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Subash Bhattarai, Merina Gyawali, Khus Raj Dewan, Gaurav Shrestha
INTRODUCTION: Liver cirrhosis is an important health problem worldwide and is a common disease in Nepal. The profile of cirrhosis may vary due to different factors. This study was undertaken to see the demographic and clinical profiles of patients with cirrhosis of liver attending a tertiary care hospital in Central Nepal. METHODS: Six hundred patients with clinical features, laboratory and sonological findings suggestive of chronic liver dysfunction and endoscopic evidence of portal hypertension were included in the study...
October 2017: JNMA; Journal of the Nepal Medical Association
Yue Tao, Shixue Wang, Xiaojie Zhang, Zhen Wang, Youhua Tao, Xianhong Wang
Alternating polypeptoids are particularly appealing because alternating sequence may impart highly-ordered structure and special functions, while their simple synthesis still remains a key challenge. Herein, we describe that natural amino acid monomers can be polymerized via Ugi reaction in a step-growth fashion as an AA' BB' system, which leads to alternating polypeptoids with molecular weight up to 15 kg/mol. These alternating polypeptoids are thermally responsive and exhibit cloud points (Tcps) between 27 and 37 oC...
February 13, 2018: Biomacromolecules
Uzma Rahman, Salvatore Docimo, Aurora D Pryor, Andrew Bates, Nabeel R Obeid, Konstantinos Spaniolas
BACKGROUND: Although multiple studies demonstrate that routine postoperative contrast studies have a low yield in diagnosing patients with early gastrointestinal (GI) leak after bariatric surgery, the practice pattern is unknown. Additionally, routine imaging may hinder procedural pathways that lead to accelerated postoperative discharge. OBJECTIVES: To report on the nationwide use of routine upper GI studies (UGI) and evaluate the effect on hospital resource utilization...
January 3, 2018: Surgery for Obesity and related Diseases: Official Journal of the American Society for Bariatric Surgery
Matthew J Carr, Christopher Oxner, Eric A Elster, Eric M Ritter, Diego Vicente
Management of complex acute surgical pathology in austere environments necessitates rapid evaluation and resource appropriate management to avoid time-associated morbidity and potentially mortality. Obstructive upper gastrointestinal (UGI) pathologies can be particularly challenging and associated with significant morbidity. Herein, we present six patients with UGI obstructions encountered over the course of an 8-mo deployment onboard a US Navy Aircraft Carrier. Each patient presented to our medical department with signs and symptoms of obstructive UGI pathology including one gastric volvulus requiring operative management at sea, one with a new diagnosis of achalasia requiring transportation and continental United States outpatient evaluation, and four patients with food impaction requiring urgent endoscopic management...
February 6, 2018: Military Medicine
Alessia Griglio, Enza Torre, Marta Serafini, Alice Bianchi, Roberta Schmid, Giulia Coda Zabetta, Alberto Massarotti, Giovanni Sorba, Tracey Pirali, Silvia Fallarini
Indoleamine 2,3-dioxygenase plays a crucial role in immune tolerance and has emerged as an attractive target for cancer immunotherapy. In this study, the Passerini and Ugi multicomponent reactions have been employed to assemble a small library of imidazothiazoles that target IDO1. While the p-bromophenyl and the imidazothiazole moieties have been kept fixed, a full SAR study has been performed on the side-chain, leading to the discovery of nine compounds with sub-micromolar IC50 values in the enzyme-based assay...
February 2, 2018: Bioorganic & Medicinal Chemistry Letters
O Van der Poorten, R Van Den Hauwe, K Hollanders, B U W Maes, D Tourwé, M Jida, S Ballet
A 3-step methodology for the synthesis of 1,5-benzothiazepin-4(5H)-one dipeptidomimetics has been elaborated via an Ugi-4CR followed by a S-trityl deprotection and an intramolecular Cu(i)-catalyzed Ullmann condensation with moderate to good yields. In silico and NMR conformational studies showed that the lowest energy conformers stabilize γ- and β-turn structures.
January 30, 2018: Organic & Biomolecular Chemistry
Itziar Guerrero, Marcos San Segundo, Arkaitz Correa
An efficient ligand-free Fe-catalyzed oxidative Ugi-type reaction toward the assembly of α-amino amides and short peptides is described. The reaction proceeds through the α-C(sp3)-H oxidation of N,N-dimethylanilines and further nucleophilic attack of the resulting iminium species by isocyanides. Additive screening showed that judicious choice of the carboxylic acid could lead to the formation of α-amino imides via a 3-component reaction. The process occurs with operational simplicity and is compatible with a variety of sensitive functional groups...
