Non-steroidal anti-inflammatory drugs (NSAIDs) contain free –COOH which thought to be responsible for the GI irritation associated with all traditional NSAIDs. The esterification of this group is one of an approach to ultimate aim for reduce the gastric irritation; so in this study we synthesized and preliminarily evaluated new ester compounds as new analogues with expected selectivity toward COX-2 enzyme. Synthetic procedures have been successfully developed for the generation of the target compounds (III a and b). The synthetic approach involved multi-steps procedures which include: Synthesis of 4-hydroxy benzene sulphonamide ( I b ), synthesis of Naproxen and Ibuprofen acyl chloride and then reacting them with 4-hydroxy benzene sulphonamide to form final compounds ( III a-b) .The structures of these compounds were identified and characterized using (TLC), infrared spectroscopy (FT-IR), 1H NMR data and microanalysis (CHN).Pharmacological study as anti-inflammatory activities for the final compounds were studied in rats by induced edema type of inflammation. Moreover, the results of a docking study of compounds III a-b into the COX-2 binding site revealed that its mechanism was possibly similar to that of naproxen, a COX-2 inhibitor. The effect of them on COX-2 antibody was showed it could significantly inhibit COX-2 activity.
This study describes the preparation of tetradentate Schiff base derived from the condensation of 2-Hydroxy naphthaldehyde with 2-amine benzhydrazide and the synthesis of new complexes series with a good yield.The prepared ligand was characterized using a microanalysis technique, UV-visible, FT-IR, nuclear magnetic resonance 1H-NMR, mass spectrometry, thermal gravimetric analysis TGA, and the addition of conductivity measurement and magnetic moment of complexes. The invitro antimicrobial activity of the prepared compounds was tested against Gram-negative Klebsiella pneumonia, Gram-positive Staphylococcus aureu, and Candida albicans by the agar well diffusion method. The spectroscopy and measurement studies showed that the li
... Show MoreThe research presented the experience of creating a new sustainable city, and this experience of establishing an Eco-City (Environmentally friendly) is considered the first experience in Iraq. The current study stressed the importance of the need for environmental planning in the early stages of planning new cities based on realism in planning, design and implementation. Subsequently, that aims to preserve the ecosystem, which is difficult to compensate if degraded or polluted. The research incorporated environmental planning indicators within sustainable urban planning (Reliance on generating electric power that is based on clean and renewable energy sources, Availability of public t
Trichomonas vaginalis is a unicellular flagellated protozoan that resides in female and male genital tract and considered the most prevalent sexually transmitted infectious parasite. The infection rate is relatively equivalent between male and female but trichomoniasis is usually asymptomatic in men. Primary triggering of host inflammatory response to this parasite is not fully understood and most studies address the local reaction of the parasite in female genital tract. In this study, two pro-inflammatory cytokines, IL-8 and IL-12, were investigated in the serum of infected women with Trichomonas vaginalis during acute and chronic stages of the disease. The results demonstrated that the level of IL-8 was significantly
... Show MoreIn this paper, we proposed a modified Hestenes-Stiefel (HS) conjugate
gradient method. This achieves a high order accuracy in approximating the second
order curvature information of the objective function by utilizing the modified
secant condition which is proposed by Babaie-Kafaki [1], also we derive a nonquadratic
conjugate gradient model. The important property of the suggestion
method that is satisfy the descent property and global convergence independent of
the accuracy of the line search. In addition, we prove the global convergence under
some suitable conditions, and we reported the numerical results under these
conditions.
The locus of enterocyte effacement LEE-encoded regulator (Ler( is a global regulator of multiple virulence genes expression in the Enteropathogenic Escherichia coli (EPEC), including those encoding the type III secretion pathway and adhesion proteins such as intimin. Ler is central to the process of the formation of the attaching and effacing (AE) lesions. This study aimed to perform the molecular detection of Ler gene in EPEC, since there is no related previous study in Iraq. Two hundred and fifty stool specimens from children under two years of age for both sexes were collected from some Iraqi hospitals. All isolates were diagnosed according to morphological characteristics and biochemical tests. The results showed th
... Show More1,3,4-oxadizole and pyrazole derivatives are very important scaffolds for medicinal chemistry. A literature survey revealed that they possess a wide spectrum of biological activities including anti-inflammatory and antitumor effects.
To describe the synthesis and evaluation of two classes of new niflumic acid (NF) derivatives, the 1,3,4-oxadizole derivatives (compounds 3 and (4A-E) and pyrazole derivatives (compounds 5 and 6), as EGFR tyrosine kinase inhibitors in silico and in vitro.
The designed compounds were synthesized using convent
Coronary artery disease (CAD) is a major health concern and leading of death in individuals with type 2 diabetes mellitus (T2DM). Glutathione S – Transferase(GST) are known for their broad range of detoxification and in the metabolism of xenobiotics . The role of functional variants of these genes in the development of various disorder is proven. We investigated the possible role of these variants in the development of CAD in T2DM patients. In this case – control study a total of 60 patients (T2DM = 30 ; T2DM – CAD = 30) and 30 controls were included. Serum lipid profiles were measured and DNA was extracted from the blood samples. Multiplex PCR for GSTT1/M1 (present / null) polymorphism, were performed for genotyping of study pa
... Show MoreThe removal of Ibuprofen antibiotics (IBU) by photo-degradation UV/H2O2/Fe+2 system was investigated in a batch reactor under different initial concentrations of H2O2 (100-500) mg/L, Fe+2 (10-40) mg/L, pH (3-9) and initial concentrations of IBU (10-80) mg/L, and their relationship with the degradation efficiency were studied. The result demonstrated that the maximum elimination of IBU was 85.54% achieved at 300 mg/L of H2O2, 30 mg/L of Fe+2, pH=3, and irradiation time of 150 min, for 10 mg/L of IBU. The results have shown that the oxidation reagent H2O2 plays a very important role in IBU degradation.
Synthesis and preliminary biological evaluation of imidazo (2, 1-b) Thiazole derivatives is reported. Under Mannich conditions, a series of new imidazo (2, 1-b) Thiazole derivatives were synthesized. Starting from the reaction of 2- amino thiazole with 4- bromo phenyl bromide to produce 5-(4-bromo phenyl) imidazo (2, 1-b) thiazoles, following by introduce the substituted aminomethyl at position 6-by reacting with different aromatic amines under Mannich conditions to afford 6-secondary amine-5-(4-bromo phenyl) imidazo (2,1-b) thiazole in high yields.
FT-IR, 1H NMR, and 13C NMR techniques were used to characterize the synthesized derivatives. In addition, all compounds were tested for their antioxidant activity, and thr
... Show MoreIn this research , phthallic anhydride ring is opened with 4-methyl aniline and acetone as a solvent to results the compound [I] that reacted with dimethyl sulphate and anhydrous sodium carbonate formation to phathalate ester [II], while the acid hydrazide compound [III], was obtained from mixed the compound [II]with hydrazine hydrate, Synthesis four type of shiff bases[IV]a-d was synthesized from the reaction of acid hydrazide [III] with aromatic aldehyde or ketone , when reacted Shiff bases with phthalic anhydride or naphthalicanhydride,I get eight derivatives of oxazepine [V]a-d , [VI]a-d. The bacterial activity of the new compounds studied by four species of bacteria: Esherichia Coli, Enterobactecloacae (Gram negative) and staphylococcu
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