Mefenamic acid (MA) is one of the non-steroidal anti-inflammatory drugs, it is widely used probably due to having both anti-inflammatory and analgesic activity, the main side effects of mefenamic acid include gastrointestinal tract (GIT) disturbance mainly diarrhea, peptic ulceration, and gastric bleeding. The analgesic effects of NSAIDs are probably linked to COX-2 inhibition, while COX-1 inhibition is the major cause of this classic adverse effects. Introduction of thiazolidinone may lead to the increase in the bulkiness leads to the preferential inhibition of COX-2 rather than COX-1 enzyme. The study aimed to synthesize derivatives of mefenamic acid with more potency and to decrease the drug's potential side effects, new series of 4-thiazolidinone derivatives of mefenamic acid were synthesized IVa-g. The synthetic procedures for target compounds and their intermediates are designed to be as follows: acylation of secondary amine of mefenamic acid by chloroacetylchloride to produce compound (I), then reaction between compound (I) and hydrazine hydrate to form hydrazine derivative of mefenamic acid (compound II). After that, Schiff base formation by addition of seven benzaldehyde derivatives and finally, cyclization in presence of thioglycolic acid to form 4-thiazolidinone heterocyclic ring. The characterization of the titled compounds has been established on the basis of their spectral FTIR, 1HNMR data, and by measurements of their physical properties. In vivo acute anti-inflammatory effect of the synthesized compounds was evaluated in rats using egg-white induced edema model of inflammation. The tested compounds and the reference drug produced significant reduction of paw edema with respect to the effect of dimethyl sulfoxide 10%v/v (control group). Compound IVe showed more potent effect than mefenamic acid at 240-300 min, while at time 300 min, compounds IVa and IVd exhibit more potent anti-inflammatory effect than mefenamic acid (50mg/kg, i.p.) as they reduced paw edema significantly more than mefenamic acid at mentioned intervals (p<0.05) . On the other hand compound IVc exhibited lower anti-inflammatory effect.
60 patients diagnosed as having urticaria were included in the study ; 30 patients were effected with acute urticaria and 30 patients were affected with chronic urticaria. In addition, 30 healthy adult volunteers were selected as control group .The patients and control groups sera were examined with enzyme linked immunosorbent assay ( ELISA) to detect total level IgE and radial immunodiffusion (RID) to detect levels of IgG , IgA and IgM . The total level of IgE in acute urticaria ( 1.45±0.13) IU/mL and chronic urticaria (2.12 ± 0.10) IU/mL patients were significantly higher than the control groups ( 0.85 ± 0.10)IU/mL (p<0.05). The level of IgG in acute urticaria ( 12.5± 0.42) g/L and chronic (13.16±0.40) g/L patients , IgA in acute (2.
... Show MoreThe purpose of this research work is to synthesize conjugates of some NSAIDs with sulfamethoxazole as possible mutual prodrugs to overcome the local gastric irritation of NSAID with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo group that undergo reduction only by colonic bacterial azo reductaze enzyme to liberate the parent compound to act locally (treatment of inflammation and infections in colon)
The purpose of this research work is to synthesize conjugates of some NSAIDs with sulfamethoxazole as possible mutual prodrugs to overcome the local gastric irritation of NSAID with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo group that undergo reduction only by colonic bacterial azo reductaze enzyme to liberate the parent compound to act locally (treatment of inflammation and infections in colon).
