRSA strains. Structure- and substituent-dependent activities have been found within the (sub)classes and promising lead compounds have been identified. In addition, bacterial pyruvate kinase was found to be the molecular target of the active compounds. In conclusion, simple one-pot synthesis of benzothiophene-indoles represents a promising strategy for the search of novel antimicrobial compounds.

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“…The antimicrobial activity of benzofused thiophene, also known as benzothiophene, was investigated in vitro for the chalcone structures linked by an amide bond . Compounds 218 and 219 demonstrated moderate activity against bacterial strains and significant activity against fungal strains in this series (Figure ).…”

Section: Biological Activities Of Chalcone Derivativesmentioning

confidence: 99%

Synthesis of Chalcones Derivatives and Their Biological Activities: A Review

et al. 2022

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Chalcone derivatives are considered valuable species because they possess a ketoethylenic moiety, CO–CH=CH–. Due to the presence of a reactive α,β-unsaturated carbonyl group, chalcones and their derivatives possess a wide spectrum of antiproliferative, antifungal, antibacterial, antiviral, antileishmanial, and antimalarial pharmacological properties. Recent developments in heterocyclic chemistry have led to the synthesis of chalcone derivatives, which had been biologically investigated toward certain disease targets. The major aspect of this review is to present the most recent synthesis of chalcones bearing N, O, and/or S heterocycles, revealing their biological potential during the past decade (2010–2021). Based on a review of the literature, many chalcone–heterocycle hybrids appear to exhibit promise as future drug candidates owing to their similar or superior activities compared to those of the standards. Thus, this review may prove to be beneficial for the development and design of new potent therapeutic drugs based on previously developed strategies.

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Synthesis and Antimicrobial Activities of Benzothiophene Derivatives

Cited by 14 publications

References 9 publications

Synthesis, radioiodination and biological evaluation of a novel phthalimide derivative

Synthesis, radioiodination and biological evaluation of a novel phthalimide derivative

Novel Effective Fluorinated Benzothiophene-Indole Hybrid Antibacterials against S. aureus and MRSA Strains

Synthesis of Chalcones Derivatives and Their Biological Activities: A Review

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