Synthesis of A575C, a combined angiotensin converting enzyme inhibitor-beta adrenoceptor antagonist

Hardy, G.; Bull, Donald; Mills, G.; Allan, Geoffrey

doi:10.1016/s0040-4039(00)80213-0

Cited by 11 publications

(1 citation statement)

References 6 publications

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“…The Hemetsberger reaction was chosen as the synthetic preparation method for the designated indole compounds since it readily forms derivatives of 2-carboxyindoles from aromatic or heterocyclic aldehydes. [30][31][32] The position 2 was chosen as the first location on the indole ring for the preparation of the first set of compounds. 4,6-Dimethoxyindole-2-carbaldehyde 33 was prepared by reduction and oxidation of methyl 4,6-dimeth oxyindole-2-carboxylate, respectively.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and characterisation of novel 4,6-dimethoxyindole-7- and -2-thiosemicarbazone derivatives: Biological evaluation as antioxidant and anticholinesterase candidates

Bingül

2019

Journal of Chemical Research

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Two sets of novel indole-based thiosemicarbazone systems 8a–d and 9a–d are prepared by the Schiff base condensation reaction of indole carbaldehydes 4 and 6 with a range of thiosemicarbazides 7a–d in high yields and purity. The antioxidant properties of the synthesised compounds 8a–d and 9a–d are determined by employing three different assays, namely 2,2-diphenyl-1-picrylhydrazyl hydrate–free radical scavenging, ABTS [2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)] cationic radical decolarization and cupric ion reducing antioxidant capacity. The anticholinesterase properties of the products are investigated by acetylcholinesterase and butyrylcholinesterase enzyme inhibition assays. The methyl-substituted compounds 8b and 9b display the highest inhibition for the ABTS assay and absorbance values for the cupric ion reducing antioxidant capacity assay, while compound 9c shows the best activity for 2,2-diphenyl-1-picrylhydrazyl hydrate assay. Moderate inhibition of acetylcholinesterase and butyrylcholinesterase is determined in the case of compound 8b.

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Section: Introductionmentioning

confidence: 99%

Synthesis and characterisation of novel 4,6-dimethoxyindole-7- and -2-thiosemicarbazone derivatives: Biological evaluation as antioxidant and anticholinesterase candidates

Bingül

2019

Journal of Chemical Research

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Cyclization of Vinyl and Aryl Azides into Pyrroles, Indoles, Carbazoles, and Related Fused Pyrroles

Berkowitz

McCombie

2017

Organic Reactions

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This chapter reviews in detail those reactions that form of a new pyrrole ring from vinyl, aryl, and heteroaryl azides via formal C–H insertion processes under thermal, photochemical, and metal‐catalyzed conditions. These reactions proceed via the intermediacy of vinyl or aryl nitrenes (or their metallonitrene equivalents) and generate a wide variety of pyrroles, indoles, carbazoles, and related systems. Methods for the synthesis of the starting azides are summarized, and a comprehensive survey of the cyclization processes is provided.

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Synthesis and Reactivity of 1,4-Oxazinoindole Derivatives

et al. 2002

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Synthesis of A575C, a combined angiotensin converting enzyme inhibitor-beta adrenoceptor antagonist

Cited by 11 publications

References 6 publications

Synthesis and characterisation of novel 4,6-dimethoxyindole-7- and -2-thiosemicarbazone derivatives: Biological evaluation as antioxidant and anticholinesterase candidates

Synthesis and characterisation of novel 4,6-dimethoxyindole-7- and -2-thiosemicarbazone derivatives: Biological evaluation as antioxidant and anticholinesterase candidates

Cyclization of Vinyl and Aryl Azides into Pyrroles, Indoles, Carbazoles, and Related Fused Pyrroles

Synthesis and Reactivity of 1,4-Oxazinoindole Derivatives

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