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Angiotensin-converting enzyme (ACE) plays an important role in regulating blood pressure in the body by converting angiotensin-I into angiotensin-II. It is the basic component of Renin angiotensin aldosterone system (RAAS), imbalance of RAAS may leads to many cardiovascular and renal diseases. There are many marketed available drugs for the inhibition of ACE, but prolonged use of some drugs may cause the progressive side effects. Repurposing of existing drugs can be a way to find new inhibitors of ACE. In this study, a high-throughput and sensitive method of HPLC-ESI-QqQ-MS with good reproducibility (%RSD < 9.98) and linearity (R2 = 0.999) was used to investigate the 77 commercial drugs for their inhibitory potential as antihypertensive drugs. Among these drugs, 41 drugs were found active and 36 of them showed moderate to good inhibition with lowest IC50 = 272 µM. This study showed that different pharmaceutical drugs can also be used as ACE inhibitor after necessary clinical trials or validation.