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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
Kurosh Kalantar, Nasser Gholijani, Nashmin Mousaei, Malihe Yazdani, Zahra Amirghofran
BACKGROUND: Dracocephalum kotschyi is traditionally used for its anti-inflammatory effects. We aimed to investigate the effects of ethyl acetate extract of D. kotschyi on the expression of key inflammatory mediators and main signaling molecules involved in regulation of inflammation. METHODS: Lipopolysaccharide (LPS)-stimulated J774.1 mouse macrophages were cultured in the presence of the plant extract and examined by the real time-PCR for gene expressions of interleukin (IL)-1β, tumor necrosis factor (TNF)-α, inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2...
June 7, 2018: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Alejandra de Moreno de LeBlanc, Romina Levit, Graciela Savoy de Giori, Jean Guy LeBlanc
BACKGROUND: Current therapies for against inflammatory bowel disease (IBD) are sometimes limited by high costs, high toxicities and/or undesirable side effects, reasons for which new treatments are constantly being developed and studied. In this regards an increasing mass of data has demonstrated that fecal transplantations and probiotic supplementations have shown promising effects and could be considered as adjunct IBD treatments to decrease some of the unwanted side effects caused by primary treatments...
May 2, 2018: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Ritchu Sethi, Sandeep Jain, Sandeep Arora, Deepika Saini, Neelam Jain
A series of N-(benzimidazol-1-ylmethyl)-4-chlorobenzamide derivatives (3a-3m) were synthesized by Mannich reaction using 2-substituted benzimidazole, formaldehyde and p-chlorobenzamide as reactants. The structures of novel target compounds were elucidated by spectral and analytical techniques and screened for in-vivo anti-inflammatory activity and ulcerogenic activity. In addition, the prepared derivatives were also evaluated for in vitro antimicrobial activity against gram negative, gram positive and fungal strains...
April 26, 2018: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Yousery E Sherif, Ryan A Ansary, Moustafa A Gouda
Interaction of dibenzobarallene 3 with thiosemicarbazides 4-8 afforded the Phthalazinediones 10-15. The structures of the newly synthesized compounds were confirmed on the basis of elemental analysis and spectral data. One equation was predicted using quantitative structure activity relationship (QSAR) and regression analysis for the anti-inflammatory activity with a regression correlation (R) close to unity. The anti-inflammatory activity and analgesic effect of the thioamides 10-15 were determined by collagen II-adjuvant induced paw edema test in rats...
April 12, 2018: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Arash Ghasemi, Behzad Danesh, Jamshid Yazdani, Seyed Jalal Hosseinimehr
BACKGROUND: The skin toxicity-induced by ionizing radiation may limit the duration of treatment and may lead discomfort to quality life of patients during radiotherapy. OBJECTIVE: The purpose of this randomized, placebo-controlled, double-blind study was to investigate the preventive effect of oral administration of celecoxib (CLX) on the acute radiation-induced skin toxicity in patients with breast cancer. METHODS: Sixty breast cancer patients were randomly assigned to use CLX (400 mg per day) or placebo capsules during radiotherapy...
April 11, 2018: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Sujeet Kumar Gupta, Pratik Khanal, Arun Kumar, Arun Kumar, Neha Srivastava, Bhumika Yogi, Anshuman Sinha
BACKGROUND: Recently, pyrazole derivatives have shown significant anti-inflammatory activity. Non-steroidal anti-inflammatory drugs have the drawbacks of such as gastric irritation and gastric ulceration in treatment of inflammation. So the current study deals with the synthesis and pharmacological evaluation of a series of novel pyrazole derivatives as anti-inflammatory agents. METHODS: A series of novel ethyl 5-(substituted)-1H-pyrazole-3-carboxylate (2a-j) were synthesized and evaluated for anti-inflammatory activity using carrageenan-induced inflammation in rat paw edema model...
April 11, 2018: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Ashwani K Dhingra, Bhawna Chopra, Jagdeep S Dua, Deo N Prasad
BACKGROUND: Various mediators and anti-inflammatory drugs were used since from a long time but it is still a challenge for the medicinal chemists to treat or reduce the symptoms of inflammatory diseases. Most of the clinically used anti-inflammatory drugs such as NSAIDs, Coxibs and GCs are allied with considerable toxicity. OBJECTIVE: The search of novel anti-inflammatory agent is not an ending process. Although the drug treatment has been improved steadily but yet, it is still there is a need to develop more potent therapeutic agents...
2017: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Sasikumar Murugan, Bharathi Bethapudi, Divya Purusothaman, Prasanna R Chandrasekaran, Chandrasekaran C Velusami
BACKGROUND: Curcuma longa Linn, "the golden spice" is a common spice used in Southern Asia and Middle East countries. It has a history of ethnopharmacological use for its various activities like anti-septic, anti-inflammatory, anti-oxidant, anti-microbial, anti-cancer and so on. OBJECTIVE: To investigate the effects of polar extract of C. longa (PCL) against monosodium iodoacetate (MIA) induced osteoarthritis in rat and to compare with curcuminoids, which are contemporarily believed to be the only active phytochemicals of C...
