Prodrugs of nonsteroidal anti-inflammatory drugs (NSAIDs), more than meets the eye: a critical review.
Prodrugs of nonsteroidal anti-inflammatory drugs (NSAIDs), more than meets the eye: a critical review.
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DOI：
10.3390/ijms131217244
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发表时间：
2012-12-17
影响因子：
5.6
通讯作者：
Qandil AM
中科院分区：
文献类型：
--
作者：
Qandil AM
非甾体抗炎药前体药物的设计和合成一直受到药物化学家的关注，特别是在过去的十年中。作为一个治疗组，NSAID是最广泛使用的处方药和非处方药（OTC）。关于潜在的NSAID前药的丰富文献清楚地显示了从具有掩蔽羧酸基团的唯一作用的烷基酯、芳烷基酯或芳基酯到含有精心选择的基团以用于特定目的的更精细的缀合物的转变，所述特定目的例如增强水溶性和溶解、一氧化氮释放、硫化氢释放、抗氧化活性、抗胆碱能和乙酰胆碱酯酶抑制（AChEI）活性以及位点特异性靶向和递送。这篇评论将集中在NSAID前药，已被设计或后来被发现，具有内在的药理活性作为一个完整的化学实体。这种内在活性可能增强NSAID的抗炎活性，减少其副作用或将潜在的治疗用途从经典抗炎作用转变为其他作用。本综述中讨论的报告将包括NO-NSAID、抗胆碱能和AChEI-NSAID、磷酸化NSAID和一些杂项药物。在大多数情况下，本综述将涵盖2006年及以后与这些NSAID前药有关的文献。必要时将使用旧文献，例如，来解释其化学和生物学作用机制。
The design and the synthesis of prodrugs for nonsteroidal anti-inflammatory drugs (NSAIDs) have been given much attention by medicinal chemists, especially in the last decade. As a therapeutic group, NSAIDs are among the most widely used prescribed and over the counter (OTC) medications. The rich literature about potential NSAID prodrugs clearly shows a shift from alkyl, aryalkyl or aryl esters with the sole role of masking the carboxylic acid group, to more elaborate conjugates that contain carefully chosen groups to serve specific purposes, such as enhancement of water solubility and dissolution, nitric oxide release, hydrogen sulfide release, antioxidant activity, anticholinergic and acetylcholinesterase inhibitory (AChEI) activity and site-specific targeting and delivery. This review will focus on NSAID prodrugs that have been designed or were, later, found to possess intrinsic pharmacological activity as an intact chemical entity. Such intrinsic activity might augment the anti-inflammatory activity of the NSAID, reduce its side effects or transform the potential therapeutic use from classical anti-inflammatory action to something else. Reports discussed in this review will be those of NO-NSAIDs, anticholinergic and AChEI-NSAIDs, Phospho-NSAIDs and some miscellaneous agents. In most cases, this review will cover literature dealing with these NSAID prodrugs from the year 2006 and later. Older literature will be used when necessary, e.g., to explain the chemical and biological mechanisms of action.
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影响因子：
7.2
作者：
Fabbri, F;Brigliadori, G;Zoli, W
通讯作者：
Zoli, W
DOI：
10.1016/j.bbrc.2005.06.149
发表时间：
2005-08-26
影响因子：
3.1
作者：
Downing, JEG;Madden, JC;Rostron, C
通讯作者：
Rostron, C
影响因子：
5.9
作者：
DUGGAN, DE
通讯作者：
DUGGAN, DE
DOI：
10.1016/j.bbrc.2012.02.051
发表时间：
2012-03-16
影响因子：
3.1
作者：
Chattopadhyay, Mitali;Kodela, Ravinder;Kashfi, Khosrow
通讯作者：
Kashfi, Khosrow
影响因子：
7.3
作者：
Biava, Mariangela;Porretta, Giulio Cesare;Anzini, Maurizio
通讯作者：
Anzini, Maurizio