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- Title
Antimicrobial Activity of Some Novel Armed Thiophene Derivatives and Petra/Osiris/Molinspiration (POM) Analyses.
- Authors
Mabkhot, Yahia Nasser; Alatibi, Fatima; El-Sayed, Nahed Nasser E.; Al-Showiman, Salim; Kheder, Nabila Abdelshafy; Wadood, Abdul; Rauf, Abdur; Bawazeer, Saud; Hadda, Taibi Ben
- Abstract
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.
- Subjects
THIOPHENE derivatives; ANTI-infective agents; NUCLEOPHILES; ANILINE; CHLOROANILINE
- Publication
Molecules, 2016, Vol 21, Issue 2, p222
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules21020222