Open Medicinal Chemistry Journal最新文献

{"title":"Synthesis, Spectral and Thermo-Gravimetric Analysis of Novel Macromolecular Organo-Copper Surfactants","authors":"Anju Joram, Rashmi Sharma, A. Sharma","doi":"10.2174/1874842201805010145","DOIUrl":"https://doi.org/10.2174/1874842201805010145","url":null,"abstract":"\u0000 \u0000 The present paper highlights:\u0000 Synthesis of copper surfactants derived from edible oils i.e. Groundnut & Sesame and non-edible oils i.e. Neem & Karanj.\u0000 \u0000 \u0000 \u0000 Spectral studies (IR, NMR) have been carried out to understand the structural insight of the surfactants synthesized.\u0000 \u0000 \u0000 \u0000 Thermogravimetric analysis of copper surfactants derived from Groundnut, Sesame, Neem & Karanj has been done to confirm the thermal decomposition/stability. Kinetic parameter i.e. activation energy and thermodynamic parameters i.e. Gibbs free energy, entropy and enthalpy were calculated by five different well-known equations namely Freeman Carroll, Coats - Redfern, Horowitz – Metzger, Broido, and Piloyan –Novikova.\u0000","PeriodicalId":39133,"journal":{"name":"Open Medicinal Chemistry Journal","volume":"25 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75393968","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A Non-Ionic Gadolinium Complex whose Relaxometric Behavior is Sensitive to the variation of pH. An Experimental and Theoretical Study on Geometry, Bonding Nature of polyaminocarboxylic Ligand and Their Gadolinium Complex","authors":"E. Rustoy, N. Raggio","doi":"10.2174/1874842201805010102","DOIUrl":"https://doi.org/10.2174/1874842201805010102","url":null,"abstract":"","PeriodicalId":39133,"journal":{"name":"Open Medicinal Chemistry Journal","volume":"10 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-10-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82227482","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Fungicidal Activities and Characterization of Novel Biodegradable Cu (II) Surfactants Derived from Lauric Acid","authors":"A. Sharma, M. Saxena, Rashmi Sharma","doi":"10.2174/1874842201805010089","DOIUrl":"https://doi.org/10.2174/1874842201805010089","url":null,"abstract":"\u0000 \u0000 Colloidal systems are extremely widespread in nature and are of great practical importance in our daily life. Surfactants are very important in modern engineering and pharmaceutical soap and the complexes of soaps with different ligands are used in almost all sectors of national economy due to the formation of micelles in solutions and high surface activity i.e. the ability of their molecules to form surface adsorption layers. For this purpose, first time we thought about the synthesis of copper surfactants/soaps and their complexation by N/S donor ligands. \u0000 \u0000 \u0000 \u0000 In this paper, we report the synthesis of copper laurate thiourea by conventional methods and its characterization by elemental analysis, IR, NMR, ESR spectral studies. In order to understand their biological aspects and application of these surfactants/complexes as antifungal agents, astudy has also been conducted in the field of biochemistry. In order to understand their biological aspects with special reference to fungicidal activities, three different fungi namely Aspergillus alternaria, Aspergillus Fumigatus and Aspergillus niger were taken and tested by different concentrations of copper laurate soap and its thiourea complex by P.D.A. (Potato dextrose agar) technique. \u0000 \u0000 \u0000 \u0000 Biological studies of these compounds will also provide an important account of information about their industrial utilization.\u0000","PeriodicalId":39133,"journal":{"name":"Open Medicinal Chemistry Journal","volume":"39 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-10-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82240365","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Exploration of Adhesion Molecule Expression in Cardiac Muscle of Early Atherosclerosis Dyslipidemic Sprague Dawley Rats.","authors":"Titin A Wihastuti, Fitria N Aini, Nurul C Lutfiana, Teuku Heriansyah, Nafisatuz Zamrudah","doi":"10.2174/1874104501812010124","DOIUrl":"10.2174/1874104501812010124","url":null,"abstract":"<p><strong>Objective: </strong>This study is aimed to examine the expression of ICAM-1 and VCAM-1 in cardiac tissue of dyslipidemic Sprague Dawley rats.