2017: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Aniket P Sarkate, Deepak K Lokwani, Kshipra S Karnik, Devanand B Shinde
BACKGROUND: Due to the need and adverse effects associated with the available anti-inflammatory agents, an attempt was made to develop the new anti-inflammatory agents with better activity and lesser adverse effects. OBJECTIVE: Synthetic approaches based on chemical modification of NSAIDs have been undertaken with the aim of improving NSAIDs safety profile. METHOD: In the present study, a series of thiazole derivatives (3a-3x) was synthesized and tested for its anti-inflammatory with analgesic and nitric oxide releasing properties...
2017: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Amit S Tapkir, Sohan S Chitlange, Ritesh P Bhole
BACKGROUND: We have developed a new series of 36 substituted thiazole derivatives prepared via reaction of substituted benzothiazole-2-amine with substituted phenacyl bromide. OBJECTIVE: This study was aimed to develop and successfully evaluate anti-inflammatory activity of substituted thiazole derivatives. METHOD: A new series of 36 substituted thiazole derivatives was synthesized and derivatives were characterized by analytical and spectrometric methods like IR, MS, and 1H NMR...
2017: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Cosimo Chelazzi, Gianluca Villa, Paola Mancinelli, Matteo Becatti, Maria Boddi, Mirella Coppo, Stefano Romagnoli
BACKGROUND: Low circulating levels of adiponectin are associated with the occurrence of infection after surgery in patients with cancer. Data are lacking on whether surgical stress is associated with a reduction in circulating levels of adiponectin. Furthermore, the relationship between oxidative stress and postoperative complications has not been investigated. OBJECTIVE: The aim of this study was to evaluate the pre-, intra-, and postoperative levels of adiponectin in patients who underwent major abdominal surgery for malignancy and their association with postoperative complications...
2017: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Honnegowdanahally K Kumara, Doddahindaiah M Suyoga Vardhan, J Shiva Kumar, D Channe Gowda
BACKGROUND: Studies on anti-inflammatory and antimicrobial agents remains a challenging and important area in medicinal chemistry research due to more toxic and rapid development of resistance against first effective drugs. In search of novel anti-inflammatory and antimicrobials agents, bisthiourea derivatives of dipeptide conjugated to 6-fluoro-3- (piperidin-4-yl)benzo[d]isoxazole were synthesized. METHODS: The peptides were synthesized by solution phase method and conjugated to 6- fluoro-3-(piperidin-4-yl)benzo[d]isoxazole using 1-ethyl-3-(3-dimethyl aminopropyl)carbodiimide (EDCI)/hydroxybenzotriazole (HOBt) as a coupling agent and N-methylmorpholine (NMM) as a base...
2017: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Nadav Shraibom, Alka Madaan, Vidushi Joshi, Ritu Verma, Anika Chaudhary, Gautam Mishra, Anshumali Awasthi, Anu Taneja Singh, Manu Jaggi
BACKGROUND: We have developed a novel aqueous polyherbal formulation (SIRB-001) consisting of 3 herbs; Rheum palmatum L., Lonicera Japonica and Rehmannia glutinosa Libosch in the ratio 1:1:3. SIRB-001 has demonstrated efficacious effects in psoriasis patients. OBJECTIVE: This study was aimed at scientifically evaluating the in vitro antipsoriatic activity of SIRB-001. METHOD: The in vitro anti-psoriatic properties of SIRB-001 were assessed in human keratinocyte cell line; HaCaT...
2017: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Inna P Tsypysheva, Sophia S Borisevich, Liana F Zainullina, Nina S Makara, Alena V Koval'skaya, Polina R Petrova, Sergey L Khursan, Yulia V Vakhitova, Felix S Zarudii
BACKGROUND AND OBJECTIVES: Neurodegenerative diseases and inflammation are always linked to each other; therefore the elaboration of new chemical compounds, which interact with pharmacological targets involved into these two processes, can become one of ways of correction of these types of human CNS pathology. In the field of this problem the anti-inflammatory activity of ten 3-amino derivatives of quinolizidine alkaloid (.)-cytisine (the data about nootropic activity of these compounds are outlined by us previously) was studied by using in vivo, in vitro and in silico approaches...
2017: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Ajmer Singh Grewal, Viney Lather, Deepti Pandita, Ruchi Dalal
BACKGROUND: Phosphodiesterase 4 (PDE4), is one of the members of PDE superfamily which catalyzes the hydrolysis of cyclic adenosine monophosphate to adenosine monophosphate in pro-inflammatory and immunomodulatory cells, leading to increased inflammatory processes. PDE4 has been reported as an attractive therapeutic target involved in various inflammatory disorders. OBJECTIVE: The present work was designed to synthesize and evaluate the anti-inflammatory activity of some new triazole amine derivatives as potential PDE4 inhibitors...
2017: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
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