Design, synthesis and anti-inflammatory activity of diterpenoid alkaloids and non-steroidal anti-inflammatory drug hybrids based on molecular hybridization strategy

Guo, Minghao; Wen, Peng; Xiao, Yao; Ji, Wan-Sheng; Zhou, Xian‐Li; Gao, Feng; Shan, Lianhai

doi:10.1016/j.fitote.2023.105536

Cited by 6 publications

(2 citation statements)

References 21 publications

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“…Molecular hybridization is widely used in pharmaceutical chemistry, involving the combination of two drug molecules or their pharmacodynamic groups into a single entity. 21 This strategy leads to produce new chemicals with combined features of the original medications that demonstrate synergistic therapy benefits or reduce adverse effects. 22 The non-steroidal anti-inflammatory medicine benorylate is a notable example of a hybrid molecule, produced by combining the carboxyl group of aspirin with the phenolic hydroxyl group of acetaminophen.…”

Section: Introductionmentioning

confidence: 99%

Design, synthesis, and anti-inflammatory activity of indole-2-formamide benzimidazole[2,1-b]thiazole derivatives

Lin,

Jiang,

Chen

et al. 2024

RSC Adv.

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Section: Introductionmentioning

confidence: 99%

Design, synthesis, and anti-inflammatory activity of indole-2-formamide benzimidazole[2,1-b]thiazole derivatives

Lin,

Jiang,

Chen

et al. 2024

RSC Adv.

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“…While many studies on lappaconitine derivatives have been reported, most research to date has focused on minor substituent modifications, such as acylation or alkylation of hydroxyl and amino groups, without significant improvements in biological activities (Figure ). ,− In contrast, our work focuses on substantial structural alterations to the core of LA ( 1 ), with the goal of discovering novel derivatives with improved biological properties. We aimed to rearrange the carbon framework of LA ( 1 ), inspired by the presence of its vicinal diol at the C-8 and C-9 positions, hoping to identify alternative lappaconitine derivatives with improved biological properties and reduced toxicities (Figure ).…”

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confidence: 99%

Structural Modification and Characteristics of Lappaconitine Alkaloid for the Discovery of Bioactive Components by Hypervalent Iodine Reagent

Moon,

Kang,

Nam

et al. 2024

Org. Lett.

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Lappaconitine, a diterpene alkaloid isolated from Aconitum sinomontanum Nakai, exhibits a wide range of biological activities, making it a promising candidate for the development of novel derivatives with therapeutic potential. In our research, we executed a two-step transformation via oxidative cleavage of lappaconitine's vicinal diol using the hypervalent iodine reagent PhI(OAc) 2 , followed by strong alkaline hydrolysis. This approach yielded four new unanticipated compounds, whose structures were identified by spectroscopic methods and/or X-ray crystallography. Thus, we proposed plausible reaction mechanisms for their formations and particularly investigated the remarkable diastereoselectivity for the formation of single stereoisomer 8 observed during the alkaline hydrolysis step. Among them, compound 8 (code name: QG3030) demonstrated both enhanced osteogenic differentiation of human mesenchymal stem cells and significant osteogenic effect in an ovariectomized rat model with no acute oral toxicity.

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Isoniazid Hybrids As Potential Antitubercular Agents

Mishra,

Kumar,

Singh

2024

ChemistrySelect

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The rapid emergence of various forms of drug‐resistant tuberculosis (TB) has massively impacted people's health globally. According to the WHO, TB care and facilities have been downgraded by 21% since the COVID‐19 pandemic, which has further slowed down the progress toward the “End TB Strategy.” Multiple studies have shown drug‐resistant tuberculosis to be resilient to front‐line antituberculosis drugs, including isoniazid (INH), thus constantly prompting researchers worldwide to probe new potent chemical entities to replace/supplement the current artillery of anti‐TB therapeutics. The molecular hybridization (MH) technique has recently been adopted by many synthetic and medicinal chemists to combine different pharmacophoric units into a single molecular architecture which in most cases has been reported to exhibit a better pharmacological profile as compared to its precursors. The present review provides a concise account of the MH hybridization strategies directed at the structural manipulations of isoniazid to develop new anti‐TB agents and their structure‐activity relationships. Furthermore, their toxicity profiles and docking studies with relevant receptors are also briefly discussed.

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Design, synthesis and anti-inflammatory activity of diterpenoid alkaloids and non-steroidal anti-inflammatory drug hybrids based on molecular hybridization strategy

Cited by 6 publications

References 21 publications

Design, synthesis, and anti-inflammatory activity of indole-2-formamide benzimidazole[2,1-b]thiazole derivatives

Design, synthesis, and anti-inflammatory activity of indole-2-formamide benzimidazole[2,1-b]thiazole derivatives

Structural Modification and Characteristics of Lappaconitine Alkaloid for the Discovery of Bioactive Components by Hypervalent Iodine Reagent

Isoniazid Hybrids As Potential Antitubercular Agents

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