Mathew Bijo, Suresh Jerad, Anbazhagan Sockalingam, Mathew Githa Elizabeth
Department of Pharmaceutical Chemistry Grace College of Pharmacy, Palakkad 678004, Kerala, India.
Cent Nerv Syst Agents Med Chem. 2013;13(3):195-206. doi: 10.2174/1871524914666140129122632.
In the five membered nitrogen containing heterocyclic family, pyrazoline could be recognized as a promising scaffold for the inhibition of Monoamine oxidase. Substitution at 1, 3 and 5-position of the pyrazoline nucleus displayed a significant activity towards MAO in the past 15 years. Our study identified the detailed structure activity relationship, the structural requirement for enzyme interaction and the effect of chirality on the pyrazoline nucleus towards MAO-A and MAO-B. We propose that the selectivity of pyrazoline nucleus towards MAO isoenzyme depends up on the bulkiness of the ring in the 1 and 3 position of the scaffold. The current review revealed that the derivatives of pyrazolines have proven to be versatile pharmacophores for the inhibition of MAO on the basis of existing literatures between (1998-2013).
在含氮五元杂环家族中，吡唑啉可被视为一种有前景的单胺氧化酶抑制骨架。在过去15年里，吡唑啉核1、3和5位的取代对单胺氧化酶表现出显著活性。我们的研究确定了详细的构效关系、酶相互作用的结构要求以及吡唑啉核对单胺氧化酶A和单胺氧化酶B的手性影响。我们提出，吡唑啉核对单胺氧化酶同工酶的选择性取决于骨架1和3位环的体积大小。当前综述表明，基于1998年至2013年间的现有文献，吡唑啉衍生物已被证明是抑制单胺氧化酶的通用药效基团。
