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Design, Synthesis and Preliminary Pharmacological Evaluation of New Non-Steroidal Anti-Inflammatory Agents Having a 4-(Methylsulfonyl) Aniline Pharmacophore
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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.

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Publication Date
Sun Mar 08 2020
Journal Name
Biochem. Cell. Arch
SYNTHESIS AND SPECTROSCOPIC CHARACTERIZATION OF NEW HETEROCYCLIC COMPOUNDS DERIVATIED FROM 1-(4-AMINOPHENYL) ETHAN-1-ONEOXIME AS A STARTING MATERIAL WITH EVALUATE THEIR BIOLOGICAL ACTIVITY
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ABSTRACT : This research involves the synthesis of five to seven heterocyclic compounds starting with Schiff’s bases which derived from oxime as a starting material. 1.3-oxazepine derivatives were prepared from adding different anhydrides to the Schiff bases, tetrazole and thiazolidinone derivatives synthesized from add sodium azide and thioglycolic acid to the same Schiff’s bases as a five members ring. Pyrimidine derivatives were prepared after the reaction of the azomethine group with acetyl chloride and then urea and thiourea to synthesis on derivatives contain the six members ring. Another step included identified and confirmed these compounds by FT- IR, 1HNMR, TLC and 13CNMR finally, step included the assay of biological activity

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Publication Date
Thu May 10 2018
Journal Name
Global Journal Of Health Science; Issn 1916-9736 E-issn 1916-9744
Effects of Biological and Non Biological Agents (Disease Modifying Antirheumatic Drugs) on Bone Mineral Density in a Sample of Rheumatoid Arthritis Patients
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Background: Osteoporosis is an extra-articular complication of rheumatoid arthritis that results in increased risk of fractures and associated morbidity, mortality, and healthcare costs. Objective: To evaluate changes in bone mineral density in a sample of rheumatoid arthritis (RA) patients on biological (anti tumor necrosis factor (TNF) alpha) and non-biological agent disease modifying antirheumatic drugs (DMARDs). Patients and Methods: A cross sectional study enrolled 60 RA patients diagnosed by rheumatologist according to the 2010 American College of Rheumatology/European League Against Rheumatism (2010 ACR/EULAR) classification criteria for RA. Thirty patient on biological agent (anti TNF alpha) and 30 patient on non-biological agent (D

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Publication Date
Tue Jun 25 2024
Journal Name
Biomedical And Pharmacology Journal
Psidium guajava: A Review on Its Pharmacological and Phytochemical Constituents
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Psidium guajava, belonging to the Myrtaceae family, thrives in tropical and subtropical regions worldwide. This important tropical fruit finds widespread cultivation in countries like India, Indonesia, Syria, Pakistan, Bangladesh, and South America. Throughout its various parts, including fruits, leaves, and barks, guava boasts a rich reservoir of bioactive compounds that have been traditionally utilized as folkloric herbal medicines, offering numerous therapeutic applications. Within guava, an extensive array of Various compounds with antioxidative properties and phytochemical constituents are present, including essential oils, polysaccharides, minerals, vitamins, enzymes, triterpenoids, alkaloids, steroids, glycosides, tannins, fl

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Publication Date
Tue Mar 28 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Preliminary Antimicrobial Study of 2-Amino-5-Mercapto-1,3,4-Thiadiazole Derivatives
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Nitrogen heterocycles are of a special interest because they constitute an important class of natural and non natural products, many of which exhibit useful biological activities.Among these nitrogen heterocycles are 1, 3, 4-thiadiazole containing compounds. The therapeutic effects of these derivatives have been well studied for a number of pathological conditions including inflammation, pain, or hypertension. Moreover, synthesis of thiadiazoles has attracted wide-spread attention due to their diverse applications as antibacterial, anticancer, antifungal anti-inflammatory and antidepressant agents.According to this information’s new derivatives of 1, 3, 4-thiadiazole were designed and synthesized and in the hope of having some act

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Publication Date
Tue Mar 28 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Dose Dependent Anti-inflammatory Effect of Ammi majus Alcoholic Extract in Rat: Chronic Study
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During treatment of inflammatory diseases, many conventional therapies (non-steroidal anti-inflammatory drugs) used to relief pain and inflammation. Chronic use of  the intended drugs is frequently associated with serious side effect, which may lead to discontinuation of treatment . The efficacy and dose- response effect of ammi majus extraxt  (2 , 4, 8 , 16, and 32 mg/rat) were assessed using  formalin to induce paw edema in rats as a model of chronic inflammation respectively. In this study,  42 rats were used and allocated into 7  groups each containing 6 rats, representing control (Distilled  water) , standard (piroxicam ) and test extract ( 2 , 4 , 8 , 16 and 32 mg/rat of Ammi majus alcoholic e