</p><p><strong>Methods: </strong>Eight Sprague Dawley strain rats, with 150-200 gram body weight, were divided into two groups. The control group was fed a standard diet, the positive control group was fed a high-fat diet as our previous study for 8 weeks. The pattern of distribution of ICAM-1 and VCAM-1 in cardiac muscle cell was examined by immunofluorescence and observed with a confocal laser scanning microscope. Lipid profile was also examined at the end of the study.</p><p><strong>Result: </strong>Independent t-test showed no differences in ICAM-1 and VCAM-1 expression in cardiac muscle of hypercholesterol-diet-fed Sprague Dawley rat compared to control.</p><p><strong>Conclusion: </strong>The expression of ICAM-1 and VCAM-1 in cardiac muscle did not change after the onset of atherosclerosis.</p>","PeriodicalId":39133,"journal":{"name":"Open Medicinal Chemistry Journal","volume":"12 ","pages":"124-129"},"PeriodicalIF":0.0,"publicationDate":"2018-10-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6210500/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36727572","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Therapeutic Potential of Prodrugs Towards Targeted Drug Delivery.","authors":"Abhinav P Mishra,&nbsp;Suresh Chandra,&nbsp;Ruchi Tiwari,&nbsp;Ashish Srivastava,&nbsp;Gaurav Tiwari","doi":"10.2174/1874104501812010111","DOIUrl":"https://doi.org/10.2174/1874104501812010111","url":null,"abstract":"<p><p>In designing of Prodrugs, targeting can be achieved in two ways: site-specified drug delivery and site-specific drug bioactivation. Prodrugs can be designed to target specific enzymes or carriers by considering enzyme-substrate specificity or carrier-substrate specificity in order to overcome various undesirable drug properties. There are certain techniques which are used for tumor targeting such as Antibody Directed Enzyme Prodrug Therapy [ADEPT] Gene-Directed Enzyme Prodrug Therapy [GDEPT], Virus Directed Enzyme Prodrug Therapy [VDEPT] and Gene Prodrug Activation Therapy [GPAT]. Our review focuses on the Prodrugs used in site-specific drug delivery system specially on tumor targeting.</p>","PeriodicalId":39133,"journal":{"name":"Open Medicinal Chemistry Journal","volume":"12 ","pages":"111-123"},"PeriodicalIF":0.0,"publicationDate":"2018-10-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/1874104501812010111","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36727571","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Redox State of Human Serum Albumin and Inflammatory Biomarkers in Hemodialysis Patients with Secondary Hyperparathyroidism During Oral Calcitriol Supplementation for Vitamin D.","authors":"Wesam A Nasif,&nbsp;Mohammed H Mukhtar,&nbsp;Hoda M El-Emshaty,&nbsp;Ahmed H Alwazna","doi":"10.2174/1874104501812010098","DOIUrl":"https://doi.org/10.2174/1874104501812010098","url":null,"abstract":"<p><strong>Background: </strong>Hemodialysis (HD) patients with secondary Hyperparathyroidism (s-HPT) are exposed to increased inflammation and oxidative stress. In HD patients, oxidized albumin is a reliable marker of oxidative stress and its clinical significance has been rarely studied.</p><p><strong>Objective: </strong>The objective of this study was to evaluate Cys34 Human Serum Albumin (HSA) as oxidative stress biomarker in HD patients with s-HPT and its relationship with inflammation on bone turnover markers during oral calcitriol supplementation for vitamin D.</p><p><strong>Patients and methods: </strong>Fifteen stable hemodialysis patients with s-HPT (mean age 48.67±8.15, 11 males and 4 females) were used in the experiment to receive calcitriol treatment for 16 weeks (0.25mcg or 0.5 mcg once a day according to serum level of Ca and P for each). The changes in the serum biochemical parameters (Ca, P, ALP, and iPTH), inflammatory markers (CRP and IL-6 levels) and serum oxidative stress condition (SOD, IS and albumin ratio HNA/HMA) were evaluated before and at 8 and 16 weeks of calcitriol treatment. The correlations between those factors were studied.