DESIGN, SYNTHESIS AND ANTIDIABETIC ACTIVITY OF SOME NEW 4-AMINO (OR 6-OXO)-2-METHYL/BENZYLTHIO (OR SUBSTITUTED AMINO) PYRIMIDINE DERIVATIVES
Abdel-Aziz, S., Hussein, M., Abdel-Raheem, I. (2011). DESIGN, SYNTHESIS AND ANTIDIABETIC ACTIVITY OF SOME NEW 4-AMINO (OR 6-OXO)-2-METHYL/BENZYLTHIO (OR SUBSTITUTED AMINO) PYRIMIDINE DERIVATIVES. EKB Journal Management System, 34(2), 149-158. doi: 10.21608/bfsa.2011.63262
Salah Abdel-Muttalib Abdel-Aziz; Mostafa Ahmad Hussein; Ihab Talat Abdel-Raheem. "DESIGN, SYNTHESIS AND ANTIDIABETIC ACTIVITY OF SOME NEW 4-AMINO (OR 6-OXO)-2-METHYL/BENZYLTHIO (OR SUBSTITUTED AMINO) PYRIMIDINE DERIVATIVES". EKB Journal Management System, 34, 2, 2011, 149-158. doi: 10.21608/bfsa.2011.63262
Abdel-Aziz, S., Hussein, M., Abdel-Raheem, I. (2011). 'DESIGN, SYNTHESIS AND ANTIDIABETIC ACTIVITY OF SOME NEW 4-AMINO (OR 6-OXO)-2-METHYL/BENZYLTHIO (OR SUBSTITUTED AMINO) PYRIMIDINE DERIVATIVES', EKB Journal Management System, 34(2), pp. 149-158. doi: 10.21608/bfsa.2011.63262
Abdel-Aziz, S., Hussein, M., Abdel-Raheem, I. DESIGN, SYNTHESIS AND ANTIDIABETIC ACTIVITY OF SOME NEW 4-AMINO (OR 6-OXO)-2-METHYL/BENZYLTHIO (OR SUBSTITUTED AMINO) PYRIMIDINE DERIVATIVES. EKB Journal Management System, 2011; 34(2): 149-158. doi: 10.21608/bfsa.2011.63262

DESIGN, SYNTHESIS AND ANTIDIABETIC ACTIVITY OF SOME NEW 4-AMINO (OR 6-OXO)-2-METHYL/BENZYLTHIO (OR SUBSTITUTED AMINO) PYRIMIDINE DERIVATIVES

Bulletin of Pharmaceutical Sciences Assiut University
Article 11, Volume 34, Issue 2, 2011, Page 149-158  XML PDF (289.33 K)
Document Type: Original Article
DOI: 10.21608/bfsa.2011.63262
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Authors
Salah Abdel-Muttalib Abdel-Aziz1; Mostafa Ahmad Hussein* 2; Ihab Talat Abdel-Raheem3
1Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Al-Azhar University, Assiut-71524, Egypt
2Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut-71526, Egypt
3Department of Pharmacology and Toxicology, Faculty of Pharmacy, Al-Azhar University, Assiut-71524, Egypt
Abstract
A new series of 4-amino-5-cyano-2-methyl/benzylthio (or substituted amino) 6-substituted phenyl pyrimidines 5a-l, and 2-methyl/benzylthio (or substituted amino)-5-cyano-1,6-dihydro-6oxo-4-(substitutedphenyl) pyrimidines 6a-l was prepared. The reaction of S-methyl (or benzyl) isothiourea salts 1a,b with benzylidenemalononitriles 2a-c afforded compounds 5a-f. Reaction of compounds 5a-c (R= methylthio) with the appropriate amines 4a,b (cyclohexylamine or 2phenylethylamine) afforded 4-amino-2-substituted amino-5-cyano-6- (substituted phenyl) pyrimidines 5g-l. On the other hand, reaction of S-methyl (or benzyl) isothiourea salts 1a,b with ethyl α-cyanocinnamates 3a-c afforded compounds 6a-f. Reaction of compounds 6a-c (R= methylthio) with the appropriate amines 4a,b afforded 2-substituted amino-5-cyano-4-oxo-6(substituted phenyl) pyrimidines 6g-l. The purity of the new compounds was checked by TLC and elucidation of their structures was confirmed by IR, 1H-NMR, and mass spectrometry along with elemental microanalyses. All the target compounds were evaluated for their in-vivo antidiabetic effects in rates in comparison with metformin as a reference drug.
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