Enhanced water-soluble derivative of PC407 as a novel potential COX-2 inhibitor injectable formulation

Liu, Hongfei; Wan, Ning; Huan, Meng‐Lei; Jia, Yiyang; Yuan, Xiaofeng; Zhou, Siyuan; Zhang, Bang-Le

doi:10.1016/j.bmcl.2014.09.007

Cited by 3 publications

(2 citation statements)

References 17 publications

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“…The prodrug showed highly improved solubility, from 1.6 μg/mL to 20.3 mg/mL. Prodrug 84 showed analgesic activity in vivo and aqueous stability and is a promising candidate COX-2 inhibitor for injectable formulation [112].…”

Section: Other Chemical Prodrugsmentioning

confidence: 99%

The Prodrug Approach: A Successful Tool for Improving Drug Solubility

et al. 2015

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Prodrug design is a widely known molecular modification strategy that aims to optimize the physicochemical and pharmacological properties of drugs to improve their solubility and pharmacokinetic features and decrease their toxicity. A lack of solubility is one of the main obstacles to drug development. This review aims to describe recent advances in the improvement of solubility via the prodrug approach. The main chemical carriers and examples of successful strategies will be discussed, highlighting the advances of this field in the last ten years.

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Section: Other Chemical Prodrugsmentioning

confidence: 99%

The Prodrug Approach: A Successful Tool for Improving Drug Solubility

et al. 2015

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“…[15][16][17][18][19] Sulfonamides have a wide range of medical applications due to their anti-inflammatory, [15][16][17] antibacterial, [18][19][20][21] antimicrobial, [22][23][24] anticancer, [25][26][27][28][29][30][31] antimalarial, 32 and antipsychotic activities. 33 They have been reported to be inhibitors of DNA double-strand break repair, 34 dual angiotensin II and endothelin A receptor antagonists, 35 cyclooxygenase-2 inhibitors associated with different diseases, [36][37][38][39][40][41][42][43][44] inhibitors of caspase-3 and caspase-7, 45 and voltage gated sodium channel modulators. 46 The synthesis of functionalized sulfonamides including substituted sultams has been reviewed by Majumdar and Mondal in 2011 47 and Ashfaq et al in 2013.…”

Section: Application Of Sulfonamidesmentioning

confidence: 99%

Recent Functionalizations of Primary Sulfonamides

Chen

2016

Synthesis

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Sulfonamides are common building blocks in organic synthesis. They have a wide range of medical applications. This review aims to delineate recent efforts towards the functionalization of primary sulfonamides during last three years and to provide an overview of the synthesis of N-alkylated, N-acylated, and N-arylated sulfonamides from primary sulfonamides. Among other reactions, the sulfonamide-directed C-H functionalization is highlighted.

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