</p><p><strong>Results: </strong>All patients responded to oral calcitriol therapy, with a significant decrease in the serum iPTH. The results showed that calcitriol could effectively suppress iPTH secretion with a significant elevation of serum Ca and P but ALP remained unchanged during the study. It can also effectively reduce the inflammatory markers (CRP and IL-6), while increasing the oxidative markers (SOD and IS). Oxidative albumin ratio HNA/HMA showed a significant (<i>p</i>=0.001) reduction after 16 weeks of calcitriol treatment and the redox state of HSA showed a positive prediction for hyperparathyroidism and for inflammation.</p><p><strong>Conclusion: </strong>The redox state of HSA could be used as a predictor for monitoring hyperparathyroidism and inflammation during calcitriol treatment by retarding albumin oxidation in HD patients with secondary hyperparathyroidism.</p>","PeriodicalId":39133,"journal":{"name":"Open Medicinal Chemistry Journal","volume":"12 ","pages":"98-110"},"PeriodicalIF":0.0,"publicationDate":"2018-10-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/1874104501812010098","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36693602","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"C-C Forming Reactions with Palladium and Platinum: Lessons Learned in Our Group","authors":"A. Hashim, Abdullah Al-Hemyari, Muna S. Bufaroosha, Masataka Watanabe, K. G. Dongol, T. Thiemann","doi":"10.2174/1874842201805010076","DOIUrl":"https://doi.org/10.2174/1874842201805010076","url":null,"abstract":"This short paper details our experiences with Pdand Pt-catalyzed cross-coupling and cyclization reactions in investigations covering the years from 1997 until now. Pd-catalysed Suzuki-Miyaura-, Heckand Sonogashira-type cross coupling reactions in conjunction with other transformations in one pot, especially with the Wittig reaction, are highlighted. This is followed by a description of a combination of Heckand cyclization reactions. Finally, Pt-catalyzed diene-yne cyclization reactions are discussed.","PeriodicalId":39133,"journal":{"name":"Open Medicinal Chemistry Journal","volume":"397 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-09-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78090260","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Biogenic Synthesis of Silver Nanoparticle from Mushroom Exopolysaccharides and its Potentials in Water Purification","authors":"A. Adeeyo, J. Odiyo","doi":"10.2174/1874842201805010064","DOIUrl":"https://doi.org/10.2174/1874842201805010064","url":null,"abstract":"This study reports a novel eco-friendly biosynthesis of Silver Nanoparticles (AgNPs) from Exopolysaccharides (EPS) ofLentinus edodesafter an attempt to optimise the production of EPS through mutagenesis. It further describes some potential application of silver nanoparticles in water treatment.A wild strain ofL. edodeswas subjected to UV irradiation, a physical mutagen, at 254 nm. The wild and resultant irradiated strains were then assessed for the production of EPS and subsequent application of the crude EPSs for biosynthesis of AgNPs. The particles were characterised by colour pattern and UV-visible spectroscopy. Based on superior EPS production and nanoparticle attributes, nanoparticles obtained from UV irradiated process were further subjected to Scanning Electron Microscopy (SEM). EPS produced was quantified by the phenol-sulphuric acid method and studied by GC-MS.Results obtained for EPS productivity indicated the presence of monomer sugars such as arabinose (50.65%), mannose (19.20%), mannitol (15.58%), fructose (7.96%), trehalose (6.49%), and glucuronic acid, xylose, galactose and glucose with low percentages of ≤ 0.11. EPS productivity of wild and mutant strains was obtained as 1.044 and 2.783 mg/ml, respectively, after 7 days of fermentation. The result of EPS production for UV irradiated strain corresponds to a yield improvement of 2.7 fold of the wild-type. UV Spectroscopy and SEM analysis studies on EPS nanoparticle product of the improved (UV irradiated) strain indicated the formation of AgNPs at the absorption band of 421 nm with a size range of 50-100 nm.This study, which aimed at eco-friendly synthesis of myco-nanoparticle has