Mar 28, 2018 - Author(s): Bilal Ahmad Khan*, Safeena Zafar, Ehsan Ullah Mughal, ... Akhter, Ihsan -ul- Haq, Amina Sadiq, Khalid Mohammed Khan.
3/28/2018
Design and Synthesis of Novel 1,3,4-Oxadiazole Derivatives Bearing Azo Moiety as Biologically Significant Scaffolds | BenthamScience
(/)
Search
Search for... Search in:
All
Article
Chapter
eBook
Design and Synthesis of Novel 1,3,4-Oxadiazole Derivatives Bearing Azo Moiety as Biologically Significant Scaffolds (E-pub Abstract Ahead of Print)
Full-Text Inquiry
Author(s): Bilal Ahmad Khan*, Safeena Zafar, Ehsan Ullah Mughal, Muhammad Naeem Ahmed, Syeda Shamila Hamdani, Tashfeen Akhter, Ihsan -ul- Haq, Amina Sadiq, Khalid Mohammed Khan. Journal Name: Letters in Drug Design & Discovery Volume 15 , 2018 DOI : 10.2174/1570180815666180326152204 (https://doi.org/10.21 74/1570180815666180326152204) Journal Home (/node/634)
Abstract: A series of 1,3,4-oxadiazole-2-thiol derivatives bearing azo moiety have been designed and synthesized by multistep reaction sequences. The newly synthesized compounds were characterized by spectroscopic techniques (IR, UV-Vis, NMR and MS). These compounds were investigated for their antimicrobial, cytotoxic, α-amylase and protein kinase inhibitory and antileishmanial potential. Antibacterial activity was investigated against four bacterial strains i.e. E. coli, P. aeruginosa, S. aureusand B. subtilis and good level of microbial inhibition was exhibited by most of the compounds with MIC 6.25 μg/mL. Brine Shrimp lethality assay revealed that the compound 31 is an excellent cytotoxic agent. (E)-5-(4-((4Butoxyphenyl)diazenyl)phenyl)-1, 3,4-oxadiazole-2-thiol (21) showed good α-amylase inhibition (46.3± 0.45%) and (E)-2-(Decyloxythio)-5-(4-((propoxyphenyl)diazenyl)phenyl)-1,3,4-oxadiazole (30) exhibited
http://www.eurekaselect.com/160728
1/2
3/28/2018
Design and Synthesis of Novel 1,3,4-Oxadiazole Derivatives Bearing Azo Moiety as Biologically Significant Scaffolds | BenthamScience
excellent antileishmanial activity (88.4± 0.34%) at 10 µg/mL concentration. In case of protein kinase inhibition, remarkably, the oxadiazole-2-thiols (20-25) were found more active than the standard surfactinat tested concentration (25 µg/disc). Keywords: Azo-compounds, 1, 3, 4-Oxadiazole, Biological Activity, Thioethers, Cytotoxicity, Enzyme Inhibition, Protein Kinase Inhibition Full-Text Inquiry
Rights & Permissions
Print
Export
Other
Article Details VOLUME: 15 Year: 2018 (E-pub Abstract Ahead of Print) DOI: 10.2174/1570180815666180326152204 (https://doi.org/10.2174/1570180815666180326152204) Price: $95
(/terms/termandcondition.html?1)
© 2018 Bentham Science Publishers (http://www.eurekaselect.com/136826/page/terms-and-conditions)
http://www.eurekaselect.com/160728
2/2
