Crop Protection Chemicals Division, CSIR-Indian Institute of Chemical Technology, Hyderabad, 500 007, India.
Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad, 500 007, India.
Eur J Med Chem. 2014 Aug 18;83:344-54. doi: 10.1016/j.ejmech.2014.06.035. Epub 2014 Jun 17.
A series of novel 2-(diarylalkyl)aminobenzothiazoles were designed based on commercial synthetic calcium channel blockers (CCBs) and angiotensin converting enzyme (ACE) inhibitors. Which are further modified based on the natural products which are angiotensin converting enzyme (ACE) inhibitors. Completely green protocol was developed for their synthesis. As they are initially designed based on CCBs, they were screened for their ACE inhibition property believing that almost all the compounds will be CCBs. Out of 42 compounds two lead molecules were identified as ACE inhibitors, which were further screened for CCB. As expected both were identified as CCBs with different selectivity over ACE inhibition. Their selectivity over ACE and CCB can be used to treat resistant hypertension.
基于商业合成钙通道阻滞剂 (CCB) 和血管紧张素转化酶 (ACE) 抑制剂,设计了一系列新型 2-(二芳基烷基)氨基苯并噻唑。这些抑制剂进一步基于血管紧张素转化酶 (ACE) 抑制剂的天然产物进行了修饰。为它们的合成开发了完全绿色的方案。由于它们最初是基于 CCB 设计的,因此根据它们具有 ACE 抑制特性对它们进行了筛选,认为几乎所有化合物都将是 CCB。在 42 种化合物中,确定了两种先导分子作为 ACE 抑制剂,然后对它们进行 CCB 筛选。正如预期的那样,两种化合物均被鉴定为 CCB,对 ACE 抑制的选择性不同。它们对 ACE 和 CCB 的选择性可用于治疗耐药性高血压。