955949-99-2Relevant academic research and scientific papers
Synthesis, antibacterial, antifungal and antiviral activity evaluation of some new bis-Schiff bases of isatin and their derivatives
Jarrahpour, Aliasghar,Khalili, Dariush,De Clercq, Erik,Salmi, Chanaz,Brunel, Jean Michel
, p. 1720 - 1730 (2007)
Twelve new bis-Schiff bases of isatin, benzylisatin and 5-fluoroisatin 3a-3l were prepared by condensation of isatin, benzylisatin and 5-fluoroisatin with primary aromatic amines. The chemical structures of the products were confirmed by 1H- and 13CNMR, IR and mass spectral data. The compounds were screened for antiviral activity against a panel of DNA and RNA viruses. Minimum cytotoxic and minimum virusinhibitory concentrations of these compounds were determined. Compounds 3c and 3i were the most cytotoxic in HEL cells. These newly synthesized bis-Schiff bases were also tested for their antibacterial and antifungal activities. They did not display activity against S. cerevisiae (ATCC 28383) or C. albicans (CIP 1180-79).
Computational evaluation and experimental in vitro antibacterial, antifungal and antiviral activity of bis-Schiff bases of isatin and its derivatives
Jarrahpour, Aliasghar,Sheikh, Javed,Mounsi, Ibrahim El,Juneja, Harjeet,Hadda, Taibi Ben
, p. 1203 - 1211 (2013)
A computational model has been developed for the rational design of bioactive pharmacophore sites as an antibacterial, antifungal and antiviral candidates based on available X-ray structures of bis-Schiff bases (Blagus et al., Maced J Chem Chem Eng 29:117-138, 2010; Nabei et al., Polyhedron 28:1734-1739, 2009; Zhang et al., Inorg Chem Commun 14:1636-1639, 2011; Zhong et al., Eur J Med Chem 41:1090-1092, 2006; Zhou et al., Inorg Chim Acta 359:1442-1448, 2006). A dozen of bis-Schiff bases 3-14 of isatin, benzylisatin and 5-fluoroisatin 1a-c were designed using this model. The compounds were screened for antibacterial, antifugal and antiviral activity against a panel of DNA and RNA viruses. The most potent of these compounds 8 and 11 was tested in viral cultures for their ability to present a potential (Oδ-- Nδ-) antiviral pharmacophore site. Compounds 8 and 11 were the most cytotoxic in HEL cells. All these synthesized bis-Schiff bases were also tested for their antibacterial and antifungal activities. They did not display activity against S. cerevisiae (ATCC 28383) or C. albicans (CIP 1180-79); may be because they did not have an antibacterial pharmacophore site (X δ--Yδ+). The best inhibitors tested in vitro against HIV-1 are genetically predisposed to be inhibited by similar pharmacophore sites. The results from all the aspects of this bioinformatic approaches are discussed as par with our experience with screening candidates. Graphical Abstract: [Figure not available: see fulltext.]
Synthesis of some mono- and bis-spiro-β-lactams of benzylisatin
Jarrahpour, Aliasghar,Khalili, Dariush
, p. 7140 - 7143 (2008/03/11)
Some new mono- and bis-spiro-β-lactams of benzylisatin were prepared by Staudinger's ketene-imine [2+2] cycloaddition reaction. The cycloadducts were characterized by spectral data including 1H NMR, 13C NMR, IR and mass spectra. The
