Objective: Rosmarinus officinalis L. is an aromatic perennial herb with fragrant evergreen needle-like leaves, and it is member species of Lamiaceae family raised from Mediterranean region. The aims of the study were isolation, quantification, and identification of rosmarinic acid of R. officinalis leaves and essential oil analysis using various chromatographic and spectroscopic methods, and also cytotoxic and antibacterial investigation against different species of bacteria. Methods:It was isolated by preparative HPLC and preparative TLC, and then it was determined by HPTLC. The identification and the structural elucidation of isolated rosmarinic acid were performed by H-nuclear magnetic resonance, electrospray ionization mass spectrometry (MS), infrared, and ultraviolet. Essential oil was analyzed by Gas Chromatography/Mass. Results:Results highlighted that rosmarinic acid content was 0.9% and the oil content was 1.8%, and R. officinalis chemotypes of Iraqi rosemary oil were camphor 23.04%, 1, 8-cineole 14.01%, and terpinen-4-ol 13.8%. The rosemary chemotype characterized as a high concentration of terpinen-4-ol and good inhibition effect of rosemary methanolic extract against different species bacteria: Enterococcus faecalis, Staphylococcus saprophyticus, Acinetobacter baumannii, and Proteus mirabilis. Conclusions:The plant has a good content of rosemary phytochemicals and antibacterial effect, so the plantation of rosemary in Iraq has been successes. These isolated compounds are a suitable candidate for further clinical and pharmacological study.

The free –COOH present in NSAIDs is thought to be responsible for the GI irritation associated with all traditional NSAIDs. Exploitation of mutual prodrugs is an approach wherein the NSAID is covalently bounded to a second pharmacologically active carrier/drug with the ultimate aim of reducing the gastric irritation. In this study some NSAIDs were conjugated with gabapentin via ester bonds using glycol spacers with the expectation of reducing gastric adverse effects and obtaining synergistic analgesic effects. The kinetics of ester hydrolysis were studied in two different non enzymatic buffer solutions at pH 1.2 and 7.4, as well as in 80% human plasma using HPLC with chloroform -methanol as mobile phase. Compounds 9a–c with ethylene glycol spacers showed significant stability at buffer solutions with half lives ranging from about 8–25 h, while the underwent a reasonable plasma hydrolysis (49%–88%) in 2 h. Compound 9d with a propylene glycol spacer shows a higher rate of enzymatic hydrolysis than the corresponding ethylene glycol compound 9c. The result of compounds 9a-c indicate that these compounds may be stable during their passage through the GIT until reaching the blood circulation.

A series of six pyrazoline ring derivatives as a pharmacophore were incorporated to the naproxen; to increase its size were synthesized and preliminarly evaluated as antiinflammatory agents with expected selectivity toward COX-2 enzyme. In vivo acute antiinflammatory effects of the final compounds (5a-f) were evaluated in rats using egg-white induced edema model of inflammation. The tested compounds and the reference drug (naproxen) produced significant reduction of paw edema with respect to the effect of control group (propylene glycol 50%, v:v). However, compound 5d and 5e show comparable effect to naproxen at all experimental time while compounds 5a, 5b and 5c produced significantly lower inhibitory effect than naproxen at time 120-240 minutes. Furthermore, compound 5f exert significantly higher paw edema reduction than naproxen at 60-240 min. Also the antibacterial activities of the final compounds were evaluated by Well Diffusion Method. All tested compounds exert significant antibacterial activity against tested Gram positive and Gram negative bacteria in comparison to dimethyl sulfoxide as control group. In comparison the antibacterial results among the tested compound 5e may regard the best one and compound 5c the lower one.

A series of 4-(methylsulfonyl)aniline derivatives were synthesized in order to obtain new compounds as a potential anti-inflammatory agents with expected selectivity against COX-2 enzyme. In vivo acute anti-inflammatory activity of the final compounds 11–14 was evaluated in rat using an egg-white induced edema model of inflammation in a dose equivalent to 3 mg/Kg of diclofenac sodium. All tested compounds produced significant reduction of paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the activity of compounds 11 and 14 was significantly higher than that of diclofenac sodium (at 3 mg/Kg) in the 120–300 minute time interval, while compound 12 expressed a comparable effect to that of diclofenac sodium in the 60–240 minute time interval time, and compound 13 showed a comparable effect to that of diclofenac sodium at all experimental times. The result of this study indicates that the incorporation of the 4-(methylsulfonyl)aniline pharamacophore into naproxen, indomethacine, diclofenac and mefanamic acid maintained their anti-inflammatory activity and may increase selectivity towards the COX-2 enzyme which will be confirmed in the future by assessing COX-2: COX-1 inhibitory ratios using a whole blood assay.

Background: Undoubtedly, cancer is regarded as a major concern for researchers alongside the whole humanity for its high mortality rates. At this moment, there must be some researchers working hard to design, synthesize, and biologically investigate the effects of some potential candidates to fight back cancer. Materials and methods: In previous unpublished work, the authors successfully designed, synthesized, characterized a potential two spebrutinib analogues. Consequently, these analogues were evaluated with the employment of MCF-7, HCT116, and MDCK cell lines. Results: In respect to the spebrutinib standard, one of these analogues has superior activity against MCF-7 cell line (IC50; 10.744 µg/mL against 13.566 µg/mL for spebrutinib) and an enhanced toxicity profile on MDCK cell line (IC50; 8.653 mg/mL against 4.011 mg/mL for spebrutinib). Conclusion: The two compounds showed good activity against breast and colon cell lines and enhanced toxicity profile against normal kidney cell line in respect to spebrutinib standard.