title: Synthesis and evaluation of chalcone analogues based pyrimidines as angiotensin converting enzyme inhibitors.
abstract: Hypertension is a widespread and frequently progressive ailment that imparts a foremost threat for cardiovascular and renal disorders. Mammoth efforts are needed for the synthesis of innovative antihypertensive agents to combat this lethal disease. Chalcones have shown antihypertensive activity through inhibition of Angiotensin Converting Enzyme (ACE). Hence, a series of chalcone analogues is synthesized and used as precursor for the synthesis of novel series of pyrimidines. Precursor chalcones were prepared by reacting aldehydes and ketones in presence of sodium hydroxide followed by synthesis of corresponding pyrimidines by reaction with urea in presence of potassium hydroxide. Both groups were then evaluated for their effects on ACE. The results depicted that pyrimidines were more active than chalcones with methoxy (C5 and P5) substitution showing best results to inhibit ACE. Given that chalcone analogues and pyrimidines show a potential as the angiotensin converting enzyme inhibitors.
authors: S N A
authors: SN
authors: Bukhari
authors: Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Kuala Lumpur,50300, Malaysia.
authors: A M
authors: AM
authors: Butt
authors: Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Kuala Lumpur,50300, Malaysia.
authors: M W B
authors: MW
authors: Amjad
authors: Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Kuala Lumpur,50300, Malaysia.
authors: W
authors: W
authors: Ahmad
authors: Department of Chemistry, Saurashtra University, Rajkot- 360 005, Gujarat, India.
authors: V H
authors: VH
authors: Shah
authors: Department of Chemistry, Saurashtra University, Rajkot- 360 005, Gujarat, India.
authors: A R
authors: AR
authors: Trivedi
mesh_terms: D000806:Angiotensin-Converting Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002599:Chalcone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006973:Hypertension / Q000188:drug therapy / Q000378:metabolism; D007703:Peptidyl-Dipeptidase A / Q000378:metabolism; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011817:Rabbits
chemical_list: D000806:Angiotensin-Converting Enzyme Inhibitors; D000959:Antihypertensive Agents; D011743:Pyrimidines; D002599:Chalcone; D007703:Peptidyl-Dipeptidase A