Muhammad Shakeel Aslam

Synthesis, biological assay in vitro and molecular docking studies of new Schiff base derivatives as potential urease inhibitors.

A series of new and novel Schiff base derivatives were synthesized and investigated as potential new inhibitors of Jack bean urease. The most potent compounds were 3f with (K(i) = 0.09 μM) and 3k (K(i) = 0.122 μM). A pure competitive mechanism of inhibition was observed. Molecular docking studies were also performed to illustrate the binding mode of the compounds. Docking studies were performed on both enzymes from Jack bean urease and H. pylori urease. It was observed that both share the same binding mode. The binding sites of the two urease structures also aligned very well indicating the similarity in binding sites of the enzymes.

Academic dishonesty and perceptions of Pakistani students

Purpose – Academic dishonesty has been a matter of great concern in higher education for last few decades. The dishonest behavior of students at graduate and undergraduate level has become a severe issue for education and business sectors, especially when the students exercise same dishonest practices at their jobs. The present research aims to address this matter by investigating the perceptions of students towards academic dishonesty and exploring the security and penalties for dishonest acts of students.Design/methodology/approach – A well‐structured questionnaire was used to collect the data from 958 respondents studying at graduate and undergraduate levels in different Pakistani universities.Findings – It has been found that students involve in academic dishonest acts more frequently about which they believe to be less severe. Moreover, they also suggested lower or no penalties for the same dishonest acts which are perceived as less severe.Practical implications – The results provide a strong implica...

Synthesis, Acetylcholinesterase and Alkaline Phosphatase Inhibition of Some New 1,2,4-Triazole and 1,3,4-Thiadiazole Derivatives

A new series of 4,5-disubstituted-2,4-dihydro-3H-1,2,4-triazole-3-thiones (6a–s) and 2,5-disubstituted-1,3,4-thiadiazoles (7a–h) was synthesized by intramolecular dehydrocyclization of various 1,4-disubstituted thiosemicarbazide derivatives (5a–s) by refluxing in 4 N aqueous sodium hydroxide and by overnight stirring with polyphosphoric acid, respectively. The structures of these compounds were characterized by IR, 1H and 13C NMR, elemental analysis and mass spectroscopic studies. All the synthesized compounds were screened for their acetylcholinesterase and alkaline phosphatase inhibition studies. Most of the tested compounds showed promising activities, amongst them (6k) and (6q) showed excellent acetylcholinesterase inhibitory activity with IC50 0.241 ± 0.012 and 0.260 ± 0.013 µM, respectively, as compared with those of standard drug whereas the compound (6p), with IC50 0.044 ± 0.001 µM, was found to be the most potent inhibitor of alkaline phosphatase.