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Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry

Evgeniya A Beskhmelnitsyna, Mikhail V Pokrovskii, Aleksandr L Kulikov, Anna A Peresypkina, Evgeniy I Varavin
INTRODUCTION: Nowadays, the group of NSAIDs is used the most widely in order to treat the inflammatory process. But its long-term administration increases the risk of complications of pharmacotherapy. Therefore, today it is urgent to search for new molecules that can selectively block biological targets that directly perceive inflammatory mediators. One of such targets is TRPA1. ZC02-0012, a compound from the group of substituted pyrazinopyrimidinones, which is a selective inhibitor of TRPA1 ion channel...
February 8, 2019: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Altug Kucukgul, Mehmet Mustafa Isgor, Vesile Duzguner, Azime Kucukgul, Meryem Nur Atabay
BACKGROUND: Persistent oxidative stress can lead to chronic inflammation and mediate most chronic diseases including neurological disorders. Oleuropein has been shown to be a potent antioxidant molecule in olive oil leaf having antioxidative properties. OBJECTIVE: The aim of this study was to investigate the protective effects of oleuropein against oxidative stress in human glioblastoma cells. METHOD: Human glioblastoma cells (U87) were pretreated with oleuropein (OP) essential oil 10 µM...
February 1, 2019: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Marcelo Rodrigues BacciI, Lívia Silva Svrzutt CabralI, Glaucia Luciano da VeigaI, Beatriz da Costa Aguiar AlvesI, Neif MuradI Fernando Luiz Affonso Fonseca
INTRODUCTION: Hemodialysis stands out as an eligible treatment for patients with chronic kidney disease. The subsequent inflammatory process resulting from this disease and hemodialysis per se is exacerbated in this therapy. Selenium (Se) is an essential trace element that can participate in the inhibition of pro-oxidant and pro-inflammatory processes and could be considered a measurement that indicates the progression of chronic kidney disease and inflammation. OBJECTIVES: The present study investigated selenemia in hemodialysis patients of the ABC region of São Paulo and aimed to establish the correlation between an inflammatory marker and selenemia in this conditions disease...
January 21, 2019: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Amaldoss M J Newton, L Prabakaran
OBJECTIVE: Number of various natural polymer-based drug delivery systems targeting the colon is reported for different applications. Most of the research is based on the class of natural polymers such as polysaccharides. This study compares the anti-inflammatory effect of different polysaccharide based tablets on IBD when a drug carrier is targeted to the colon as matrix and coated systems. METHODS: The TNBS induced IBD Wistar rats were used as a model for the study...
January 17, 2019: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Martynenko Yu V, Antypenko O M, Nosulenko I S, Berest G G, Kovalenko S I
BACKGROUND: (Quinazoline-4-ylidene)hydrazides are valued intermediates in modern organic chemistry, they are commonly used for the synthesis of substituted [1,2,4]triazolo[1,5-c]quinazolines. OBJECTIVE: Unknown N-acyl-2-([1,2,4]triazolo[1,5-c]quinazoline-2-yl)-alkyl-(alkaryl-, aryl-)amines were synthesized and evaluated for anti-inflammatory potential. METHOD: The peculiarities of the synthesized compounds structures were studied by IR-, NMR spectroscopy and chromatography-mass spectrometry and were discussed in detail...
January 14, 2019: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Sandi L Navarro, Marta Herrero, Helena Martinez, Yuzheng Zhang, Jon Ladd, Edward Lo, David Shelley, Timothy W Randolph, Johanna W Lampe, Paul D Lampe
BACKGROUND: Non-steroidal anti-inflammatory drugs, e.g., celecoxib, are commonly used for inflammatory conditions, but can be associated with adverse effects. Combined glucosamine hydrochloride plus chondroitin sulfate (GH+CS) are commonly used for joint pain and have no known adverse effects. Evidence from in vitro, animal and human studies suggests that GH+CS have anti-inflammatory activity, among other mechanisms of action. OBJECTIVE: We evaluated the effects of GH+CS versus celecoxib on a panel of 20 serum proteins involved in inflammation and other metabolic pathways...
