Since its discovery in December 2019, corona virus was outbreak worldwide with very rapid rate, so it described by WHO as pandemic. It associated with severe acute respiratory distress syndrome, and can enter to cells through Angiotensin Converting Enzyme 2 (ACE 2) receptor which play an important role as regulator for blood pressure. Hypertension is a potential risk factor for sever acute respiratory syndrome COVID-19, and associated with high mortality rate as shown in many epidemiological studies. Moreover, specific antihypertensive medications that infected patients were receiving are not known; only data about renin-angiotensin-aldosterone system (RAAS) are available.

Objective: The objective of this search was to synthesize a new naproxen analogues having a 1,2,4-triazole-3-thiol heterocyclic ring, and preliminary pharmacological assessment of the anti-inflammatory activity of the synthesized compounds. Methods:The synthesis of naproxen analogues that having 1,2,4-triazole-3-thiol heterocyclic ring occur through esterification of naproxen, and then its reaction with hydrazine hydrate, and carbon disulfide, finally different aromatic aldehydes reacted with triazole derivatives of naproxen containing amino group to produce schiff bases. Results:In vivo acute anti-inflammatory activity of the synthesize compounds (Va-Vd) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (50 mg/kg) of naproxen. All tested compounds were produced a significant reduction in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Compound Vd produced superior anti-inflammatory activity compared to naproxen. Conclusion:The results obtained in this work give evidence about the valid synthesis of 1,2,4 triazole-3-thiol derivatives of naproxen, which reacted with different aldehydes to yield several schiff bases. The incorporation of benzaldehyde possess para-electron donating group (parahydroxyl benzaldehyde) will increase the anti-inflammatory activity of naproxen.

A group of amine derivatives [4-aminobenzenesulfonamide derivatives, 2-aminopyridine and 2-aminothiazole] incorporated to α-carbon of diclofenac a well known non-steroidal anti-inflammatory drug (NSAID) to increase bulkiness were designed and synthesized for evaluation as  a potential anti-inflammatory agents with expected COX-2 selectivity. In vivo acute anti-inflammatory activity of the selected final compounds (9, 12 and 13) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (3 mg/Kg) of diclofenac sodium. All tested compounds  produced a significant reduction  in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the 4-aminobenzenesulfonamide derivative (compound 9) exhibited superior anti-inflammatory activity compared to diclofenac sodium at times 180-300 minutes with the same onset of action. The results of this study indicate that the incorporation of the selected aromatic amino groups in to diclofenac maintain its anti-inflammatory activity.                                                                                                                              Key words: amine derivatives, anti-inflammatory, diclofenac derivatives, COX-2 selectivity.

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The Objective of this study is created a   novel derivative of the naproxen with the heterocyclic (1,2 and 4 the triazole) ring that reacted with benzoyl chloride derivatives, as well as preliminary antibacterial activity testing of the formed products. The derivatives are synthesized by esterifying naproxen hydrazine hydrate, then reacting with hydrated hydrazine and carbon disulfide, and finally reaction the benzoyl chloride derivatives (in the final step) with the triazole the derivatives of the naproxen including of amino group via a nucleophilic substitution reaction. In addition to naproxen, the antibacterial properties of the novel compounds (Va-Vd) were evaluated in agar at known doses (IN vivo). The antibacterial action of the compounds Va and Vd against staph was demonstrated in the topmost inhibited zone. In the case of E. coli, compound Vb has the smallest inhibitory zone. The findings of this study have implications to produce naproxen 1,2 and 4 the triazole-three-thiol derivatives, which reacted including the variety of benzoyl chloride derivatives. The potential of naproxen will be affected by the attraction of benzoyl chloride derivatives with para-groups on the benzen ring.

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Series of gatifloxacin derivatives (IVa-IVd) were synthesized by incorporation of thiazole ring (Which has antibacterial activity) and some of its derivatives into a secondary amine of piperazine ring at C-7 position of gatifloxacin nucleus, in order to increase bulkiness at this position by that reduce the affinity toward the efflux pump of bacterial cells, leading to reduction in bacterial resistance. By using FT-IR spectroscopy, 1H-NMR spectral and some of the physicochemical properties, the synthesized compounds were confirmed and characterized for their chemical structures. In-vitro study was performed to evaluate the antibacterial effect of all synthesized compounds and was revaluated by using agar- well diffusion method (AWD). The antibacterial study was shown a topmost inhibition zone for the compounds IVa and IVb against Staphylococcus aureus and the lowest inhibition zone for the two compounds IVc and IVd against E. coli. In silico study was performed using Molecular Operating Environment program and showed that all synthesized compounds were give affinity toward topoisomerase enzyme and these studies were compatible with the in vitro studies, as the compound IVb give the highest S score value.