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Saeed Balalaie, Raihaneh Ramezani Kejani, Elmira Ghabraie, Fatemeh Darvish, Frank Rominger, Fatima Hamdan, Hamid Reza Bijanzadeh
A diversity-oriented access to diastereoselective arylidene2,5-diketopiperazines is elaborated via a sequential Ugi Post-transformation involving catalytic cyclization and oxidative Heck reactions sequence. This sequence offers an interesting multicomponent entry to a library of 2,5-diketopiperazines and arylidene 2,5-diketopiperazines under mild reaction conditions in good to excellent yields.
October 19, 2017: Journal of Organic Chemistry
S Shaabani, C G Neochoritis, A Twarda-Clapa, B Musielak, T A Holak, A Dömling
Using the pharmacophore-based virtual screening platform ANCHOR.QUERY, we morphed our recently described Ugi-4CR scaffold towards a β-lactam scaffold with potent p53-MDM2 antagonizing activities. 2D-HSQC and FP measurements confirm potent MDM2 binding. Molecular modeling studies are used to understand the observed SAR in the β-lactam series.
May 1, 2017: MedChemComm
Behzad Adibi-Motlagh, Abbas Sahebghadam Lotfi, Aram Rezaei, Ehsan Hashemi
The immobilization of bioactive peptides as key molecules in numerous biological and physiological functions holds promise for designing advanced biomaterials. Graphene and its derivatives, having unique physicochemical properties, have brought considerable attention in the life sciences. In this regard, the chemical manipulation of the graphene surface with bioactive peptides opens a new horizon to design bioactive materials for a variety of future nanobiotechnologies. In this study, the first straightforward strategy for the covalent immobilization of the cell-adhesion peptide onto the graphene surface based on the Ugi four-component assembly process (Ugi 4-CAP) will be presented...
January 1, 2018: Materials Science & Engineering. C, Materials for Biological Applications
Karen Queliza, Faith D Ihekweazu, Deborah Schady, Craig Jensen, Richard Kellermayer
OBJECTIVES: Differentiating ulcerative colitis (UC) and Crohn's disease (CD) can be clinically challenging, especially in children. Granulomatous inflammation has traditionally been attributed to CD. Crypt-associated giant cells and granulomas, however, have been observed in colonic biopsies of UC patients. This phenomenon has not been described in the upper gastrointestinal (UGI) tract with UC. METHODS: Seven pediatric UC patients with granulomatous UGI (gUGI) lesions were identified...
October 6, 2017: Journal of Pediatric Gastroenterology and Nutrition
Matthew J Nelson, Frank H Miller, Nelson Moy, Angelika Zalewski, Nirmala Gonsalves, Dyanna Gregory, Ikuo Hirano
BACKGROUND AND AIMS: Eosinophil predominant mucosal inflammation is central to the diagnosis and activity assessment of eosinophilic esophagitis (EoE). Esophageal mural remodeling is an important consequence of EoE that is responsible for adverse events of dysphagia, food impaction, and esophageal stenosis. The aim of this study was to compare upper endoscopy (EGD) with barium upper gastrointestinal study (UGI) for the detection of esophageal inflammation and remodeling in adults with EoE...
October 5, 2017: Gastrointestinal Endoscopy
Cristine S Velazco, Brenna S Fullerton, Joseph A Brazzo, Charles R Hong, Tom Jaksic, Carol E Barnewolt
PURPOSE: Small bowel length is the most reliable predictor of enteral independence in pediatric short bowel syndrome. Retrospectively measured bowel lengths on upper GI with small bowel follow-through (UGI/SBFT) were compared to operative measurements. METHODS: A pediatric radiologist and surgical trainees blinded to operative measurements retrospectively analyzed UGI/SBFT studies using the digital radiography curved measurement tool. Children with SBS and severe intestinal failure (parenteral nutrition >90days) at a multidisciplinary intestinal failure program 2002-2015 were included...
September 5, 2017: Journal of Pediatric Surgery
Georges Antoine Bazolo Ba Ngouala, Loubna Bourgi, Joao Arm Indo Da Veiga, Arona Sakho
INTRODUCTION: This study aimed to determine the epidemiological, clinical and endoscopic profile of patients referred for upper gastrointestinal (UGI) endoscopy to the Clinique Magou in Louga and to analyze the difficulties encountered. METHODS: We conducted a retrospective and descriptive study by analysing the reports of 248 gastrointestinal endoscopies performed between 1(st) January and 31(st) December 2014. RESULTS: The average age was 39...
