SYNTHESIS AND PRELIMINARY ALKYLATING ACTIVITIES OF CERTAIN NEW 1,4-DIHYDROPYRIDINES, PYRIDINIUM SALTS AND 2,7-DIAZABICYCLO [4.1.0] HEPT-3-ENES | ||
| Bulletin of Pharmaceutical Sciences Assiut University | ||
| Article 4, Volume 16, Issue 2, December 1993, Pages 141-150 PDF (484.24 K) | ||
| Document Type: Original Article | ||
| DOI: 10.21608/bfsa.1993.70043 | ||
| Authors | ||
| Hassan H. Farag; Abdel-Alim M. Abdel-Alim; Mahmoud M. El-Gendy; Nawal A. El-Koussi | ||
| Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiut, Egypt | ||
| Abstract | ||
| 3-Substituted-1-{2-chloro- or [2-bis (2-chloroethyl)amino]}ethyl-1,4-dihydropyridines 3 and 6 were prepared by reduction of the corresponding pyridinium chlorides 2 and 5 with sodium dithionite in alkaline medium. The l,3-dipolar cycloaddition of either phenylsulphonyl or p-tolylsulphonyl azides to the l,4-dihydropyridines 3 afforded the corresponding 2,7-diazabicyclo[4.1. 0]hept-3-enes 7. The alkylating activities of twelve new compounds (2b-d; 3b,c; 5a-c and 7a-d) were determined kinetically in comparison to chlorambucil as a reference drug. Compounds 5a-c showed higher activities than chlorambucil while 2c,d and 7a,b showed lower activities. The dihydropyridines (the CDS) 3b,c were inactive as alkylating agents as expected. | ||
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