title: Discovery of indole-based tetraarylimidazoles as potent inhibitors of urease with low antilipoxygenase activity.
abstract: A series of tetraarylimidazoles (5A-5O) were prepared by one pot four component condensation reactions of 2-arylindole-3-carbaldehydes, substituted anilines, benzil and ammonium acetate in acetic acid. The synthesized compounds exhibited potent antiurease activity with IC50 values ranging from 0.12 ± 0.06 μM to 29.12 ± 0.18 μM as compared with thiourea. However, low inhibition profiles were observed for lipoxygenase. The data show that tetraarylimidazoles containing a substituted 2-penylindole have emerged as a new class of potent inhibitors of urease enzyme.
authors: Institute of Chemistry, University of the Punjab, Quaid-e-Azam Campus, Lahore, Pakistan. Electronic address: phdline123@yahoo.com.
authors: Sadia
authors: S
authors: Naureen
authors: Institute of Chemistry, University of the Punjab, Quaid-e-Azam Campus, Lahore, Pakistan.
authors: Faryal
authors: F
authors: Chaudhry
authors: Institute of Chemistry, University of the Punjab, Quaid-e-Azam Campus, Lahore, Pakistan.
authors: Nadia
authors: N
authors: Asif
authors: Institute of Chemistry, University of the Punjab, Quaid-e-Azam Campus, Lahore, Pakistan.
authors: Munawar Ali
authors: MA
authors: Munawar
authors: Department of Chemistry, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan.
authors: Muhammad
authors: M
authors: Ashraf
authors: Department of Chemistry, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan.
authors: Faizul Hassan
authors: FH
authors: Nasim
authors: Department of Chemistry, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan.
authors: Humera
authors: H
authors: Arshad
authors: Institute of Chemistry, University of the Punjab, Quaid-e-Azam Campus, Lahore, Pakistan; Department of Chemistry, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan.
authors: Misbahul Ain
authors: MA
authors: Khan
mesh_terms: D032449:Canavalia / Q000201:enzymology; D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008084:Lipoxygenase / Q000378:metabolism*; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D014510:Urease / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D007093:Imidazoles; D008084:Lipoxygenase; D014510:Urease
keywords: Ammonium acetate; Lipoxygenase inhibition; Multicomponent reaction; Thiourea; Urease inhibition