Department of Pharmaceutical Science "Pietro Pratesi", Università degli Studi di Milano, Via Mangiagalli, 25-20133 Milano, Italy.
Expert Rev Clin Pharmacol. 2011 Jan;4(1):109-21. doi: 10.1586/ecp.10.122.
A new class of hydrogen sulfide (H(2)S)-donating hybrids combined with pharmacologically active compounds is presented in this article. The pharmacological profiles of some hybrid lead compounds in the areas of inflammation, H(2)S-donating diclofenac (ACS 15); cardiovascular, H(2)S-donating aspirin (ACS 14); urology, H(2)S-donating sildenafil (ACS 6); and neurodegenerative, H(2)S-donating latanoprost (ACS 67) for glaucoma treatment and H(2)S-donating levodopa (ACS 84) for Parkinson's disease, are described. The new H(2)S-releasing hybrids demonstrate remarkable improvement in activity and tolerability as compared with the related parent compounds, suggesting an active pharmacological role for H(2)S. Finally the mechanism(s) of action of glutathione-dependent and independent, and of gas (H(2)S) release (spontaneous or enzymatic) and its implications for clinical pharmacology perspectives will be also discussed.
本文介绍了一类新型的氢硫化物（H（2）S）供体型杂合化合物与具有药理活性的化合物相结合。一些杂种先导化合物在炎症、H（2）S 供体型双氯芬酸（ACS 15）；心血管、H（2）S 供体型阿司匹林（ACS 14）；泌尿科、H（2）S 供体型西地那非（ACS 6）和神经退行性疾病、H（2）S 供体型拉坦前列素（用于治疗青光眼的 ACS 67）和 H（2）S 供体型左旋多巴（用于治疗帕金森病的 ACS 84）的药理特征进行了描述。与相关母体化合物相比，新型 H（2）S 释放杂合化合物在活性和耐受性方面表现出显著改善，表明 H（2）S 具有积极的药理作用。最后还将讨论谷胱甘肽依赖和非依赖的作用机制、气体（H（2）S）释放（自发或酶促）及其对临床药理学的影响。