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Publication Date
Sat Dec 21 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization and Preliminary Anticancer Study of Novel 5-fluorouracil Conjugate with Pyrrolidine Dithiocarbamate as a Mutual Anticancer Prodrug
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 5-Fluorouracil is one of the commonly used chemotherapy drugs in anticancer therapy; unfortunately treatment with 5-FU by solely has many drawbacks  low lipophilicity, low permeability, low molecular weight, and its relatively poor plasma protein binding; also a brief half-life therefore frequent administration is required to maintain the optimal therapeutic plasma level which in addition to its poor selectivity, drug resistance and limited penetration to cancer cells; leads to increased incidence of side-effects to healthy cells/tissues and low response rates. In order to minimize these drawbacks; 5-FU was chemically  conjugated with pyrrolidine dithiocarbamate (PDTC) in a mutual prodrug moiety (S-(9H-purin-6-yl) 3-(

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Publication Date
Wed Jan 01 2020
Journal Name
Iop Conference Series: Materials Science And Engineering
Synthesis of anti-corrosion polymers from thiadiazole
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Abstract<p>One of the biggest problems facing many industries particularly oil, is the problem of corrosion, where the metal parts under the influence of the vital factors are eroded during use and storage, therefore, to lift the metal’s ability and to protect it against corrosion, corrosion inhibitors are used. For the first time in this research, polymers which contain sulfur - heterocyclic ring with a thiadiazole base were made. Anti- corrosion polymers were made on two stages, in the first stage, thiadiazole was made from hydrazine hydrate reaction to carbon disulfide, afterwards the first product was reacted with an excess of hydrazine. In the second stage, polymers were prepared by the r</p> ... Show More
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Publication Date
Sat Jun 18 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Some Pro and Anti-Inflammatory Cytokines in Children with Tonsillitis and their Correlations with Vitamin D Deficiency
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Inflammation of the tonsils could be described as acute tonsillitis, mainly due to infection. Recurrent tonsillitis could be defined as 3-7 episodes during the first 3 years of age. Vitamin D, which is a neuro-hormone with pleiotropic biological activities may modulate the immune response by alleviation, and stimulation of Th1 and Th2 cell proliferation, respectively, that influence the stimulation, synthesis, and secretion of both pro and anti-inflammatory cytokines. In this study we aimed to shed light on the levels of vitamin D in children with different episodes of tonsillitis in association with levels of interleukins (TNFα, IL-2, IL-4, IL-10). Blood samples were collected from 48 participants in 3 groups: control, acute tonsilliti

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Publication Date
Thu Dec 28 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
Synthesis, Characterization and Biological Evaluation of New Dithiocarbamate Ligand and Its Complexes with some Metal Ions
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New bidentate dithiocarbamate ligand (NaL) namely [Sodium-2-(((3-methyl -4- “(2,2,2-tri fluoro ethoxy) pyridin-2”-yl) methyl) sulfinyl)-1H-benzoimidazole -1-carbodithioate] was prepared. This free ligand was synthesized from the reaction of a (RS)-2-([3-methyl -4-(2,2,2-tri fluoroethoxy) pyridin-2-yl] methyl sulfinyl)-1H benzoimidazole, CS2 and NaOH in methanol as solvent. From reaction of dithiocarbamate salt (NaL) with metal ions (M); Co(II), Ni(II), Cu(II), Zn(II), Cd(II) and Pd(II)”, have obtained the DTC complexes at general molecular formula [M(L)2(H2O)2] and [Pd(L)2]. To characterize the ligand and its complexes, used different analyses methods such FTIR, UV-Vis, elemental microanalysis, atomic absoreption, magnetic susceptibil

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Publication Date
Wed Mar 25 2020
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization and Antimicrobial Evaluation of New Azo Compounds Derived from Sulfonamides and Isatin Schiff Base
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The present study deals with the synthesis of four different azo-azomethine derivatives; this is done by two steps; the first step is diazotization of sulfonamides (sulfanilamide, sulfacetamide, sulfamethoxazole, and sulfadiazine) separately, followed by the second step; the coupling reaction of diazotized compounds with isatin bis-Schiff base named 3-((4-nitrobenzylidene) hydrazono)indolin-2-one. The later one (bis-Schiff base) was synthesized by the reaction of 3-hydrazono-indolin-2-one with p-nitrobenzaldehyde. The chemical structures of newly synthesized compounds were approved on the basis of their FTIR, 1H-NMR, and CHNS elemental analysis data results. The synthesized azo compounds were tested in vitro for their antimicrobial potentia

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