Department of Chemical Technology of Drugs, Medical University of Gdansk, Al. Gen. Hallera 107, Gdansk, Poland.
Expert Opin Ther Pat. 2009 Oct;19(10):1417-48. doi: 10.1517/13543770903216675.
The guanidine group defines chemical and physicochemical properties of many compounds of medical interest and guanidine-containing derivatives constitute a very important class of therapeutic agents suitable for the treatment of a wide spectrum of diseases.
To review the most important pharmacological properties, mechanisms of action and therapeutic uses of simple guanidine derivatives, cyclic analogues of guanidines as well as peptides, peptidomimetics and peptoids incorporating arginine.
The review presents both the recent patent literature and original papers dealing with guanidine derivatives that show interesting biological activity and emphasizes the newest developing drugs.
Recent achievements in the synthesis of guanidine-containing molecules with diverse chemical, biochemical and pharmacological properties make them of great importance to the design and development of novel drugs acting at CNS, anti-inflammatory agents, inhibitors of Na(+)/H(+) exchanger, inhibitors of NO synthase, antithrombotic, antidiabetic and chemotherapeutic agents as well as guanidinium-based transporters and vectors.
胍基定义了许多具有医学意义的化合物的化学和物理化学性质，胍基衍生物构成了一类非常重要的治疗剂，适用于治疗广泛的疾病。
综述简单胍基衍生物、胍类的环状类似物以及包含精氨酸的肽、拟肽和肽类的最重要的药理学特性、作用机制和治疗用途。
本综述既介绍了最近的专利文献，也介绍了具有有趣生物学活性的原始论文，并强调了最新的开发药物。
胍基化合物的合成方面的最新进展，具有多样化的化学、生化和药理学特性，使它们在设计和开发作用于中枢神经系统的新型药物、抗炎药物、Na(+)/H(+)交换抑制剂、一氧化氮合酶抑制剂、抗血栓、抗糖尿病和化学治疗药物以及胍基基转运蛋白和载体方面具有重要意义。