January 26, 2018: Chemical Communications: Chem Comm
Satish K Chitneni, Zachary J Reitman, Rebecca Spicehandler, David M Gooden, Hai Yan, Michael R Zalutsky
Mutations in the metabolic enzyme isocitrate dehydrogenase 1 (IDH1) are commonly found in gliomas. AGI-5198, a potent and selective inhibitor of the mutant IDH1 enzyme, was radiolabeled with radioiodine and fluorine-18. These radiotracers were evaluated as potential probes for imaging mutant IDH1 expression in tumors with positron emission tomography (PET). Radioiodination of AGI-5198 was achieved using a tin precursor in 79 ± 6% yield (n = 9), and 18F-labeling was accomplished by the Ugi reaction in a decay-corrected radiochemical yield of 2...
January 12, 2018: Bioorganic & Medicinal Chemistry Letters
Jie Lei, Jiang-Ping Meng, Dian-Yong Tang, Brendan Frett, Zhong-Zhu Chen, Zhi-Gang Xu
Isocyanide-based multicomponent reactions are among the most powerful synthetic tools available. Particularly, the isocyanide-based Ugi reaction can allow rapid preparation of [Formula: see text]-aminoacyl amide derivatives and polyazaheterocycles with extensive pharmaceutical applications. Moreover, bridged polyazaheterocycles, including one or more quaternary carbon centers, can be constructed via the Ugi cascade reaction in a few steps. This review will emphasize synthesis and bioactivities of bridged compounds with quaternary centers constructed through Ugi cascade reactions...
January 16, 2018: Molecular Diversity
Lhassane Ismaili, Maria do Carmo Carreiras
Alzheimer's disease (AD) is a multifactorial and fatal neurodegenerative disorder affecting around 35 million people worldwide, which is characterized by decline of cholinergic function, deregulation of amyloid beta (Aβ) oligomers formation and Aβ fibril deposition. Multi-target--directed ligands (MTDLs) have emerged as an original strategy for developing new therapeutic agents on AD. Multicomponent reactions (MCRs) are a useful alternative to sequential multistep syntheses, allowing scaffold diversity and a rapid and easy access to biologically relevant compounds...
January 12, 2018: Current Topics in Medicinal Chemistry
Eman M M Abdelraheem, Samad Khaksar, Katarzyna Kurpiewska, Justyna Kalinowska-Tłuścik, Shabnam Shaabani, Alexander Dömling
The direct non-peptidic macrocycle synthesis of α-isocyano-ω-amines via the classical Ugi 4-component reaction (U-4CR) is introduced. Herein, an efficient and flexible, just 2-step procedure to complex macrocycles is reported. In the first step, the reaction between unprotected diamines and isocyanocarboxylic acids gives high diversity of unprecedented building blocks in high yield. In the next step, the α-isocyano-ω-amines undergo an U-4CR with high diversity of aldehydes and carboxylic acids in a one-pot procedure...
January 12, 2018: Journal of Organic Chemistry
Vunnam Srinivasulu, Scott McN Sieburth, Raafat El-Awady, Noor M Kariem, Hamadeh Tarazi, Matthew John O'Connor, Taleb H Al-Tel
Employing a build/couple/pair strategy, a serendipitous one-pot protocol for the diastereoselective construction of diverse collections of chromenopyrroles is described. This methodology features an unprecedented five-step cascade including azomethine ylide generation followed by in situ intramolecular [3 + 2]-cycloaddition. Furthermore, this protocol was extended to access enantiopure chromenopyrroles using amino acids as chiral auxiliary. Moreover, postpairing reactions were employed to increase the diversity and complexity of our pilot compound collections...
January 12, 2018: Organic Letters
Giulia Rainoldi, Fabio Begnini, Mariska De Munnik, Leonardo Lo Presti, Christophe M L Vande Velde, Romano V A Orru, Giordano Lesma, Eelco Ruijter, Alessandra Silvani
We developed two Ugi-type three-component reactions of spirooxindole-fused 3-thiazolines, isocyanides and either carboxylic acids or trimethylsilylazide, to give highly functionalized spirooxindole-fused thiazolidines. Two diverse libraries were generated using practical and robust procedures affording the products in typically good yields. The obtained thiazolidines proved to be suitable substrates for further transformations. Notably, both the Ugi-Joullié and the azido-Ugi reactions resulted highly diastereoselective, affording predominantly the trans-configured products, as confirmed by X-ray crystallographic analysis...
January 11, 2018: ACS Combinatorial Science
O Bouglouga, A Bagny, L M Lawson-Ananissoh, K Amanga, R El-Hadj Yakoubou, L Kaaga, M Djibril, D Redah
To analyze the indications for upper gastrointestinal endoscopy (UGIE) and determine the frequency of the pathological findings observed in rural areas of Africa. This retrospective study includes 9 series of 5-day visits to perform these examinations. Patients were informed of the presence of the endoscopy team by a bulletin on a rural radio station and by general practitioners at the Kara University Hospital. Patients were recruited from the hospital clinics and from the general population of the Kara region...