2017: Pan African Medical Journal
Jing Li, Ran Chen, Ye Yang, Zhemin Zhang, Guang-Chen Fang, Wei Xie, Weiguo Cao
The uracil DNA glycosylase superfamily consists of at least six families with a diverse specificity towards DNA base damage. Family 1 UNG exhibits exclusive specificity on uracil-containing DNA. Here, we report a family 1 UNG homolog from Nitratifractor salsuginis with distinct biochemical features that differentiate it from conventional family 1 UNGs. Globally, the crystal structure of N. salsuginis UNG shows a few additional secondary structural elements. Biochemical and enzyme kinetic analysis, coupled with structural determination, molecular modeling and molecular dynamics simulations, shows that N...
October 4, 2017: FEBS Journal
Olivier Van der Poorten, Mouhamad Jida, Dirk Tourwé, Steven Ballet
BACKGROUND: Benzazepines received great attention in the field of medicinal chemistry since this scaffold has been recognized to belong to the important family of privileged templates. More specifically, the 4-amino-1,2,4,5-tetrahydro-2-benzazepin-3-one (Aba) is used as a core structure in a variety of constrained therapeutic peptide (turn) mimetics. Most of the synthetic approaches towards this template have focused on cyclizations which form the central 7-membered azepine ring. OBJECTIVE: Previous investigations in our group allowed an expansion of the substitution patterns in the 4-amino-benzazepin-3-one scaffold by introduction of methyl substituents at positions 4 and 5 of the azepinone ring system, but also to 1-aryl substituted compounds...
October 2, 2017: Medicinal Chemistry
Ahmad Shaabani, Ronak Afshari
Herein, we report the direct synthesis of carboxamide-functionalized graphene oxide (carboxamide-f-GO) for the development of new nanocatalysts, with highly dispersed particles, through covalent functionalization with a facile and direct strategy. This surface functionalization was carried out through a one-pot sequential four-component Ugi reaction. Subsequently, the Ugi-ligand decorated on the surface of the graphene oxide sheets coordinated with copper nanoparticles (Cu NPs) and finally covered with magnetic nanoparticles...
September 23, 2017: Journal of Colloid and Interface Science
Ahmad Shaabani, Seyyed Emad Hooshmand
A planning strategy for diversity-oriented catalyst-free synthesis of pseudopeptides containing rhodanine scaffolds has been developed via a novel one-pot sequential six-component reaction in water. This approach is an efficient, environmentally friendly and expeditious procedure for direct access to wide ranges of pharmacologically significant and structurally interesting compounds based on the union of multicomponent reactions approach via tandem Michael/domino cycloaddition/Ugi reactions sequence from readily available starting materials...
January 2018: Ultrasonics Sonochemistry
Kai Chen, Gaobo Yu, Furui He, Qingfeng Zhou, Dunchao Xiao, Jiacheng Li, Yuhong Feng
Alginate (Alg) was grafted on the surface of anisotropic silica (SiO2-x) via the Ugi reaction (Alg-SiO2-1, Alg-SiO2-2, and Alg-SiO2-4). Compared with pristine SiO2-x, modified SiO2-x is more sensitive to pH. Three stable liquid paraffin-in-water emulsions were prepared with Alg-SiO2-1, Alg-SiO2-2, and Alg-SiO2-4. Alg-SiO2-2 exhibited satisfactory emulsification ability. The emulsions became more stable as emulsion pH varied from 2.0 to 6.2 because of polymer chain interactions that led to the formation of a three-dimensional network...
November 15, 2017: Carbohydrate Polymers
Eman M M Abdelraheem, Michel P de Haan, Pravin Patil, Katarzyna Kurpiewska, Justyna Kalinowska-Tłuścik, Shabnam Shaabani, Alexander Dömling
A concise two step synthesis of tetrazole containing macrocycles from readily accessible starting materials is presented. The first step comprises a chemoselective amidation of amino acid derived isocyanocarboxylicacid esters with unprotected symmetrical diamines to afford diverse α-isocyano-ω-amines. In the second step, the α-isocyano-ω-amines undergo an Ugi tetrazole reaction to close the macrocycle. Advantageously, this strategy allows short access to 11-19-membered macrocycles in which substituents can be independently varied at three different positions...
October 6, 2017: Organic Letters
Guangzu Gao, Nariman Nezami, Mahan Mathur, Patricia Balcacer, Gary Israel, Michael Spektor
OBJECTIVE: To determine if the attenuation of contrast material in the excluded stomach compared with the gastric pouch is helpful in diagnosing gastrogastric (GG) fistula. MATERIALS AND METHODS: In a retrospective study, 13 CT scans in 12 patients (age 43.2 ± 9.2, 10 females) who had undergone Roux-en-Y gastric bypass and who had oral contrast in both the gastric pouch and excluded stomach were qualitatively and quantitatively evaluated for GG fistula by two radiologists, using upper GI series (UGI) as the gold standard...
