Hypertension is a chronic increase in blood pressure, characterized as primary and secondary hypertension. The disorder is associated with various risk factors like obesity, diabetes, age, lack of exercise etc. Hypertension is being treated since ancient times by Ayurvedic, Chinese and Unani medicine. Now various allopathic drugs are available which include diuretics, calcium channel blockers, α-blockers, β-blockers, vasodilators, central sympatholytics and ACE-inhibitors. Non-pharmacological treatments include weight reduction, dietary sodium reduction, increased potassium intake and reduction in alcohol consumption. ACE-inhibitors are widely used in the treatment of hypertension by inhibiting the angiotensin converting enzyme responsible for the conversion of angiotensin I to angiotensin II (responsible for vasoconstriction). Various structure activity relationship studies led to the synthesis of ACE-inhibitors, some are under clinical development. This comprehensive review gives various guidelines on classification of hypertension, hypertension therapy including ancient, pharmacological, nonpharmacological therapies, pharmacoeconomics, historical perspectives of ACE, renin, renin angiotensin system (circulating vs local RAS), mechanism of ACE inhibitors, and development of ACE inhibitors. Review also emphasizes on the recent advancements on ACE inhibitors including drugs in clinical trials, computational studies on ACE-inhibitors, peptidomimetics, dual, natural, multi-functional ACE inhibitors, and conformational requirements for ACE-inhibitors. HYPERTENSION: Hypertension is a chronic increase in arterial blood pressure. In general if the diastolic blood pressure is more than 80 mm/Hg and systolic blood pressure more than 120 mm/Hg the person is said to be hypertensive 1 . The Natural history of hypertension was first reported by Frederick Mahomed (1849-1884) 2 . Hypertension is categorized primarily two types viz primary hypertension and secondary hypertension.Primary Hypertension: Primary hypertension also known as essential hypertension which is a heterogeneous disorder having different causal factors in different patients that lead to high blood pressure. It may be due to stress, high fat, high sodium diet, secondary causes such as renovascular disease, renal failure, pheochromocytoma, aldosteronism or other causes of hypertension are not present. It includes total of 95% of all cases of hypertension 3-4 .