10.1002/ardp.19893220607
Prazosin, a selective a1-adrenergic antagonist used in antihypertensive therapy, has limitations due to its short half-life and side effects. To address these issues, the researchers synthesized new analogues by modifying the C-2 side-chain of prazosin, incorporating fragments from tienilic acid, guanethidine, and lidoflazine. The compounds were synthesized using various chemical procedures and their structures were confirmed through analytical data. The pharmacological properties were evaluated in terms of acute toxicity and hypotensive effects in mice and genetically hypertensive rats, respectively. The results showed that compound 5, featuring a tienilic residue in place of the furan ring, exhibited the highest hypotensive effect and a more long-lasting activity compared to prazosin. The study concludes that the new compounds, particularly compound 5, have potential for improved pharmacokinetic properties and hypotensive activity, warranting further investigation for their therapeutic applications.