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Volume 77
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Article

Synthesis of Tetrahydrobenzothieno[ 2,3-d]pyrimidine and Tetrahydrobenzothieno[3,2-e]- [1,2,4]triazolo[4,3-c]pyrimidine Derivatives as Potential Antimicrobial Agents

by
Raafat SOLIMAN
,
Nargues S. HABIB
,
Alaa A. EL-TOMBARY
*,
Soad A. M. EL-HAWASH
and
Omaima G. SHAABAN
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, Alexandria, Egypt
*
Author to whom correspondence should be addressed.
Sci. Pharm. 2009, 77(4), 755-774; https://doi.org/10.3797/scipharm.0904-17
Submission received: 1 August 2009 / Accepted: 17 August 2009 / Published: 18 August 2009
Versions Notes

Abstract

Five series of tetrahydrobenzothieno[2,3-d]pyrimidine and tetrahydrobenzothienotriazolopyrimidine derivatives have been synthesized namely: 4-(substituted amino)-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidines 4a–d, 4-substituted (methylidenehydrazino)-5,6,7,8-tetrahydro[1]benzothieno- [2,3-d]pyrimidines 6a–c, 4-(3,5-disubstituted pyrazol-1-yl)-5,6,7,8-tetrahydro- [1]benzothieno[2,3-d]pyrimidines 7a,b, 3-substituted-8,9,10,11-tetrahydro- [1]benzothieno[3,2-e][1,2,4]triazolo[4,3-c]pyrimidines 8a,b, N-(phenyl or 4-substituted phenyl)-2-(8,9,10,11-tetrahydro[1]benzothieno[3,2-e][1,2,4]- triazolo[4,3-c]pyrimidin-3-ylsulfanyl)acetamides 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: Tetrahydrobenzothieno[2,3-d]pyrimidine; Triazolotetrahydrobenzothienopyrimidine; Pyrazole; Synthesis; Antimicrobial activity Tetrahydrobenzothieno[2,3-d]pyrimidine; Triazolotetrahydrobenzothienopyrimidine; Pyrazole; Synthesis; Antimicrobial activity

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MDPI and ACS Style

SOLIMAN, R.; HABIB, N.S.; EL-TOMBARY, A.A.; EL-HAWASH, S.A.M.; SHAABAN, O.G. Synthesis of Tetrahydrobenzothieno[ 2,3-d]pyrimidine and Tetrahydrobenzothieno[3,2-e]- [1,2,4]triazolo[4,3-c]pyrimidine Derivatives as Potential Antimicrobial Agents. Sci. Pharm. 2009, 77, 755-774. https://doi.org/10.3797/scipharm.0904-17

AMA Style

SOLIMAN R, HABIB NS, EL-TOMBARY AA, EL-HAWASH SAM, SHAABAN OG. Synthesis of Tetrahydrobenzothieno[ 2,3-d]pyrimidine and Tetrahydrobenzothieno[3,2-e]- [1,2,4]triazolo[4,3-c]pyrimidine Derivatives as Potential Antimicrobial Agents. Scientia Pharmaceutica. 2009; 77(4):755-774. https://doi.org/10.3797/scipharm.0904-17

Chicago/Turabian Style

SOLIMAN, Raafat, Nargues S. HABIB, Alaa A. EL-TOMBARY, Soad A. M. EL-HAWASH, and Omaima G. SHAABAN. 2009. "Synthesis of Tetrahydrobenzothieno[ 2,3-d]pyrimidine and Tetrahydrobenzothieno[3,2-e]- [1,2,4]triazolo[4,3-c]pyrimidine Derivatives as Potential Antimicrobial Agents" Scientia Pharmaceutica 77, no. 4: 755-774. https://doi.org/10.3797/scipharm.0904-17

APA Style

SOLIMAN, R., HABIB, N. S., EL-TOMBARY, A. A., EL-HAWASH, S. A. M., & SHAABAN, O. G. (2009). Synthesis of Tetrahydrobenzothieno[ 2,3-d]pyrimidine and Tetrahydrobenzothieno[3,2-e]- [1,2,4]triazolo[4,3-c]pyrimidine Derivatives as Potential Antimicrobial Agents. Scientia Pharmaceutica, 77(4), 755-774. https://doi.org/10.3797/scipharm.0904-17

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