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Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry

Gianfranco Calogiuri, Lene H Garvey, Paolo Romita, Luigi Macchia, Caterina Foti
Glucocorticoids are the most widely used drugs for the treatment of hypersensitivity, however these drugs themselves and the excipients contained in commercial corticosteroid formulations are able to induce severe immediate-type hypersensitivity reactions. Reactions involving excipients have been confirmed to be IgE mediated by the demonstration of specific-IgE to excipients such as carboxymethylcellulose and lactose. In case of hypersensitivity reactions to corticosteroid preparations, a complete allergy work-up with skin tests and/or challenge tests should include testing excipients as well as the active ingredients...
November 9, 2016: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Rinu K Rana, Rakesh K Patel
BACKGROUND: The involvement of debilitating side effects of allopathic antiasthmatic drugs provides a strong impetus for the development of new herbal therapeutics. Myrica nagi Thunb. (Syn. Kaiphal) of Myricaceae family is a known drug of the Ayurveda system used for the treatment of several diseases including asthma. METHODS: The present study deals with the preparation and phytochemical screening of polar, non-polar and methanolic extracts of Myrica nagi bark followed by the evaluation of their antiasthmatic activity using four different animal experimental models: acetylcholine induced bronchospasm in conscious guinea pigs, acetylcholine induced contraction on isolated guinea pig tracheal chain preparation, compound 48/80 induced mast cell degranulation using rat, and trypsin and egg albumin induced bronchospasm in conscious rat...
September 23, 2016: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Natalia Lucia Rukavina Mikusic, María Inés Rosón, Silvana Lorena Della Penna, Susana Gorzalczany, Elsa Zotta, Marcelo Roberto Choi, Jorge Eduardo Toblli, Belisario Enrique Fernandez
BACKGROUND: Endothelial nitric oxide synthase (eNOS) is known to be expressed in endothelium and smooth muscle cells of arteries. The aim of this study was to investigate the expression of eNOS in intimal and medial layer of aorta from rats fed a high salt diet and its modulation by losartan and tempol. METHODS: Rats were fed during three weeks with: normal salt diet (NS, 0.4% NaCl); high salt diet (HS, 8% NaCl); NS plus tempol 1 mM (NS-T); HS plus tempol (HS-T); NS plus losartan 40mg...
September 22, 2016: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Mayura A Kale, Rajesh Nawale, Manjiri Peharkar, Sharad V Kuberkar
BACKGROUND: Currently used anti-inflammatory drugs are associated with some severe side effects such as gastric irritation, which may range from simple discomfort to ulcer formation. Therefore, the development of potent anti-inflammatory drugs with fewer side effects is important. Benzimidazole, tetrazole and its various derivatives have been used in the synthesis of numerous heterocyclic compounds. In the past few decades, these compounds received much attention due to their diverse array of biological activities...
September 15, 2016: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Tomokazu Ohishi, Shingo Goto, Pervin Monira, Mamoru Isemura, Yoriyuki Nakamura
BACKGROUND: Green tea has been shown to have beneficial effects against a variety of diseases such as cancer, obesity, diabetes, cardiovascular disease, and neurodegenerative diseases. Through cellular, animal, and human experiments, green tea and its major component, epigallocatechin-3-gallate (EGCG) have been demonstrated to have anti-inflammatory effects. Our previous findings have indicated that green tea and EGCG suppress the gene and/or protein expression of inflammatory cytokines and inflammation-related enzymes...
September 15, 2016: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Amj Newton, Jatinder Kumar
BACKGROUND: Although, a number of formulations have been developed for the treatment of IBD yet the developed formulations are having side effects such as high dose, lack of solubility and permeability problems at the site of action. Very few formulations have been developed for the IBD treatment in the form of nanoparticles. Nanoparticles have shown their potential in the recent findings in the treatment of IBD at cellular level. This research work aims to develop nanosuspension of newly introduced drug Rifaximin currently available in the form of tablet for the treatment of IBD...
July 20, 2016: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Elpidio Santillo, Monica Migale, Demetrio Postacchini, Fabrizio Balestrini, Raffaele Antonelli Incalzi
BACKGROUND: At present, ischemic heart disease (IHD) is one of the main causes of morbidity and mortality world-wide. An important insight into both IHD pathophysiology and cardioprotection was achieved in 1986 when Murry et al. described for the first time the ischemic preconditioning (IP). IP can be defined as an innate phenomenon by which brief episodes of ischemia confer protection to a tissue from a subsequent more protracted ischemic insult. Suggested mechanisms explaining IP comprise the action of circulating substances (e...
