Synthesis of Tetrahydrobenzothieno 2,3-dpyrimidine and Tetrahydrobenzothieno3,2-e- 1,2,4triazolo4,3-cpyrimidine Derivatives as Potential Antimicrobial AgentsReport as inadecuate




Synthesis of Tetrahydrobenzothieno 2,3-dpyrimidine and Tetrahydrobenzothieno3,2-e- 1,2,4triazolo4,3-cpyrimidine Derivatives as Potential Antimicrobial Agents - Download this document for free, or read online. Document in PDF available to download.

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, Alexandria, Egypt





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Abstract Five series of tetrahydrobenzothieno2,3-dpyrimidine and tetrahydrobenzothienotriazolopyrimidine derivatives have been synthesized namely: 4-substituted amino-5,6,7,8-tetrahydro1benzothieno2,3-dpyrimidines 4a–d, 4-substituted methylidenehydrazino-5,6,7,8-tetrahydro1benzothieno- 2,3-dpyrimidines 6a–c, 4-3,5-disubstituted pyrazol-1-yl-5,6,7,8-tetrahydro- 1benzothieno2,3-dpyrimidines 7a,b, 3-substituted-8,9,10,11-tetrahydro- 1benzothieno3,2-e1,2,4triazolo4,3-cpyrimidines 8a,b, N-phenyl or 4-substituted phenyl-2-8,9,10,11-tetrahydro1benzothieno3,2-e1,2,4- triazolo4,3-cpyrimidin-3-ylsulfanylacetamides 10a–c. Preliminary antimicrobial testing revealed that compounds 4a and 10b were the most active among the tested compounds against C. albicans showing IZ = 22 mm and MIC = MBC = 31.25 μg-ml, with no significant antibacterial activity. Compounds 6b and 6c showed the highest antibacterial activity against S. aureus IZ = 21 mm, MIC = 62.5 μg-ml, MBC = 125 μg-ml for 6b; IZ = 21 mm, MIC = MBC = 125 μg-ml for 6c. Compounds 4c and 6c showed the highest antibacterial potency against P. aeruginosa among the tested compounds IZ = 19–20 mm, MIC = MBC = 62.5 μg-ml. None of the tested compounds showed significant antibacterial activity against E. coli.

Keywords: Tetrahydrobenzothieno2,3-dpyrimidine; Triazolotetrahydrobenzothienopyrimidine; Pyrazole; Synthesis; Antimicrobial activity Tetrahydrobenzothieno2,3-dpyrimidine; Triazolotetrahydrobenzothienopyrimidine; Pyrazole; Synthesis; Antimicrobial activity





Author: Raafat SOLIMAN, Nargues S. HABIB, Alaa A. EL-TOMBARY * , Soad A. M. EL-HAWASH and Omaima G. SHAABAN

Source: http://mdpi.com/



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