Vasorelaxant activity of phthalazinones and related compounds

Bioorganic & Medicinal Chemistry Letters
E del OlmoA San Feliciano

Abstract

Several series of dihydrostilbenamide, imidazo[2,1-a]isoindole, pyrimido[2,1-a]isoindole and phthalazinone derivatives were obtained and their vasorelaxant activity was measured on isolated rat aorta rings pre-contracted with phenylephrine (10(-5)M). Some phthalazinones attained, practically, the total relaxation of the organ at micromolar concentrations. For the most potent compound 9h (EC(50)=0.43microM) the affinities for alpha(1A), alpha(1B) and alpha(1D) adrenergic sub-receptors were determined.

References

Sep 4, 1992·Journal of Medicinal Chemistry·T MatsuiK Ohmoto
Oct 2, 1990·European Journal of Pharmacology·H K LeeN Sperelakis
Aug 24, 2000·Journal of Medicinal Chemistry·S GrassoC De Micheli
Aug 22, 2001·Bioorganic & Medicinal Chemistry Letters·E del OlmoA San Feliciano
Oct 10, 2001·Bioorganic & Medicinal Chemistry Letters·E del OlmoA San Feliciano
Oct 16, 2001·European Journal of Medicinal Chemistry·G R MadhavanR Rajagopalan
Feb 19, 2004·Archives of Pharmacal Research·Seref DemirayakBasar Sirmagul
Jun 29, 2005·Bioorganic & Medicinal Chemistry Letters·Alejandro ZamilpaArturo San Feliciano

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Citations

Dec 22, 2012·The Journal of Organic Chemistry·Nayyef AljaarUwe Beifuss
Dec 21, 2019·The Journal of Antimicrobial Chemotherapy·Julianna Siciliano De AraújoMaria de Nazaré Correia Soeiro
May 21, 2020·Acta Crystallographica. Section E, Crystallographic Communications·David Chukwuma IzuoguEdward R T Tiekink
Aug 12, 2019·Bioorganic & Medicinal Chemistry·Jaiprakash SangshettiDevanand B Shinde

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