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Molecules 2015, 20(2), 1824-1841; doi:10.3390/molecules20021824

Synthesis, Bioactivity, Molecular Docking and POM Analyses of Novel Substituted Thieno[2,3-b]thiophenes and Related Congeners

1
Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia
2
King Abdulaziz City for Science and Technology, P.O. Box 6086, Riyadh 11442, Saudi Arabia
3
Department of Chemistry, Faculty of Science, Alexandria University, P.O. Box 426, Ibrahimia 21321 Alexandria, Egypt
4
Lab of Chemical Material, Faculty of Sciences University Mohammed Premier, Oujda 60000, Morocco
5
Department of Chemistry, The University of Jordan, Amman 11942, Jordan
6
Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75210, Pakistan
7
Institute of Chemical Sciences, University of Peshawar, Peshawar 25120, Pakistan
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 17 December 2014 / Revised: 13 January 2015 / Accepted: 14 January 2015 / Published: 23 January 2015
(This article belongs to the Section Organic Synthesis)
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Abstract

Several series of novel substituted thienothiophene derivatives were synthesized by reacting the synthone 1 with different reagents. The newly synthesized compounds were characterized by means of different spectroscopic methods such as IR, NMR, mass spectrometry and by elemental analyses. The new compounds displayed significant activity against both Gram-positive and Gram negative bacteria, in addition to fungi. Molecular docking and POM analyses show the crucial role and impact of substituents on bioactivity and indicate the unfavorable structural parameters in actual drug design: more substitution doesn’t guaranty more efficiency in bioactivity. View Full-Text
Keywords: thienothiophene; antibacterial activity; antifungal activity, molecular docking; Petra/Osiris/Molinspiration (POM) analyses thienothiophene; antibacterial activity; antifungal activity, molecular docking; Petra/Osiris/Molinspiration (POM) analyses
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Mabkhot, Y.N.; Aldawsari, F.D.; Al-Showiman, S.S.; Barakat, A.; Hadda, T.B.; Mubarak, M.S.; Naz, S.; Ul-Haq, Z.; Rauf, A. Synthesis, Bioactivity, Molecular Docking and POM Analyses of Novel Substituted Thieno[2,3-b]thiophenes and Related Congeners. Molecules 2015, 20, 1824-1841.

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