September 8, 2017: Abdominal Radiology
K F Axelsson, M Wallander, H Johansson, D Lundh, M Lorentzon
BACKGROUND: There is high evidence for secondary prevention of fractures, including hip fracture, with alendronate treatment, but alendronate's efficacy to prevent hip fractures in the oldest-old (≥80 years old), the population with the highest fracture risk, has not been studied. OBJECTIVE: To investigate if alendronate treatment among the oldest old with prior fracture was related to decreased hip fracture rate and sustained safety. METHODS: Using a national database of men and women undergoing a fall risk assessment at a Swedish healthcare facility, we identified 90 795 patients who were 80 years or older and had a prior fracture...
August 30, 2017: Journal of Internal Medicine
Pablo Pertejo, Pablo Peña-Calleja, Israel Carreira-Barral, Roberto Quesada, Nicolás Alejandro Cordero, Francisco Javier Rodríguez, María García-Valverde
Pyrrolo[2,1-c][1,4]benzodiazepines (PBDs) and other benzo-fused N-heterocycles constitute privileged structures found in numerous bioactive compounds. Thus, developing simple and selective syntheses to furnish these derivatives from easily accessible starting materials is an important and challenging goal. In this work, novel pyrrolobenzodiazepine and pyrroloquinazoline derivatives have been synthesized following a common two step synthetic strategy. This strategy involves a one-pot Ugi/cyclization sequence followed by a reduction with spontaneous thermocontrolled cyclization...
September 20, 2017: Organic & Biomolecular Chemistry
Mitchell S Cappell, Charlton E Stevens, Mitual Amin
AIM: To systematically review the syndrome of giant gastric lipomas, report 2 new illustrative cases. METHODS: Literature systematically reviewed using PubMed for publications since 1980 with following medical subject heading/keywords: ("giant lipoma") AND ("gastric") OR [("lipoma") and ("gastric") and ("bleeding")]. Two authors independently reviewed literature, and decided by consensus which articles to incorporate. Computerized review of pathology/endoscopy records at William Beaumont Hospitals, Royal Oak and Troy, Michigan, January 2005-December 2015, revealed 2 giant gastric lipomas among 117110 consecutive esophagogastroduodenoscopies (EGDs), which were thoroughly reviewed, including re-review of original endoscopic photographs, radiologic images, and pathologic slides...
August 14, 2017: World Journal of Gastroenterology: WJG
Thimmalapura M Vishwanatha, Katarzyna Kurpiewska, Justyna Kalinowska-Tłuścik, Alexander Dömling
An alternative approach toward the simple and robust synthesis of highly substituted peptidic thiazole derivatives using Ugi-multicomponent reaction (U-MCR) is described. Thus, we introduced the enantiopure (R)-2-methyl-2-isocyano-3-(tritylthio)propanoate as a novel class of isocyanide in MCR. This bifunctional isocyanide was found to undergo mild cyclodehydration to afford thiazole containing peptidomimetics in a short synthetic sequence. Several examples of bis-heterocyclic rings were also synthesized through the proper choice of the aldehyde component in the U-4CR...
September 15, 2017: Journal of Organic Chemistry
Jung Wan Choe, Seung Young Kim, Jong Jin Hyun, Sung Woo Jung, Young Kul Jung, Ja Seol Koo, Hyung Joon Yim, Sang Woo Lee
Background/Aims: Various clinical scoring systems, including the Glasgow-Blatchford score (GBS), Rockall risk score (RS), and AIMS65 score (AIMS65), have been validated to predict the clinical outcomes in patients with upper gastrointestinal bleeding (UGIB). We compared the performance of these three scoring systems in predicting clinical outcomes in patients with UGIB in Korea. Methods: We retrospectively evaluated 286 patients with UGIB who visited emergency department...
August 14, 2017: Gut and Liver
Rabbinu Rangga Pribadi, Ari Fahrial Syam, Ening Krisnuhoni
Helicobacter pylori infection is commonly found worldwide. In Indonesia, the prevalence of H. pylori infection is 22.1%. The bacteria are responsible for gastritis, peptic ulcer disease (PUD), and gastric cancer.Helicobacter pylori may also has a role in functional dyspepsia. Diagnostic approach consists of noninvasive and invasive examinations. One of the invasive strategy is upper gastrointestinal (UGI) endoscopy and gastric mucosa biopsy.
April 2017: Acta Medica Indonesiana
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