SYNTHESIS OF SOME NOVEL 1,3,6-TRISUBSTITUTED-1HTHIAZOLO[3,2-f]PURINE-2,4-DIONES AND XANTHINE SCHIFF BASES AS POTENIAL ANTI-ASTHMATIC AND ANTIINFLAMMATORY AGENTS
Hayallah, A., Shmeis, R., Talhouni, A. (2015). SYNTHESIS OF SOME NOVEL 1,3,6-TRISUBSTITUTED-1HTHIAZOLO[3,2-f]PURINE-2,4-DIONES AND XANTHINE SCHIFF BASES AS POTENIAL ANTI-ASTHMATIC AND ANTIINFLAMMATORY AGENTS. EKB Journal Management System, 38(1), 31-46. doi: 10.21608/bfsa.2015.63174
Alaa M. Hayallah; Reham Abu Shmeis; Ahmad A. Talhouni. "SYNTHESIS OF SOME NOVEL 1,3,6-TRISUBSTITUTED-1HTHIAZOLO[3,2-f]PURINE-2,4-DIONES AND XANTHINE SCHIFF BASES AS POTENIAL ANTI-ASTHMATIC AND ANTIINFLAMMATORY AGENTS". EKB Journal Management System, 38, 1, 2015, 31-46. doi: 10.21608/bfsa.2015.63174
Hayallah, A., Shmeis, R., Talhouni, A. (2015). 'SYNTHESIS OF SOME NOVEL 1,3,6-TRISUBSTITUTED-1HTHIAZOLO[3,2-f]PURINE-2,4-DIONES AND XANTHINE SCHIFF BASES AS POTENIAL ANTI-ASTHMATIC AND ANTIINFLAMMATORY AGENTS', EKB Journal Management System, 38(1), pp. 31-46. doi: 10.21608/bfsa.2015.63174
Hayallah, A., Shmeis, R., Talhouni, A. SYNTHESIS OF SOME NOVEL 1,3,6-TRISUBSTITUTED-1HTHIAZOLO[3,2-f]PURINE-2,4-DIONES AND XANTHINE SCHIFF BASES AS POTENIAL ANTI-ASTHMATIC AND ANTIINFLAMMATORY AGENTS. EKB Journal Management System, 2015; 38(1): 31-46. doi: 10.21608/bfsa.2015.63174

SYNTHESIS OF SOME NOVEL 1,3,6-TRISUBSTITUTED-1HTHIAZOLO[3,2-f]PURINE-2,4-DIONES AND XANTHINE SCHIFF BASES AS POTENIAL ANTI-ASTHMATIC AND ANTIINFLAMMATORY AGENTS

Bulletin of Pharmaceutical Sciences Assiut University
Article 3, Volume 38, Issue 1, 2015, Pages 31-46    PDF (533.99 K)
Document Type: Original Article
DOI: 10.21608/bfsa.2015.63174
Authors
Alaa M. Hayallah* 1, 2; Reham Abu Shmeis3; Ahmad A. Talhouni4
1Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut, Egypt
2Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Deraya University, El-Minia, Egypt
3Department of Basic Pharmaceutical Sciences (Analytical Chemistry), Faculty of Pharmacy, Israa University, Amman, Jordan
4Department of Applied Pharmaceutical Sciences (Pharmacology), Faculty of Pharmacy, Israa University, Amman, Jordan
Abstract
In this study, the design, synthesis and preliminary pharmacological investigation of novel 1,3-diethyl-8-disubstituted xantines 12-18, 1,3,6-trisubstituted-1H-thiazolo[3,2-f]purine-2,4diones 19-25 and xanthine Schiff bases 28-33 was described. 1,3-Diethyl-8-substituted xantines 12-18 were prepared by the reaction of 1,3-diethyl-8-thioxo-3,7,8,9-tetrahydropurine-2,6-dione 4 with the appropriate phenacyl bromides 5-11. Compound 4 was in turn prepared by the reaction of 5,6-diamino-1,3-diethyluracil 3 with carbon disulfide. The derivatives 19-25 were obtained by cyclodehydration of compounds 12-18 in polyphosphoric acid (PPA). Schiff bases 28-33 were synthesized by the reaction of acetohydrazide 27 with appropriate aldehyde in refluxed ethanol. The effect of the new derivatives as potential anti-asthmatic was evaluated using acetycholine induced brocnhospasm in Guinea pigs, most of tested compounds showed significant anti-bronchoconstriction activity in comparison with aminophylline as a standard drug. Anti-inflammatory activity of the target compounds was investigated using indomethacin as a reference drug and some compounds exhibited potent anti-inflammatory activity.
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