- Solution-phase microwave assisted parallel synthesis, biological evaluation and in silico docking studies of 2-chlorobenzoyl thioureas derivatives
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An efficient and facile microwave-assisted solution phase parallel synthesis for a 38-member library of N-aroyl-N′-aryl thioureas was accomplished successfully. These analogues (1–38) were synthesized under identical set of conditions. It has been observe
- Khan, Muhammad Riaz,Zaib, Sumera,Rauf, Muhammad Khawar,Ebihara, Masahiro,Badshah, Amin,Zahid, Muhammad,Nadeem, Muhammad Arif,Iqbal, Jamshed
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p. 354 - 362
(2018/05/29)
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- Biological evaluation of halogenated thioureas as cholinesterases inhibitors against alzheimer's disease & molecular modeling studies
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Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition is thought to be an encouraging approach towards the therapy of Alzheimer's disease (AD). The current paper targets to give a concise information of mono and dihalo- substituted thioureas similarity with anti-AD potential. The present results represent evaluation of cholinesterase inhibitory potential for halogenated thioureas derivatives. Compound 1t was constituted to be highly potent inhibitor with Ki value 0.12 ± 0.05 μM against AChE, while 1b was most the active inhibitor for BChE with Ki value of 0.03 ± 0.001 μM. Molecular docking simulations were performed using the homology models of both cholinesterases in order to explore the plausible binding modes of synthesized compounds.
- Iqbal, Jamshed,Zaib, Sumera,Saeed, Aamer,Muddassar, Muhammad
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p. 488 - 494
(2015/06/22)
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- Synthesis and antimicrobial activity of some novel 2-(substituted fluorobenzoylimino)-3-(substituted fluorophenyl)-4-methyl-1,3-thiazolines
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The synthesis of several 2-(substituted fluorobenzoylimino)-3-(substituted fluorophenyl)-4-methyl-1,3-thiazolines (2a-t) was carried out by base-catalyzed cyclization of corresponding 1-(fluorobenzoyl)-3-(fluorophenyl)thioureas (1a-t) with 2-bromoacetone in aqueous medium. The structures of the synthesized compounds were confirmed by spectral and elemental analysis. All synthesized compounds were evaluated for in vitro antibacterial activity using Gram-positive bacteria (Staphylococcus aureus, Bacillus subtilis) and Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa). The minimum inhibitory concentration (MIC) was determined for the most active compounds. In vitro antifungal activity was also determined against the five fungal species (Rhizopus oryzae, Fusarium oxysporum, Aspergillus terreus, A. niger and A. fumigatus).
- Saeed, Aamer,Shaheen, Uzma,Hameed, Abdul,Kazmi, Faiza
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body text
p. 333 - 339
(2010/04/30)
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- Synthesis, characterization and antimicrobial activity of some new 1-(fluorobenzoyl)-3-(fluorophenyl)thioureas
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Synthesis of a variety of new 1-(isomeric fluorobenzoyl)-3-(isomeric fluorophenyl)thioureas (1a-t) was accomplished in two steps. The synthetic route involves the reaction of equimolar quantities of isomeric fluorobenzoyl chlorides with potassium thiocyanate in anhydrous acetone to afford the corresponding isothiocyantes in situ, followed by treatment with equimolar quantities of isomeric fluoroanilines. All of the synthesized compounds (1a-t) were screened for their in vitro antibacterial activity using Gram-positive bacteria (Staphylococcus aureus, Bacillus subtilis) and Gram-negative bacteria (Escherichia coli, Pseudomonas aureginosa). The minimum inhibitory concentration (MIC) was also determined for the most active compounds. In vitro antifungal activity was also determined against the five fungal species (Rhizopus oryzae, Aspergillus tereus, Fusarium oxysporum, Aspergillus niger, Aspergillus fumigatus). In general, the antifungal activity of compounds was better than their antibacterial activity.
- Saeed, Aamer,Shaheen, Uzma,Hameed,Naqvi, S.Z. Haider
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experimental part
p. 1028 - 1034
(2010/04/28)
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