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Molecules 2016, 21(2), 222;

Antimicrobial Activity of Some Novel Armed Thiophene Derivatives and Petra/Osiris/Molinspiration (POM) Analyses

Department of Chemistry, College of Science, King Saud University, P. O. Box 2455, Riyadh-11451, Saudi Arabia
National Organization for Drug Control and Research, Agouza, Giza 35521, Egypt
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, King Khalid University, Abha 61441, Saudi Arabia
Department of Chemistry, Faculty of Science, Cairo University, Giza 12613, Egypt
Department of Biochemistry, UCSS, Abdul Wali Khan University Mardan, Mardan 23250, Pakistan
Department of Geology, University of Swabi, Khyber Pakhtunkhwa, Anbar 23561, Pakistan
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Umm Al-Qura University, P. O. Box 42, Makkah 21955, Saudi Arabia
LCM Laboratory, Faculty of Sciences, University of Mohamed Premier, Oujda 60000, Morocco
Author to whom correspondence should be addressed.
Academic Editor: Maria Emília de Sousa
Received: 5 January 2016 / Revised: 28 January 2016 / Accepted: 1 February 2016 / Published: 17 February 2016
(This article belongs to the Section Bioorganic Chemistry)
Full-Text   |   PDF [6830 KB, uploaded 22 February 2016]   |  


Tetrasubstituted 2-acetylthiophene derivative 5 was synthesized and then condensed with various nitrogen nucleophiles such as 5-amino-1,2,4-triazole, 2-aminobenzimidazole, aniline or p-chloroaniline to afford the corresponding iminothiophene derivatives 6–8a,b. Condensation of thiophene 5 with malononitrile as carbon nucleophile afforded compound 9, which underwent nucleophilic addition with DMF-DMA to afford compound 10. The newly synthesized products were characterized by elemental analysis, IR, MS, 1H-13C-NMR and CHN analysis and then evaluated for their antimicrobial activity. Results of the in vitro antibacterial activity showed that thiophene derivative 7 was found to be more potent than the standard drug gentamicin against Pseudomonas aeruginosa. Some of these compounds showed potential antimicrobial activities. Molecular docking and Osiris/Molinspiration analyses show the crucial role and impact of substituents on bioactivity and indicate the unfavorable structural parameters in actual drug design: more substitution with electronic donor group doesn’t guarantee more effective bioactivity. This study should greatly help in an intelligent and a controlled pharmacomodulation of antibiotics. View Full-Text
Keywords: armed thiophenes; antimicrobial activity; Petra/Osiris/Molinspiration (POM) analyses armed thiophenes; antimicrobial activity; Petra/Osiris/Molinspiration (POM) analyses

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Mabkhot, Y.N.; Alatibi, F.; El-Sayed, N.N.E.; Al-Showiman, S.; Kheder, N.A.; Wadood, A.; Rauf, A.; Bawazeer, S.; Hadda, T.B. Antimicrobial Activity of Some Novel Armed Thiophene Derivatives and Petra/Osiris/Molinspiration (POM) Analyses. Molecules 2016, 21, 222.

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