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Biologically active scaffolds: Synthesis, characterization and studies of oxino bis-pyrazoles by environmental friendly method

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dc.contributor.author Aslam, Noreen
dc.contributor.author M. White, Jonathan
dc.contributor.author Ghafoor, Abdul
dc.contributor.author Shafique, Ajmal
dc.contributor.author Hassan Nasim, Faizul
dc.contributor.author Jahan, Bakht
dc.contributor.author Ashraf, M
dc.contributor.author Jabeen, Mussarat
dc.contributor.author Madiah Zafar, Ansa
dc.contributor.author Noreen, Shazia
dc.contributor.author Sajid, Naveed
dc.contributor.author Ain Khan, Misbahul
dc.date.accessioned 2022-12-14T04:40:36Z
dc.date.available 2022-12-14T04:40:36Z
dc.date.issued 2019-03-20
dc.identifier.citation Aslam, N., White, J. M., Ghafoor, A., Shafique, A., Nasim, F. H., Jahan, B., ... & Khan, M. A. (2019). Biologically active scaffolds: Synthesis, characterization and studies of oxino bis-pyrazoles by environmental friendly method. Pakistan Journal of Pharmaceutical Sciences, 32. en_US
dc.identifier.uri http://142.54.178.187:9060/xmlui/handle/123456789/15078
dc.description.abstract In the present communication, synthesis of bis-pyrazolones containing aryl motifs (4-14) and their αglucosidase inhibitory activity, hemolytic and antihemolytic activities were reported. The newly synthesized compounds were characterized by analytical techniques such 1H-NMR, 13C-NMR, IR, mass spectrometry and compound No 4 additionally by X-ray crystallography. Compounds 4, 12, 14 were obtained in more than 85% yield. In comparison to typical acarbose (IC50 = 37.38±0.12µM), all synthesized compounds showed potent activity with IC50 values between 31.26±0.11 to 396.25±0.18μM. The most potent compounds 6, 8 and 11 showed IC50 values within the range of 31.26±0.11 to 37.48±0.12μM. Compounds 7, 10, 12 and 13 showed IC50 values within the range of 65.23±0.12 to 154.87±0.16μM, while compounds 4, 5 and 9 showed moderate inhibition with IC50 values 286.56±0.16 to 396.25±0.18μM. Structure-activity relationship (SAR) studies, suggests that electron withdrawing groups played a crucial role in enhancing α-glucosidase inhibitory effects of title compounds. In addition, results of the hemolytic and antihemolytic activity studies indicated that compound 13 possessed moderate levels of hemolytic and highest anti- hemolytic activity while 8 showed low anti- hemolytic and high hemolytic activity. en_US
dc.language.iso en en_US
dc.publisher Karachi:Pakistan Journal of Pharmaceutical Sciences, university of Karachi. en_US
dc.subject Bis-pyrazolones, Glycine en_US
dc.subject α-glucosidase activity en_US
dc.subject Haemolytic activity en_US
dc.subject Anti-haemolytic activity en_US
dc.subject X-ray crystallography en_US
dc.title Biologically active scaffolds: Synthesis, characterization and studies of oxino bis-pyrazoles by environmental friendly method en_US
dc.type Article en_US


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