Zafar Saied Saify

Characterisation of Plasmodium falciparum aspartic protease inhibition by piperidine derivatives

Piperidine derivatives are reported to exhibit a variety of pharmacological activities. In this article, synthesis and aspartic protease inhibitory activity of three nitrophenacyl derivatives of N-methyl-4-hydroxy piperidine are reported. Enzyme assays showed that the attachment of a nitro group in the benzene ring plays an important role in the inhibition of plasmepsin-II of Plasmodium falciparum. The compound 1-methyl-1-(4’-nitrophenacyl)-4-hydroxypiperidinium bromide (3), consisting of a nitro group at the para position, was the most active at the concentration of 1.0 µM. The activity of the compounds was evaluated through the observed orientation and diagrammatic representation of nitrophenacyl derivatives of 4-hydroxy piperidine.

(1H-Pyrrolo [2,3-B] Pyridine) 7-Azaindole as Cholinesterase/ Glycation Inhibitors.

As a part of our program to discover novel analoges of (1H-pyrrolo [2,3-b] pyridine) 7azaindole having useful biological activities, a variety of 7-azaindole analogs 1-9 with variable substituents on phenyl ring of phenacyl moiety were synthesized and evaluated for their AChE, BChE and antiglycation Inhibitory potential. Compounds 2-5 were found to Original Research Article International Journal of Biochemistry Research & Review, 4(6): 624-643, 2014 625 be AChE inhibitors with IC50 1.34 μM, 11.60 μM, 0.96 μM and 0.97 μM respectively, while compounds 2-5 were also found to be BChE inhibitors with IC50 1.25 μM, 3.93 μM, IC50 9.18μM and 10.20μM respectively. Compounds 2 (IC50 = 1.25±0.019uM) and 3 (IC50 = 3.93±0.36uM), showed potent BChE inhibitory potential than standard Galantamine (IC50 = 8.51±0.02uM). Besides this, compounds 2-9 were evaluated for glycation inhibition activity. Compound 5 (IC50 values 120.6+0.2uM) showed potent antiglycation potential than standard rutin (IC50=294.50+1.5uM). The size of the substituent, electron donating or withdrawing effect of substituents as well as the position of substituent on phenyl effects the activity.

Synthesis, Pharmacological Evaluation and In-Silico Studies of SomePiperidine Derivatives as Potent Analgesic Agents

In present study, some 4-piperidinopiperidine (PP) and 4-amino methylpiperidine (AMP) derivatives (PP1-3 and AMP4-9) have been synthesized to explore their analgesic potential. Activity of compounds evaluated by in-vivo thermal (tail immersion) method produced significant analgesia at different doses. Docking results explained good binding affinity of synthesized derivatives and potential interaction of all compounds with mu-opioid receptor. The pharmacophoric model of synthesized compounds showed possible structural features required for analgesic activity when compared with standards (Fentanyl, Morphine, Pethidine). Among all PP1, AMP5 and AMP6 emerged out as potent analgesic agents. Graphical abstract

Assessment of Knowledge and Practice on Consumption of Expired Pharmaceuticals: A Cross-Sectional Study at Karachi, Pakistan

Kiran Rafiq, Muhammad Bilal Azmi, Zafar Saied Saify, Waqasuddin Khan, Irfan Ashraf , Najia Rahim, Greesh Kumar, Naureen Baloch Jinnah Sindh Medical University, Karachi, Pakistan. Quality Enhancement Cell, Dow University of Health Sciences, Karachi, Pakistan. H.E.J. Research Institute of Chemistry, International Centre for Chemical & Biological Sciences, University of Karachi, Karachi Pakistan. Jamil-ur-Rahman Center for Genome Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan. 5 Dow College of Pharmacy, Dow University of Health Sciences, Karachi, Pakistan.