January 14, 2019: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Abdel Masieh Metry, Issa Al Salmi, Farida Al Balushi, Mohammed Abdalla Yousef, Faisal Al Ismaili, Alan Hola, Suad Hannawi
Systemic lupus erythematosus (SLE) is an autoimmune multisystem inflammatory condition that causes microvascular inflammation with the production of various auto-antibodies that play a major role in its pathogenesis. SLE can affect both sexes, all ages, and all ethnic groups with widespread geographical and socioeconomic backgrounds. Asia encompasses people of many sociocultural backgrounds with diverse ethnic. Due to a lack of national epidemiological research, the incidence and prevalence of SLE in Middle Eastern and Arab countries, have only recently been studied...
November 28, 2018: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Nicola Macchione, Paolo Bernardini, Igor Piacentini, Barbara Mangiarotti, Alberto Del Nero
Chronic prostatitis/chronic pelvic pain syndrome (CP/CPPS) is reported in literature ranging from 1 to 14.2%. The aim of the present study was to assess the impact on patient's quality of life and symptoms of Flower pollen extract in association with vitamins (Deprox 500®) in comparison with Serenoa repens 320 mg (Permixon 320 mg® by Pierre Fabre) in patients with CP/CPPS. All consecutive patients, with a diagnosis of CP/CPPS, referred to our center from January to August 2016, were screened to be enrolled in this single-center, randomized, controlled trial...
November 28, 2018: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Adel Qlayel Alkhedaide
BACKGROUND: Chronic inflammation is a critical health issue and implicated in several chronic health problems such as tumors, auto-immune disorder, hypertension or diabetes. However, Juniperus procera is one of the famous ancient plants that been traditionally used to treat several diseases such as hyperglycemia, hepatitis, jaundice, bronchitis, and pneumonia. OBJECTIVE: Current study is an attempt to investigate the anti-inflammatory effect of juniperus procera extract on rats exposed to cytotoxicity caused experimentally by streptozotocin injections...
November 26, 2018: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Mahmood Ahmad Khan, Rafat Sultana Ahmed, Nilesh Chandra, Vinod Kumar Arora, Athar Ali
Rheumatoid arthritis (RA) is a devastating disease characterized by continual addition of leukocytes and T cells within the articular cavity causing inflammation. Withania somnifera is reported to have antioxidant, anti-inflammatory, immunomodulatory properties. The purpose of this study was to evaluate anti-inflammatory activity of aqueous extract of Withania somnifera roots (WSAq) in collagen induced arthritic (CIA) rats. To achieve this, we assess the level of inflammatory cytokines such as tumor necrosis factor (TNF)-α, IL-1β, IL-6 and IL-10 in CIA rats...
November 15, 2018: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Pierre A Hanna, Mamdouh M Ghorab, Shadeed G Shadeed
Betamethasone dipropionate is a highly effective corticosteroid anti-inflammatory. However, the main drawback of its topical use is the limited skin penetration into deeper skin layers. Also, its systemic use has shown many side effects. The goal of this research was to formulate betamethasone dipropionate in nanostructured lipid carriers (NLC) formulae that contain oleic acid to aid its penetration to deeper skin layers and to aid absorption to local regions upon topical application.NLC formulae were prepared by high shear homogenization then sonication...
November 14, 2018: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Nittaya Chansiw, Kamonnaree Chotinuntakool, Somdet Srichairatanakool
BACKGROUND: Polygonum odoratum is an indigenous vegetable that has been used as a favoring agent and also used as a Thai traditional medicine to treat flatulence. OBJECTIVE: To analyze active ingredients, total phenolic and total flavonoid contents, anti-inflammatory and antioxidant activities from leaf and stem extracts of P. odoratum. METHODS: Leaves and stems were dried and extracted by using methanol, dichloromethane and water for obtaining methanolic leaf extract (MLE), methanolic stem extract (MTE), dichloromethane leaf extract (DLE), dichloromethane stem extract (DTE), water leaf extract (WLE) and water stem extract (WTE)...