November 1, 2017: Médecine et Santé Tropicales
Adel Alhaj Saleh, Michal R Janik, Rami R Mustafa, Mohammed Alshehri, Adil H Khan, Seyed Mohammad Kalantar Motamedi, Shiraz Rahim, Indravadan Patel, Amir Aryaie, Mujjahid Abbas, Tomasz Rogula, Leena Khaitan
INTRODUCTION: Sleeve gastrectomy (SG) is one of the most common procedures performed for weight loss. Many seek the "perfect sleeve" with the notion that the type of calibrating device affects sleeve shape, and this in turn will affect outcomes and complications. Two major concerns after SG are amount of weight loss and acid reflux. Our aim was to determine if the various calibration methods could impact sleeve shape and thereby allow for better outcomes of weight loss and reflux. METHODS: A retrospective chart review was performed of 210 patients who underwent SG and had postoperative upper gastrointestinal (UGI) study from 2011 to 2015 in a single center by a single (fellowship-trained) bariatric surgeon...
January 8, 2018: Obesity Surgery
Ammiel Martínez Canil, Angelo Iossa, Pietro Termine, Daniela Caporilli, Vincenzo Petrozza, Gianfranco Silecchia
BACKGROUND: Laparoscopic sleeve gastrectomy (LSG) has gained popularity in the last 10 years for its good results in weight loss and comorbidity control. However, guidelines on the pathological examination of the specimen are lacking. The aim of this retrospective study was to determine the usefulness of the routine specimen examination when presurgery endoscopy (upper gastrointestinal endoscopy, UGIE) and multiple gastric biopsies are part of the preoperative work-up. METHODS: A retrospective review of records of the patients submitted to LSG between January 2012 and August 2017 was carried out...
January 5, 2018: Obesity Surgery
Peter C Church, Ruth Cytter Kuint, Oren Ledder, Victor M Navas-López, Malgorzata Sladek, Annecarin Brückner, Robert N Baldassano, Batia Weiss, Baruch Yerushalmi, Shehzad A Saeed, Jeffrey Hyams, Anthony Otley, Anne M Griffiths, Dan Turner, Mary-Louise C Greer
OBJECTIVES: While magnetic resonance enterography (MRE) can accurately reflect ileal inflammation in pediatric Crohn's disease (CD), there are no pediatric data on the accuracy of MRE to detect upper gastrointestinal tract (UGI) lesions. We aimed to compare MRE and esophagogastroduodenoscopy (EGD) in detecting the spectrum and severity of UGI disease in children. METHODS: This is an ancillary study of the prospective multi-center ImageKids study focusing on pediatric MRE...
December 28, 2017: Journal of Pediatric Gastroenterology and Nutrition
Angélica de Fátima S Barreto, Veronica Alves Dos Santos, Carlos Kleber Z Andrade
Isocyanide-based multicomponent reactions (IMCRs) allow the construction of relatively complex molecules through a one-pot synthesis. The combination of IMCRs in a consecutive or sequential fashion further extends the complexity of the molecules obtained. Herein, we report the efficient application of this approach to the synthesis of acylhydrazines bearing 1,5-disubstituted tetrazoles. Our strategy was accomplished in only three steps: first, a one-pot hydrazino-Ugi-azide four-component reaction; second a hydrazinolysis and finally an additional hydrazino-Ugi-azide reaction...
2017: Beilstein Journal of Organic Chemistry
Mehdi Ghandi, Saleh Salahi, Abuzar Taheri, Alireza Abbasi
A facile one-pot method has been developed for the synthesis of novel pyrrolo[2,1-a]pyrazine scaffolds. A variety of 1-(1H-tetrazol-5-yl)-1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine derivatives were obtained in moderate to high yields in methanol using a one-pot four-component condensation of 1-(2-bromoethyl)-1H-pyrrole-2-carbaldehyde, amine, isocyanide and sodium azide at room temperature. These reactions presumably proceed via a domino imine formation, intramolecular annulation and Ugi-azide reaction. Unambiguous assignment of the molecular structures was carried out by single-crystal X-ray diffraction...
December 11, 2017: Molecular Diversity
Majid Nami, Peyman Salehi, Minoo Dabiri, Morteza Bararjanian, Sajjad Gharaghani, Mona Khoramjouy, Ahmed Al-Harrasi, Mehrdad Faizi
Novel substituted amino acid tethered norsufentanil derivatives were synthesized by the four-component Ugi reaction. Norsufentanil was reacted with succinic anhydride to produce the corresponding carboxylic acid. The resulting carboxylic acid has undergone a multicomponent reaction with different aldehydes, amines, and isocyanides to produce a library of the desired compounds. In all cases, amide bond rotation was observed in the NMR spectra. In vivo analgesic activity of the synthesized compounds was evaluated by a tail flick test...
December 8, 2017: Chemical Biology & Drug Design
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