Synthesis, crystal structure, DFT and anticancer study of dihydroartermisinin-paracetamol hybrids

Liu, Tao; Ai, Yi; Ding, Jie; Li, Bingqing; Zeng, Changguang; Zhang, Xiaohan; Zhong, Hang; Zhou, Zhixu

doi:10.1016/j.molstruc.2021.131758

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Cited by 4 publications

(1 citation statement)

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“…Moreover, novel designs of APA hybrids can raise perspective and make compounds easy to prepare with antioxidant, antimicrobial, antibacterial, and antitumor properties. 163,164 A suitable combination of the APAP core with scaffolds from natural products like artemisinin or its derivatives (APAP–dihydroartemisinin molecule, an O-modified APAP prodrug) 165 can also allow refilling the arsenal of needed drugs.…”

Section: Discussionmentioning

confidence: 99%

Exploring acetaminophen prodrugs and hybrids: a review

Kouznetsov

2024

RSC Adv.

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Section: Discussionmentioning

confidence: 99%

Exploring acetaminophen prodrugs and hybrids: a review

Kouznetsov

2024

RSC Adv.

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Discovery of new anti-diabetic potential agents based on paracetamol incorporating sulfa-drugs: Design, synthesis, α-amylase, and α-glucosidase inhibitors with molecular docking simulation

Khamees Thabet,

Ragab,

Imran

et al. 2024

European Journal of Medicinal Chemistry

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A Short Review on Biological Activities of Paracetamol Derivatives

Begum¹,

G²,

S³

2023

PCI- Approved-IJPSN

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Paracetamol reduces body temperature with multiple mechanisms. Paracetamol is chemically 4-hydroxy acetanilide and has a good safety profile. Following its successful use as an over-the-counter antipyretic and analgesic medication, several attempts were made to increase the potency, mask the bitter taste, and decrease the toxicity of this drug by modifications at the phenyl ring, acetamido group, and hydroxyl group. The free hydroxyl group of paracetamols was masked to obtain prodrugs (carbonate prodrugs, ester prodrugs like alanine-prodrug, proline-prodrug, galactosylated prodrug, and mutual prodrugs with other drugs and NSAIDs). Propacetamol is a commercially available prodrug derived from paracetamol that is effective in parenteral form. Paracetamol ester prodrugs with sulfur-containing amino acids such as N-acetyl cysteine, cysteine, and methionine showed low hepatotoxicity compared to the parent drug. In addition, paracetamol derivatives including metal complexes, chalcones, Mannich bases, nucleoside analogs, hybrids with the aryl-imidazolidinyl ring, thymol, and triazole ring displayed diverse activities like antioxidant, anticancer, and antimicrobial activities.

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Synthesis, crystal structure, DFT and anticancer study of dihydroartermisinin-paracetamol hybrids

Cited by 4 publications

References 25 publications

Exploring acetaminophen prodrugs and hybrids: a review

Exploring acetaminophen prodrugs and hybrids: a review

Discovery of new anti-diabetic potential agents based on paracetamol incorporating sulfa-drugs: Design, synthesis, α-amylase, and α-glucosidase inhibitors with molecular docking simulation

A Short Review on Biological Activities of Paracetamol Derivatives

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