established the novel ability ofL. edodes’polysaccharide in silver nanoparticles biosynthesis. It expounded potential frontiers of silver nanoparticles application in the water industry. To the best of the authors’ knowledge, this result represents the first report on the biosynthesis of AgNPs usingL. edode’sEPS.","PeriodicalId":39133,"journal":{"name":"Open Medicinal Chemistry Journal","volume":"54 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-09-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74544075","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Bacterial Biofilm Inhibition in the Development of Effective Anti-Virulence Strategy.","authors":"Barbara Parrino,&nbsp;Patrizia Diana,&nbsp;Girolamo Cirrincione,&nbsp;Stella Cascioferro","doi":"10.2174/1874104501812010084","DOIUrl":"https://doi.org/10.2174/1874104501812010084","url":null,"abstract":"It was observed that bacterial cells inside the biofilm are thousand times more resistant to the conventional antibiotics than the free-living forms [4]. The biofilm antibiotic resistance is correlatable to various mechanisms involved in both cellular and community level, including, at cellular level, enzymatic resistance, chemical modification of the antibiotic target and changes in cell permeability whereas, at biofilm level, the limited penetration of the antibiotic and the presence in the deepest layers of dormant cells intrinsically resistant to conventional antibiotic treatments [5, 6].","PeriodicalId":39133,"journal":{"name":"Open Medicinal Chemistry Journal","volume":"12 ","pages":"84-87"},"PeriodicalIF":0.0,"publicationDate":"2018-08-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/1874104501812010084","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36546989","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Hemodynamic Effects of the Light Stabilizer Tinuvin 770 in Dogs <i><i>In Vivo</i></i>.","authors":"Miklos Krepuska,&nbsp;Marta Hubay,&nbsp;Endre Zima,&nbsp;Aniko Kovacs,&nbsp;Violetta Kekesi,&nbsp;Huba Kalasz,&nbsp;Brigitta Szilagyi,&nbsp;Bela Merkely,&nbsp;Peter Sotonyi","doi":"10.2174/1874104501812010088","DOIUrl":"https://doi.org/10.2174/1874104501812010088","url":null,"abstract":"<p><strong>Introduction: </strong>Tinuvin 770 [bis(2,2,6,6-tetramethyl-4-piperidinyl) sebacate, Ciba-Geigy, Basel, Switzerland] is a UV light stabilizer that is a component of many plastic materials used world-wide in the medical and food industries. We report on the acute hemodynamic effects of Tinuvin 770 examined in dogs.</p><p><strong>Materials and methods: </strong>Tinuvin 770 was dissolved in a mixture of saline and ethanol (1:1 v/v) and was administered to 12 intravenously narcotized and respirated dogs in increasing doses (T1-T7: 1, 3.3, 6.6, 10, 33.3, 66.6 and 100 mg, respectively). The doses were given as bolus injections over a three minute period, and the effects were recorded for 12 minutes. The vehicle was used as a control. Hemodynamic parameters (heart rate, blood pressure, end-diastolic pressure, dp/dt, cardiac output) and ECG were monitored continously.</p><p><strong>Results: </strong>At doses T1-T4, systolic and diastolic blood pressures, mean pressure and ventricular contractility were significantly decreased without significant changes in cardiac output, heart rate, or PQ interval. At doses T5 and T6, declines in blood pressure and myocardial contractility were observed. At doses T6 and T7, heart rate and PQ interval decreased substantially. Irreversible circulatory failure occured in one dog after administering dose T6 and in 8 dogs following dose T7.</p><p><strong>Conclusion: </strong>Tinuvin 770 induces acute hemodynamic alterations. In lower doses, it causes peripheral vasodilatation, however at higher doses acute cardiac failure occured. Plastics containing Tinuvin 770 should be used with care in medical practice and the laboratory.</p>","PeriodicalId":39133,"journal":{"name":"Open Medicinal Chemistry Journal","volume":"12 ","pages":"88-97"},"PeriodicalIF":0.0,"publicationDate":"2018-08-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6142673/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36546990","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}