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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
Pravin Patil, Bhupendra Mishra, Gitanjali Sheombarsing, Katarzyna Kurpiewska, Justyna Kalinowska-Tłuścik, Alexander Dömling
Recently made accessible α-aminomethyl tetrazoles are excellent starting materials for a further Ugi MCR of high diversity, yielding substituted N-methyl-2-(((1-methyl-1H-tetrazol-5-yl)methyl)amino)acetamides in a library-2-library approach. In detail, we report scope and limitations of the 2-step reaction sequence based on >50 reactions. The target scaffold has four points of diversity and will find applications to fill screening decks for HTS and in structure-based drug design.
December 7, 2017: ACS Combinatorial Science
Haruka Sasaki, Kumiko Yanagi, Satoshi Ugi, Kunihisa Kobayashi, Kumiko Ohkubo, Yuji Tajiri, Hiroshi Maegawa, Atsunori Kashiwagi, Tadashi Kaname
Segmental progeroid syndromes with lipodystrophy are extremely rare, heterogeneous, and complex multi-system disorders that are characterized by phenotypic features of premature aging affecting various tissues and organs. In this study, we present a "sporadic/isolated" Japanese woman who was ultimately diagnosed with mandibular hypoplasia, deafness, progeroid features, and progressive lipodystrophy (MDPL) syndrome (MIM #615381) using whole exome sequencing analysis. She had been suspected as having atypical Werner syndrome and/or progeroid syndrome based on observations spanning a 30-year period; however, repeated genetic testing by Sanger sequencing did not identify any causative mutation related to various subtypes of congenital partial lipodystrophy (CPLD) and/or mandibular dysplasia with lipodystrophy (MAD)...
December 2, 2017: Endocrine Journal
Karandeep Singh, Bhanwar Kumar Malviya, Tapta Kanchan Roy, Venus Singh Mithu, Vimal K Bhardwaj, Ved Prakash Verma, Swapandeep Singh Chimni, Siddharth Sharma
Metal catalyzed post-Ugi cyclization of bis-amides is reported in this study. Exposure of bis-amides to Pd(II) catalyst triggered the formation of seven-membered benzoxazepinones. This investigation established that changing the catalyst to a Echavarren's gold(I) turned off cyclization to seven member ring and turned on 6-exo-dig annulations to afford family of six-membered benzoxazinones. To support the proposed mechanisms, quantum chemical based density functional theory calculations has been performed and validated...
November 28, 2017: Journal of Organic Chemistry
Muthu Thangaraj, Robert Moonsamy Gengan, Bibhuti Ranjan, Ramesh Muthusamy
A series of quinoline based peptides were synthesized by a one-pot reaction through Ugi-four component condensation of lipoic acid, cyclohexyl isocyanide, aniline derivatives and 2-methoxy quinoline-3-carbaldehyde derivatives under microwave irradiation. The products were obtained in excellent yields and high purity. Solvent optimization and the effect of microwave irradiation with various powers were also observed. All the synthesized compounds were characterized by FTIR, NMR spectral data and elemental analysis...
November 16, 2017: Journal of Photochemistry and Photobiology. B, Biology
Yuki Tanaka, Shinji Kume, Shiro Maeda, Norihisa Osawa, Naoko Takeda, Masami Chin-Kanasaki, Keiji Isshiki, Satoshi Ugi, Itsuki Oshima, Takashi Uzu, Hiroshi Maegawa, Shin-Ichi Araki
A single nucleotide polymorphism (SNP) within the acetyl CoA carboxylase (ACC) β gene (ACACB), rs2268388, has been shown to be associated with susceptibility to development of proteinuria in patients with type 2 diabetes. To investigate the biological roles of ACCβ in the pathogenesis of diabetic nephropathy, we examined the effects of overexpression of ACACB using podocyte-specific ACACB-transgenic mice or ACACB-overexpressing murine podocytes. Podocyte-specific ACACB-transgenic mice or littermate mice were treated with streptozotocin (STZ) to induce diabetes, and 12 weeks after induction of diabetes, we examined the expression of podocyte markers to evaluate the degree of podocyte injury in these mice...
November 22, 2017: Biochemical and Biophysical Research Communications
Natalie Marie Gulsrud, Kelly Hertzog, Ian Shears
A nature-based approach to climate resilience aims to challenge and re-frame conventional environmental management methods by refocusing solutions from technological strategies to socio-ecological principles such as human well-being and community-based governance models, thereby improving and legitimizing the delivery of ecosystem services (ES). There are, however, many challenges to applying a socio-ecological agenda to urban climate resilience and thereby re-framing ES delivery as community and people focused, a knowledge gap extensively outlined in the environmental governance literature...