November 9, 2018: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Bhushan R Dravyakar, Pramod B Khedekar, Tabassum Khan, Atul P Sherje, Kavit N Patel, Vasanti Suvarna
A novel series of 2-(Morpholin-4-yl)-N-phenylquinazolin-4-amine derivatives were synthesized and confirmed with spectral and elemental techniques. The compounds were tested for analgesic and anti-inflammatory activity by various pain models in rodents whereas the selectivity towards COX-2 receptor is determined by in vitro assay. Screening results of compounds exhibited comparable biological activity with that of standard compound Indomethacin used for study. Compound 5d was found to be significantly potent with respect to its anti-inflammatory and analgesic activity with substantial COX-II selectivity...
October 22, 2018: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Benarous Khedidja, Benguechoua Madjeda, Ghibeche Abderrahmane
BACKGROUND: Inhibition activity of 8 synthetic molecules known as anti-allergy drugs on lipases have been investigated. The enzymatic inhibition produced by these molecules is described here for the first time. OBJECTIVE: The used anti-allergy drugs are: loratidine, primalan, zyrtec, histagan, periactin, ketotifene, rifex and bilastine. METHODS: lipase inhibition is studied using spectrophotometric method. Molecular docking has been achieved for the first time for these drugs using AutoDock Vina program to discuss the nature of interactions, structure activity relationship and the mechanism of inhibition...
September 10, 2018: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Muhammad Saleem, Mamona Nazir, Hidayat Hussain, Muhammad Imran Tousif, Mahmoud F Elsebai, Naheed Riaz, Naseem Akhtar
Serine protease, human neutrophil elastase (HNE), has been shown to be useful in medical science, however, its over production and malfunctioning may produce devastating effects and cause serious damage to the host. Unfortunately, the present approved drug, sivelestat, only alleviates the symptoms of the diseases caused by malfunction of HNE but not the disease progression. Therefore, there is crucial need to search potent and safer molecules as elastase inhibitors and to develop better anti-inflammatory drugs in future...
September 9, 2018: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Priyanka S Chaudhari, Sohan S Chitlange, Rabindra K Nanda
BACKGROUND: A new series of 2-(4-acetyl-3-methyl-5-(arylamino) thiophen-2-yl)-3-arylquinazolin-4(3H)-one derivatives (11a-11j) were synthesized from acetyl acetone, phenyl isothiocyanate and 2-chloromethyl quinazolinone. OBJECTIVE: Due to side effects of Non Steroidal anti-inflammatory drugs (NSAID), an attempt was made to identify novel tetrasubstituted thiophene lead compound as potential anti-inflammatory and antioxidant agent. METHODS: Then newly synthesized compounds were characterized by IR spectroscopy, 1H NMR and mass spectrometry...
September 9, 2018: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Reem Al-Wabli, Mohammad Fouad, Radwan El-Haggar
The promising activity of coumarin derivatives as anti-inflammatory agents has motivated us to synthesize a new series of coumarin derivatives aiming to improve the anti-inflammatory activity and/or bioavailability. In the present work, the reaction between compound III and different aromatic acyl chloride had resulted in a series of ester derivatives 1-9. All synthesized new compounds 1-9 along with compound III as a parent compound and Celecoxib as a reference, were assessed for their anti-inflammatory activity both in-vivo and in-vitro using the formalin-induced hind paw edema method and inhibition of albumin denaturation and red blood cells (RBCs) membrane stabilization, respectively...
August 16, 2018: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
S Holowacz, I Guinobert, A Guilbot, S Hidalgo, J F Bisson
BACKGROUND: There is a growing interest in the effects of probiotics for the prevention and treatment of skin diseases due to their immunomodulatory and anti-inflammatory properties. OBJECTIVE: To assess a mixture of five bacterial strains in the prevention of chronic skin inflammation in mice. METHOD: Hairless SKH-1 mice received daily oral treatment with the probiotic mixture at the dose of 1x109 colony-forming unit (CFU)/day (or vehicle) for three weeks...
August 13, 2018: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
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2018: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Simone Carradori
No abstract text is available yet for this article.
2018: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
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