Synthesis, Bioactivity, Molecular Docking and POM Analyses of Novel Substituted Thieno[2,3-b]thiophenes and Related Congeners
Yahia N. Mabkhot,
Fahad D. Aldawsari,
Salim S. Al-Showiman,
Assem Barakat,
Taibi Ben Hadda,
Mohammad S. Mubarak,
Sehrish Naz,
Zaheer Ul-Haq,
Abdur Rauf
Affiliations
Yahia N. Mabkhot
Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia
Fahad D. Aldawsari
King Abdulaziz City for Science and Technology, P.O. Box 6086, Riyadh 11442, Saudi Arabia
Salim S. Al-Showiman
Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia
Assem Barakat
Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia
Taibi Ben Hadda
Lab of Chemical Material, Faculty of Sciences University Mohammed Premier, Oujda 60000, Morocco
Mohammad S. Mubarak
Department of Chemistry, The University of Jordan, Amman 11942, Jordan
Sehrish Naz
Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75210, Pakistan
Zaheer Ul-Haq
Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75210, Pakistan
Abdur Rauf
Institute of Chemical Sciences, University of Peshawar, Peshawar 25120, Pakistan
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.
