Synthesis and Evaluation of Some 1,2,3,4-Tetrahydropyrimidine-2-thione and Condensed Pyrimidine Derivatives as Potential Antihypertensive Agents

Magda M. F. Ismail; Nehad A. M. El-Sayed; Heba S. Rateb; Mohey Ellithey; Yousry A. Ammar

doi:10.1055/s-0031-1296729

Arzneimittelforschung, Inhaltsverzeichnis

Arzneimittelforschung 2006; 56(5): 322-327
DOI: 10.1055/s-0031-1296729

Antihypertensives

Editio Cantor Verlag Aulendorf (Germany)

Synthesis and Evaluation of Some 1,2,3,4-Tetrahydropyrimidine-2-thione and Condensed Pyrimidine Derivatives as Potential Antihypertensive Agents

Autor*innen

Magda M. F. Ismail

¹Department of Pharmaceutical Chemistry, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt
Nehad A. M. El-Sayed

²Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Cairo, Egypt
Heba S. Rateb

¹Department of Pharmaceutical Chemistry, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt
Mohey Ellithey

³Department of Pharmacology, National Research Center, Cairo, Egypt
Yousry A. Ammar

⁴Department of Organic Chemistry, Faculty of Science, Al-Azhar University, Cairo, Egypt

Abstract

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Summary

Some new tetrahydropyrimidine-2-thione, octahydroquinazoline-2-thione and thiazolo[3,2-a]pyrimidine derivatives have been synthesized and tested for their antihypertensive activity. Among them, compounds 1 and 2b can be considered more potent than the reference, nifedipine (CAS 21829-25-4), while compounds 3b and 10a are equipotent to it. In addition, compound 6 showed significant antihypertensive activity.

Zusammenfassung

Synthese und Bewertung verschiedener 1,2,3,4-Tetrahydropyrimidin-2-thionund kondensierter Pyrimidin-Derivate als potentielle Antihypertensiva

Einige neue Tetrahydropyrimidin-2-thione, Octohydroquinazoline und Thiazolo[3.2-a]-pyrimidin-Derivate wurden synthetisiert und auf antihypertensive Wirkung getestet. Verbindungen 1 und 2b zeigten eine stärkere Wirkung als die Referenz Nifedipin (CAS 21829-25-4), während die Verbindungen 3b und 10a sich gleich stark zeigten. Auch die Verbindung 6 hatte eine signifikante antihypertensive Aktivität.

Key words

Antihypertensives - Octahydroquinazoline-2-thione derivatives, antihypertensive activity, synthesis - 1,2,3,4-Tetrahydro-pyrimidine-2-thione derivatives antihypertensive activity - synthesis - Thiazolo[3,2-a]pyrimidines, antihypertensive activity, synthesis

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