Universidade Federal do Rio de Janeiro, Instituto de Ciências Biomédicas, Laboratório de Avaliação e Síntese de Substâncias Bioativas (LASSBio) , Rio de Janeiro, RJ, P.O. Box 68023, ZIP 21941-902 , Brazil
Expert Opin Ther Pat. 2014 Nov;24(11):1161-70. doi: 10.1517/13543776.2014.959491. Epub 2014 Sep 12.
The N-acylhydrazone (NAH) moiety has been characterized as a privileged structure, capable of providing ligands points for more than one type of bioreceptor. Modifications of the subunits bonded to its acyl and imine functions resulted in several derivatives, which modulate a great diversity of molecular targets. In this context, this patent review reflects the use of the NAH moiety in different compounds.
In this review, the authors perform an analysis of the therapeutic profile of NAH compounds together with their perspective of its usability. The Espacenet and Delphion databases were used as main sources of search, and 'N-acylhydrazone,', 'Acylhydrazone' and 'hydrazone' were used as keywords. From a total of 117 patents retrieved, 22 presented pharmacological activities described in the document, thus being chosen for this review.
In the last century, only six patents disclosing NAH derivatives for therapeutic purposes were published, and only in 2010, this subunit started receiving some real attention regarding its therapeutic potential. In this review, the Brazilian and Chinese Universities were identified as the major patent applicants, especially for drug candidates for the treatment of chronic pain, inflammatory disorders and cancer. The NAH subunit is very versatile both from synthetic and medicinal chemistry point of view. This feature is a direct result from the conformational diversity that this framework presents, achievable by subtle and simple chemical changes. Therefore, our opinion is that this moiety suits a lot more drug discovery projects than it seems to at first glance. In conclusion, we strongly support and encourage a raise in the use of this unique subunit.
N-酰腙（NAH）部分被认为是一种特权结构，能够为不止一种类型的生物受体提供配体结合点。对与其酰基和亚胺功能键合的亚基进行修饰，得到了几种能够调节多种分子靶标的衍生物。在这种情况下，本专利综述反映了 NAH 部分在不同化合物中的应用。
在这篇综述中，作者分析了 NAH 化合物的治疗概况及其可用性的前景。Espacenet 和 Delphion 数据库被用作主要的搜索源，“N-酰腙”、“酰腙”和“腙”被用作关键词。在总共检索到的 117 项专利中，有 22 项提出了文件中描述的药理学活性，因此被选为本文的综述。
在上个世纪，只有六份专利披露了具有治疗用途的 NAH 衍生物，直到 2010 年，这个部分才开始因其治疗潜力而受到关注。在这篇综述中，巴西和中国的大学被确定为主要的专利申请人，特别是针对治疗慢性疼痛、炎症性疾病和癌症的药物候选物。从合成和药物化学的角度来看，NAH 部分非常多样化。这种特点是该结构所具有的构象多样性的直接结果，通过细微而简单的化学变化即可实现。因此，我们认为这个部分适合更多的药物发现项目，而不仅仅是乍一看那么多。总之，我们强烈支持和鼓励更多地使用这种独特的部分。
