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.
Activation of farnesoid X receptor (FXR) markedly attenuates development of atherosclerosis in animal models. However, the underlying mechanism is not well elucidated. Here, we show that the FXR agonist, obeticholic acid (OCA), increases fecal cholesterol excretion and macrophage reverse cholesterol transport (RCT) dependent on activation of hepatic FXR. OCA does not increase biliary cholesterol secretion, but inhibits intestinal cholesterol absorption. OCA markedly inhibits hepatic cholesterol 7α‐hydroxylase (
Let P be a right R-module, where R is a ring with identity. In the present research, a class of modules is described similar to H-μ-supplemented and μ-lifting modules. A module P is called principally H-μ-supplemented if there is a summand L of P such that pR is μ-equivalent to L for every p in P. Additionally, we present an extension of supplemented modules. A module P is considered to be principally μ-supplemented if, for every p in P, pR has a μ-supplement in P. A number of characteristics of these modules are shown, and it is demonstrated that both the Pμ-H-supplemented and Pμ-supplemented modules include the class of principally μ-lifting modules.
Marketing is one of the most important pillars on which most industrial and commercial sectors depend on evaluating their performance, improving their financial position, development and economic growth. The presence of effective marketing activities in any industrial or commercial organization (which works to meet the requirements of customers in order to ensure the integration of trading and handling rings with consumers and to ensure the growth of the marketing process regularly and not to retreat) effectively contributes to maintaining the company's position between its competitors and its customers. It is necessary to have these marketing activities in order to meet the requirements of the organization on the one hand and to
... Show MoreOsteoporosis (OP) is a systemic skeletal disorder that is characterized by reduced bone mass and micro-architectural deterioration of bone tissue, with a consequent increase in bone fragility and susceptibility to fracture. The most frequent osteoporotic fractures are fractures of the hip, wrist, and spine. The exact causes of OP are still unknown; several factors contribute to the disorder. Subjects and Methods: This study consists of patient groups, this group (Group A) was composed of 80 postmenopausal women with OP and osteopenia and the patient group was subdivided into two group; First group (GroupA1) was composed of 50 postmenopausal women with OP and the second group (Group A2) composed of (30) Postmenopausal Women with oste
... Show MoreAspirin and clopidogrel are considered the most important oral platelets aggregation inhibitors. So it is widely used for treatment and prophylaxis of cardiovascular and peripheral vascular diseases related to platelets aggregation .In this study aspirin and clopidogrel were formulated together as floating bilayer tablet system. Three different formulas of 75 mg aspirin were prepared by wet granulation method as immediate release layer; different disintegrants used to achieve rapid disintegration. Formula with crosscarmellose as disintegrant achieve rapid disintegration was selected for preparation of bilayer tablet.
Different formulas of 75 mg clopidogrel were prepared as sustained release floating layer by wet granulation (effe
... Show MoreBackground: The present study involved the following parts, the first part is evaluation of the levels of glycated hemoglobin(HbA1c), creatinine, uric acid(UA) and albumin in patients with diabetic nephropathy comparison with the group of healthy as a control group. The second part is the measurement and evaluation of oxidative stress represented in the malondihydehyde(MDA) as a biomarker of oxidative stress as well as the identification of vitamins C and E as an antioxidant in patients with diabetic nephropathy(DN) compared with the healthy group. Objective: The objective of this study is to estimate oxidative stress by calculate malondialdehyd as biomarker and evaluate some vitamins such as vit C and vit E as antioxidants in diabetic neph
... Show MoreIn spite of the contemporary development over the world in pertaining of modernization and its differences about the transformation of the knowledge but, the important instrument to transfer the thoughts and information did not have change except the language. So the evolutionary process became as a torrent or fusillade above the cliff which drifted anything. So that the objective inquiry and impressed with varieties of development the casement to evaluate the linguistic or re - correction highlight article in order to preserve on the origins of the language and its sobriety.
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