July 19, 2016: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
S L Khokra, S A Khan, D Chowdhary, S M Hasan, A Ahmad, A Husain
BACKGROUND: Furanone and pyrrolone heterocyclic ring system represent important and interesting classes of bioactive compounds. Medicinal chemists use these heterocycyclic moieties as scaffolds in drug design and discovery. METHODS: A series of 3-arylidene-5-(naphthalene-2-yl)-furan-2(3H)-ones (2a-j) were synthesized by incorporating pharmacophore of COX-2 inhibitor rofecoxib and naphthyl ring of naproxen as potential non steroidal anti-inflammatory agents. These furanone derivatives were subsequently reacted with dry ammonia gas and benzylamine to furnish corresponding 3-arylidene-5-(naphthlen-2-yl)-1H-pyrrol-2(3H)-ones (3a-e) and 3-arylidene-1-benzyl-5-(naphthalene-2-yl)-1H-pyrrol-2(3H)-ones (4a-e), respectively...
June 18, 2016: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Sanjay B Bari, Sandip D Firake
BACKGROUND: The present study reports the synthesis and biological evaluation of thiazolidinone derivatives bearing benzenesulfonamide investigated for cyclooxygenase-2 (COX-2) inhibitory activity and in vivo anti-inflammatory activity. METHODS: The synthesis of 4-(4-oxo-2-substituted-1,3-thiazolidin-3-yl) benzenesulfonamide derivatives were carried out by conventional synthesis, involves the one-pot condensation reaction of sulfanilamide. The synthesized compounds were evaluated against COX-1 and human recombinant COX-2 by using colorimetric enzyme assay kit and in-vivo study was carried out by carageenan induced rat paw edema method...
May 24, 2016: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Waleed A Bayoumi, Mariam A Ghaly, Mohamed E Shaker
A series of N-(4-substituted phenyl)glycine derivatives was designed and synthesized. The starting N-(4-acetylphenyl)glycine was converted into two intermediates: the chalcone analog 2 and the thiosemicarbazone derivative 8. Both 2 and 8 were derivatized and/or cyclized into different heterocyclic target derivatives (3-7 and 9-12). The target compounds were screened for anti-inflammatory activity using carrageenan-induced rat paw edema assay. The results showed that compounds 6, 7, and 3 were the most active compounds at a 50 mg/kg dose level with % inhibition of edema of 51...
May 18, 2016: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Ochoa-Aguilar Abraham, Ventura-Martinez Rosa, Sotomayor-Sobrino Marco Antonio, Gómez-Acevedo Claudia, Morales-Espinosa María Del Rosario
BACKGROUND: Beta-lactam molecules are a family of drugs commonly used for their antibiotic properties; however, recent research has shown that several members of this group present a large number of other effects such as neuroprotective, antioxidant, analgesic or immunomodulatory capabilities. These properties have been used in both preclinical and clinical studies in different diseases such as hypoxic neuronal damage or acute and chronic pain. The present work briefly reviews the antibiotic effect of these molecules, and will then focus specially on the non-antibiotic effects of three beta-lactam subfamilies: penicillins, cephalosporins and beta lactamase inhibitors, each of which have different molecular structure and pharmacokinetics and therefore have several potential clinical applications...
May 17, 2016: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Sujeet Kumar Gupta, Ashutosh Mishra
BACKGROUND: Non-steroidal anti-inflammatory drugs (NSAIDS) are clinically used as anti-inflammatory, analgesic and antipyretic agents but they have the drawbacks of causing gastric irritation and gastric ulceration. Recently, quinoline derivatives have shown significant anti-inflammatory and less ulcerogenic activity. The present study deals with the synthesis and pharmacological assessment of a series of novel quinoline derivatives bearing azetidinones scaffolds as anti-inflammatory and analgesic agents...
February 10, 2016: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Ramanaiah Illuri, Bharathi Bethapudi, Senthilkumar Anandhakumar, Sasikumar Murugan, Joshua Allan Joseph, Deepak Mundkinajeddu, Amit Agarwal, Chandrasekaran Chinampudur Velusami
The aim of the study was to investigate the safety and anti-inflammatory effects of polysaccharide fraction (F1) of Curcuma longa (NR-INF-02) in classical rodent models of inflammation. F1 was evaluated for its acute oral toxicity and found to be safe upto 5000 mg/kg body weight in rats. The anti-inflammatory activity of F1 was evaluated in acute (carrageenan - induced paw edema; xylene - induced ear edema) and chronic (cotton pellet - induced granuloma) models of inflammation. The results of the study demonstrated that F1 significantly (p ≤ 0...
April 7, 2015: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Mohammad Ramezani, Jamal Shamsara
BACKGROUND: Matrix metalloproteinases (MMPs) contribute to various physiological and pathophysiological processes. An imbalance in MMP activity causes pathological conditions including inflammatory diseases, cancer, and cardiovascular diseases. Each MMP member has many 3D structures available; therefore, selecting one structure for virtual screening becomes challenging. METHODS: In this study, we used the cross-docking approach to rank the available MMP structures for their probable successful performance in virtual screening...