Key words: Mutual prodrug, Ester linkage, Azo bond, Colon targeting
Background: Acute radiodermatitis is a common side effect during and after radiotherapy course in breast cancer patients treated by radiotherapy. This study assess the frequency of acute radiodermatitis and record the predictive factors for acute radiodermatitis. Patients and Methods: A descriptive case series study conducted at Baghdad, Iraq from August 2020 to September 2021. 70 female scheduled for radiotherapy sessions enrolled in this study. sociodemographic data were recorded and Skin examination before radiotherapy and weekly till the end of the radiotherapy sessions was done to report the frequency, risk factors, clinical picture and grades of acute radiodermatitis based on The National Cancer Institute’s Common Terminology Crite
... Show MoreBackground Radiotherapy is one of the main modalities in the management of cancer along with chemotherapy and surgery. Despite its great benefit it has many side effects on many systems and organs including the skin. Objective To record the frequency, grades and types of acute cutaneous side effect in patients with pelvic tumors treated with radiotherapy, in order to report the risk factors and to find appropriate strategies for prevention and management. Patient and methods. Methods A prospective observational study was carried out in Baghdad Radiation and Nuclear Medicine Centre between August 2020 and August 2021.A total 70 patients were enrolled in this study.All patients had full history and full baseline skin exam and were ass
... Show MoreAcute decompensated heart failure (ADHF) is a leading cause of hospital admission and many factors are known to precipitate decompensation. We aimed to assess the decompensating factors of heart failure and the management of patients admitted to the emergency department (ED). A total of 107 patients were examined, all diagnosed with ADHF in the ED of the Baghdad Teaching Hospital, from June 2017 to December 2017, and presenting with decom¬pensation (pulmonary oedema, peripheral oedema, and fatigue). The mean patient age was 62.5 ± 9.8 years (range: 43–85 years); the majority of them were in their 7th decade (37.4%), and men were slightly more than women. Hy¬pertension was the most commonly associated comorbidity (68.2%), follow
... Show MoreThe studies on the antiviral compound chalcone in vitro in both tissue and organ culture systems against rubella virus glass that this compound relatively non toxic to the cell culture and organ culture of the concentration of 8 ug/ml or less, chalcone have significantly antiviral activity against rubella virus in tissue culture and organ culture. We find that a concentration of 0.03ug/ml or more inhibit the IOOTCID50 of rubella virus. The therapeutic index (TI) used in this study to evaluate the drug, the (TI) which is the ratio of the dose of drug which is just toxic (Maximum tolerated dose) to the dose which is just effective (Minimum effective dose). If this index is one or less it not possible to use the drug under the conditions outli
... Show MoreThe recent emergence of sophisticated Large Language Models (LLMs) such as GPT-4, Bard, and Bing has revolutionized the domain of scientific inquiry, particularly in the realm of large pre-trained vision-language models. This pivotal transformation is driving new frontiers in various fields, including image processing and digital media verification. In the heart of this evolution, our research focuses on the rapidly growing area of image authenticity verification, a field gaining immense relevance in the digital era. The study is specifically geared towards addressing the emerging challenge of distinguishing between authentic images and deep fakes – a task that has become critically important in a world increasingly reliant on digital med
... Show MoreIn the present study, a novel ligand (L) made of 2-hydroxynaphthaldehyde and 3-hydrazone-1,3-dihydro-indole-2-one(3-[(3-hydroxynaphthalen-2-yl-ethylidene)-hydrazono]-1,3-dihydro-indol-2-one). The ligand was characterized by FTIR, UV-vis, mass, 1H-NMR, 13C-NMR, and CHN elemental analysis. New complexes of this ligand were created by treating methanol and a drop of DMF solution of the produced ligand with the hydrated metal salts of Mn(II), Co(II), Ni(II), Cu(II), and Zn(II) in a molar ratio of 2:1 (L:M). As a result, complexes have been emerged and identified FTIR, UV-vis, C.H.N., chloride-containing, molar conductance, magnetic susceptibility, and atomic absorption. The characterization result for each complex indicated complexes wi
... Show MoreAll the prepared metal complexes of Pt (IV), Au(III), Rh (III), Co (II) and V(IV) with new ligand sodium [5-(p-nitro phenyl)-/4-phenyl-1,2,4-triazole-3-dithiocarbamato hydrazide] (TRZ.DTC) have been synthesized and characterized in solid state by using flame atomic absorption, elemental analysis C.H.N.S, FT-IR ,UV-Vis Spectroscopy, conductivity and magnetic susceptibility measurements. The nature of the complexes formed in ethanolic solution has been studied following the molar ratio method also was studied stability constant and found to be stable in molar ratio1:1 of VL (IV) and CoL(II) while Pt(IV), Au(III) and Rh(III) complexes stable in molar ratio 1:2 as well as the molar absorptivity for these complexes were calculated. From the prev
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