Synthesis, spectral linearity, antimicrobial, antioxidant and insect antifeedant activities of some 2,5-dimethyl-3-thienyl chalcones

Vanangamudi, Ganesan; Subramanian, M.; Thirunarayanan, Ganesamoorthy

doi:10.1016/j.arabjc.2013.03.006

Cited by 23 publications

(20 citation statements)

References 26 publications

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“…Chalconas e seus derivados são substâncias de grande interesse químico-farmacológico e tem recebido uma grande atenção devido, sobretudo, a sua estrutura relativamente simples e a diversidade de atividades farmacológicas que apresentam, dentre as quais podemos citar: atividade antioxidante, 3 antinociceptiva, 4 anticonvulsivante, 5 e antiinflamatória. 6 Os derivados 1,3-diaril-2-propen-1-onas obtidos através de plantas ou síntese orgânica têm sido amplamente explorados.…”

Section: Figura 1 Estrutura Básica Das Chalconasunclassified

“…Todos os compostos foram testados quanto à sua atividade anticonvulsivante utilizando testes de convulsão induzida por PTZ e MES em camundongos a uma dose de 50 mg kg -1 via intraperitoneal. Os resultados da atividade anticonvulsivante demonstraram que entre os compostos testados, os derivados de 2pirazolina-1-carboxamida que transportam 5-Bromotiofen-2-il (22) e o 5-Clorotiofen-2-il (23) (Figura 14) exibiram promissora atividade no teste PTZ, uma vez que reduziram a frequência de convulsão em todos os graus (1)(2)(3)(4)(5). Assim, pode-se concluir que os referidos compostos aumentaram o limite convulsivo e prolongaram o tempo de início de 1,20 a 2,10 e 1,20 a 3,58 segundos, assim como aumentaram a taxa de sobrevivência quase duas vezes de 50 % a 95 % e 50 % a 100 %, respectivamente.…”

Section: Atividade Anticonvulsivanteunclassified

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Chalcones Pharmacological Potential: A Brief Review

et al. 2018

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Chalcones are naturally occurring aromatic ketones, consisting of an α, β-unsaturated carbonyl system linking two aromatic rings. It is a class of open chain flavonoids, abundantly found in plants of the families Leguminosae, Compositae and Moraceae, and present in fruits, vegetables, grains, roots, flowers, teas, wines, products regularly used for human consumption. Research that investigates the properties of chalcones has shown a broad spectrum of biological activity, which has been reinforcing since the isolation, synthesis, identification and investigation of biological effects. This study was carried out based on the scientific articles published on chalcones, emphasizing the following pharmacological activities: antioxidant, antinociceptive, anti-inflammatory, anxiolytic and anticonvulsant compared to the period of the last 10 years. It was verified that the reported activities prove that chalcones and their derivatives are substances of great chemical-pharmacological interest.

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Section: Figura 1 Estrutura Básica Das Chalconasunclassified

Section: Atividade Anticonvulsivanteunclassified

Chalcones Pharmacological Potential: A Brief Review

et al. 2018

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“…. Nowadays several chalcones are used to treat the inflammatory conditions 6,7 , cancer 8 viral infections 9,10 , cardiovascular diseases, parasitic infections, gastritis, microbial infections 11,12 and convulsions 13 . In addition, they are also used as food additives and cosmetic formulation ingredients.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Antibacterial, Antifungal Antitubercular Activities and Molecular Docking Studies of Nitrophenyl Derivatives

BABU

Prasad

Nissankararao³

et al. 2019

Int J Life Sci Pharm Res

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Infectious diseases are one of the common problems encountered globally. Even though there are a number of drugs available in the market for the treatment of infectious diseases, still many new molecules are required due to the problems with the existing drugs. Hence we prepared a series of chalcones (A1-A10) containing nitrophenyl moieties by Claisen-Schmidt condensation reaction. All the ten compounds were characterized by IR, NMR, Mass spectroscopy and elemental analysis. The compounds were further screened for antitubercular activity employing MABA assay and antibacterial and antifungal activities by cup plate method against selected tubercular, bacterial and fungal organisms. The compound A9 displayed potent antitubercular activity with MIC 11.02±0.030, whereas the compound A3 showed superior antibacterial and antifungal activities. Further, molecular docking studies were performed on Thymidine Kinase (TMP) of Mycobacterium tuberculosis by employing AU autodocker. The docking scores were in association with the in vitro MABA results and also identified the potent nature of A9 with the docking score-6.7. This study helped to identify novel nitrophenyl derivatives against thymidylate kinase.

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“…Pyrazoline rings can be obtained by a cyclocondensation reaction of α,β-unsaturated ketones (chalcones) with hydrazine derivatives. Their synthetic precursors (i.e., chalcones) have also shown marked biological activity as anticancer [ 27 , 28 ], antiviral [ 29 ], antimalarial [ 30 ] and antioxidant agents [ 31 ].…”

Section: Introductionmentioning

confidence: 99%

Synthesis of New 1,3,5-Triazine-Based 2-Pyrazolines as Potential Anticancer Agents

et al. 2018

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A new series of 1,3,5-triazine-containing 2-pyrazoline derivatives (8–11)a–g was synthesized by cyclocondensation reactions of [(4,6-bis((2-hydroxyethyl)amino)-1,3,5-triazin-2-yl)amine]chalcones 7a–g with hydrazine hydrate and derivatives. Chalcones 7a–g were obtained by Claisen-Schmidt condensation between aromatic aldehydes and triazinic derivative 5, which was synthesized in high yield by a microwave-assisted reaction. Seventeen of the synthesized compounds were selected and tested by the US National Cancer Institute (NCI) for their anticancer activity against 58 different human tumor cell lines. Compounds 7g and 10d,e,g showed important GI50 values ranging from 0.569 to 16.6 µM and LC50 values ranging from 5.15 to >100 µM.

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Synthesis, spectral linearity, antimicrobial, antioxidant and insect antifeedant activities of some 2,5-dimethyl-3-thienyl chalcones

Cited by 23 publications

References 26 publications

Chalcones Pharmacological Potential: A Brief Review

Chalcones Pharmacological Potential: A Brief Review

Synthesis, Antibacterial, Antifungal Antitubercular Activities and Molecular Docking Studies of Nitrophenyl Derivatives

Synthesis of New 1,3,5-Triazine-Based 2-Pyrazolines as Potential Anticancer Agents

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