2015: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Afaf A El-Malah, Asmaa E Kassab
BACKGROUND: Long term use of NSAIDS is mainly accompanied by major health implications such as gastrointestinal erosions, ulcerations and nephrotoxicity. These side effects arise from local irritation by the carboxylic acid moiety, that is common to most of NSAIDs (topical effect), in addition to decreased cytoprotective prostaglandin production. Therefore, in the medicinal chemistry research area, there is an ongoing need for the discovery of new, potent and safer anti-inflammatory lead compounds devoid of the irritant carboxylic acid moiety...
2015: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Alka N Choudhary, Arun Kumar, Vijay Juyal
BACKGROUND: Oxygen has double-edge properties as it is essential for life, but can also provoke oxidative stress by protein & lipid per oxidation. The persistent oxidative stress and excess LPO induce several inflammatory mediators such as prostaglandins and leuckotrienes by activating enzymes cyclooxygenase and lipoxygenase. The per oxidation can be blocked by free radical scavengers as antiinflammatory agents. Most of the anti-inflammatory agents, which inhibit the above mentioned enzymes, are associated with side effects such as ulceration and bleeding in gastrointestinal tract; so the attention is focused on benzylideneacetophenones having antinflammatory, antioxidant and gastric protectant activities by virtue of free radical scavengers...
2015: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Sami Bahlas, Omar Fathaldin, Nahid Janoudi, Hani Almoallim, Ashraf Ibrahim, Shereen Algohary
OBJECTIVE: To compare the ratings given by the caregivers regarding the health status of their rheumatoid arthritis (RA) patients to those recorded by the patients themselves and to assess the effect of caring for a patient with RA on the mental health of the caregiver. METHODS: This is a non-interventional, cross-sectional, multi-center epidemiological study conducted at the outpatient clinics of two hospitals in Saudi Arabia. The patients included were diagnosed with RA, over 18 years of age with 1-5 years of disease duration, and all had an identifiable single caregiver who was willing to participate in the study...
2015: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Meng-Jun Zhang, Juan Zhou, Wen Cao, Zhi-Qiang Feng, Jia-Wei Guo, Qing-Juan Han, Wen-Xuan Cao, Xiao Guan, Yun-Yun Li, Jianbo Qin, Yu Wang, Hui-Jing Zhang, Bin Li
BACKGROUND: 3,4-dihydroxycinnamic acid and its derivatives exhibit numerous biologic activities. Such activities have not previously been reported for 3,5-dihydroxycinnamic acid derivatives. In this study, ten derivatives of 3,5- dihydroxycinnamic acid were synthesized and their anti-inflammatory activities were tested in 12-O-tetradecanoylphorbol 13-acetate-induced mouse ear edema. Molecular biological studies have shed lights on their anti-inflammatory mechanism. METHODS: Anti-inflammatory activities of ten new synthesized derivatives of 3,5-dihydroxycinnamic acid were tested in 12-O-tetradecanoylphorbol 13-acetate-induced mouse ear edema, and their anti-inflammatory mechanism was studied by ELISA, real-time RT-PCR, MPO assay and AA-induced mouse ear edema...
2015: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Sherifa Hasabelnaby, Eman M Mohi El-Deen, Ayman Goudah
BACKGROUND: Inflammation is a natural reaction of our body in response to infection or any other injury to renovate that damage. The majority of the available Non-steroidal anti-inflammatory drugs is nonselective and consequently, causes gastric irritation and ulceration. Therefore, it is a beard to design and synthesize a new series of Non-steroidal anti-inflammatory drugs with minimal gastric complications. METHODS: A series of novel 4-(3,4-dimethylphenyl)-2(1H)-phthalazinone derivatives were designed, synthesized and evaluated for their in vivo anti-inflammatory activity...
2015: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Dhansay Dewangan, Kartik T Nakhate, D K Tripathi, Pranita Kashyap, Hemant Dhongde
The aim of the present investigation was to synthesize, characterize and evaluate analgesic and anti- inflammatory activities of 2, 5-disubstituted 1, 3, 4-oxadiazole derivatives. The reaction of starting material 4-chloro-m-cresol with ethyl chloroacetate in dry acetone affords ethyl (4-chloro-3-methylphenoxy) acetate, which after reacting with the hydrazine hydrate in ethanol yields 2(4-chloro-3-methylphenoxy) acetohydrazide. When 2(4-chloro-3-methylphenoxy) acetohydrazide was treated with different aromatic aldehydes, aromatic acids and carbon disulfide in alcoholic solution, different 3-acetyl-5-[(4-chloro-3-methylphenoxy) methyl]-2-aryl-2, 3-dihydro-1, 3, 4-oxadiazole and 2-[(4-chloro-3-methylphenoxy) methyl]-5-aryl-1, 3, 4-oxadiazole derivatives were obtained...
2015: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
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