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 |