A series of 1,2,4-triazole scaffold containing alkoxy moiety 4a-b and 9a-e was synthesized by stirring compounds 3a-b or 8a-d at room temperature with different acid chlorides including 4-methoxy benzoyl chloride or 3,4,5-trimethoxybenzoyl chloride. The structure of the prepared compounds was confirmed using different spectroscopic techniques such as IR, 1 H NMR, 13 C NMR, Mass spectra and high resolution mass or elemental analysis. The synthesized compounds examined for their antioxidant activity using DPPH radical scavenging activity. Results indicated that most of the tested compounds exhibited moderate antioxidant activity. Compound 9b exhibited remarkable antioxidant activity with DPPH radical scavenging rate of 49.4 % compared to trolox as a reference antioxidant agent at 10µM concentration.
The design and development of potent HIV protease inhibitors remain an attractive target for antiviral therapy. A novel class of HIV protease inhibitors containing allophenylnorstatine [Apns; (2S,3S)-3-amino-2-hydroxy-4-phenylbutyric acid] as a transition state mimic have been reported. In this work we fixed P 2` (as tert-butylamino or 2-methylbenzylamino) and changed P 2 moiety to provide two series of dipeptide analogs. Preliminary evaluation of the activity of the synthesized derivatives were determined as percentage of enzyme inhibition at 5 M level. The results showed that the introduction of 2-methylbenzylamino moiety as P 2` ligand 6a-e considerably improved HIV inhibitory activity in comparison with the tert-butyl amino analogs 5a-e. It was found that compounds in both series retained activity still less than the lead compounds KNI-577 and KNI-727.
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