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The central aim is to evaluate the hypotensive effects of new pyrimidinone derivatives in comparison to established drugs.

April 30, 2026Die PharmazieOpen Access

Computer-based drug design, synthesis and biological evaluation of new pyrimidinone derivatives linked to arylpiperazine and 2′-carbethoxy-biphenylylmethyl moeities as α1-adrenoceptor antagonists and angiotensin II AT1 receptor antagonists

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The central aim is to evaluate the hypotensive effects of new pyrimidinone derivatives in comparison to established drugs.
Designed and synthesized two series of pyrimidinone derivatives with arylpiperazine and biphenylylmethyl moieties.
Conducted in vivo biological evaluation on normotensive cats to assess blood pressure effects.
Utilized molecular modeling to predict fitting affinities of compounds against α1-AR and Ang II antagonist hypotheses.
Compound IIIc demonstrated the highest hypotensive activity among α1-AR antagonists tested.
Compound XIa showed hypotensive activity comparable to losartan in the Ang II receptor context.

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Biological evaluation demonstrates pyrimidinone derivatives lower blood pressure in normotensive cats, indicating their potential as drugs.

Ismail et al. (2010) studied this question.

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Biological evaluation demonstrates pyrimidinone derivatives lower blood pressure in normotensive cats, indicating their potential as drugs.