title: Synthesis of triazole Schiff bases: novel inhibitors of nucleotide pyrophosphatase/phosphodiesterase-1.
abstract: A series of Schiff base triazoles 1–25 was synthesized and evaluated for their nucleotide pyrophosphatase/phosphodiesterase-1 inhibitory activities. Among twenty-five compounds, three compounds 10 (IC50 = 132.20 ± 2.89 lM), 13 (IC50 = 152.83 ± 2.39 lM), and 22 (IC50 = 251.0 ± 6.64 lM) were identified as potent inhibitors with superior activities than the standard EDTA (IC50 = 277.69 ± 2.52 lM). The newly identified inhibitors may open a new avenue for the development of treatment of phosphodiesterase-I related disorders. These compounds were also evaluated for carbonic anhydrase, acetylcholinesterase and butyrylcholinesterase inhibitory potential and were found to be inactive. The compounds showed non-toxic effect towards PC3 cell lines.
authors.forename: Khalid Mohammed
authors.initials: KM
authors.lastname: Khan
authors.forename: Salman
authors.initials: S
authors.lastname: Siddiqui
authors.forename: Muhammad
authors.initials: M
authors.lastname: Saleem
authors.forename: Muhammad
authors.initials: M
authors.lastname: Taha
authors.forename: Syed Muhammad
authors.initials: SM
authors.lastname: Saad
authors.forename: Shahnaz
authors.initials: S
authors.lastname: Perveen
authors.forename: M Iqbal
authors.initials: MI
authors.lastname: Choudhary
mesh_terms: D000110:Acetylcholinesterase / Q000737:chemistry / Q000378:metabolism; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000378:metabolism / Q000633:toxicity; D002091:Butyrylcholinesterase / Q000737:chemistry / Q000378:metabolism; D002256:Carbonic Anhydrases / Q000737:chemistry / Q000378:metabolism; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004492:Edetic Acid / Q000737:chemistry / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000378:metabolism / Q000633:toxicity; D006801:Humans; D011485:Protein Binding; D011755:Pyrophosphatases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D012545:Schiff Bases / Q000737:chemistry*; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry* / Q000378:metabolism / Q000633:toxicity
chemical_list: D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D012545:Schiff Bases; D014230:Triazoles; D004492:Edetic Acid; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase; D011755:Pyrophosphatases; C021899:nucleotide pyrophosphatase; D002256:Carbonic Anhydrases