Design and green synthesis of 2-(diarylalkyl)aminobenzothiazole derivatives and their dual activities as angiotensin converting enzyme inhibitors and calcium channel blockers

• Novel hybrids were designed based on calcium channel blockers and ACE inhibitors.
• A green protocol was developed for their synthesis.
• Two lead molecules 4as and 4bn were identified as dual inhibitors.
• These new hybrids may be useful in treating resistant hypertension.

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.

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