November 14, 2017: Environmental Research
Erik Van der Eycken, Yi He, Zhenghua Li, Koen Robeyns, Luc Van Meervelt
We report herein an efficient gold(I)-catalyzed post-Ugi domino dearomatization/ipso-cyclization/Michael sequence that enables access to libraries of diverse (hetero)arene-annulated tricyclic heterocycles. This process affords novel complex polycyclic scaffolds in moderate to good yields from readily available acyclic precursors with excellent chemo-, regio-, and diastereo-selectivity. The power of this strategy has been demonstrated by the rapid synthesis of 40 highly functionalized polyheterocycles bearing indole, pyrrole, (benzo)furan, (benzo)thiophene, pyrazole and electron-rich arenes in two-operational steps...
November 16, 2017: Angewandte Chemie
Hiroyuki Harada, Shogo Shinohara, Shinji Takebayashi, Masahiro Kikuchi, Keizo Fujiwara, Tetsuhiko Michida, Ryosuke Yamamoto, Kazuki Hayashi, Koji Saida, Yasushi Naito
Background: In Japan, there has been a lot of reports showing an association between facial flushing after light alcohol consumption and heterozygosity for inactive aldehyde dehydrogenase-2 (ALDH2). Persons with inactive ALDH2 may have a higher risk of alcohol-related oral, pharyngeal and esophageal cancers, compared with those with wild-type ALDH2. The purpose of this study was to examine whether flushers with oral or pharyngeal squamous cell carcinoma have an increased risk of synchronous or metachronous cancer of the upper gastrointestinal (UGI) tract...
November 9, 2017: Japanese Journal of Clinical Oncology
Mariana Ingold, Rosina Dapueto, Sabina Victoria, Germán Galliusi, Carlos Batthyàny, Mariela Bollati-Fogolín, David Tejedor, Fernando García-Tellado, José M Padrón, Williams Porcal, Gloria V López
A one-pot efficient, practical and eco-friendly synthesis of tocopherol analogues has been developed using water or solvent free conditions via Passerini and Ugi multicomponent reactions. These reactions can be optimized using microwave irradiation or ultrasound as the energy source. Accordingly, a small library of 30 compounds was prepared for biological tests. The evaluation of the antiproliferative activity in the human solid tumor cell lines A549 (lung), HBL-100 (breast), HeLa (cervix), SW1573 (lung), T-47D (breast), and WiDr (colon) provided lead compounds with GI50 values between 1 and 5 μM...
November 3, 2017: European Journal of Medicinal Chemistry
Ali Hossein Rezayan, Safoura Hariri, Parisa Azerang, Ghazaleh Ghavami, Isabel Portugal, Soroush Sardari
A series of new fluorene bisamide derivatives were synthesized through multi-component Ugi reaction and tested for their in-vitro anti-mycobacterial activity. The structures of the products 5a-w were deduced from their IR, 1H NMR, and 13C NMR spectra. Elemental analyses (CHN) for novel compounds (5a, 5d, 5f, 5h, 5k, 5l, 5p, 5s, 5t, 5v, 5w) was done. These compounds were evaluated as anti-bacterial agents against Mycobacterium bovis and M. tuberculosis, while their activity expressed as the minimum inhibitory concentration (MIC) in μg/mL...
2017: Iranian Journal of Pharmaceutical Research: IJPR
Victoria A Roberts, Michael E Pique, Simon Hsu, Sheng Li
Protein-protein interactions are essential for biological function, but structures of protein-protein complexes are difficult to obtain experimentally. To derive the protein complex of the DNA-repair enzyme human uracil-DNA-glycosylase (hUNG) with its protein inhibitor (UGI), we combined rigid-body computational docking with hydrogen/deuterium exchange mass spectrometry (DXMS). Computational docking of the unbound protein structures provides a list of possible three-dimensional models of the complex; DXMS identifies solvent-protected protein residues...
November 16, 2017: Biochemistry
Martijn C de Koning, Marloes J A Joosen, Franz Worek, Florian Nachon, Marco van Grol, Steven D Klaassen, Duurt P W Alkema, Timo Wille, Hans M de Bruijn
Recently, a new class of reactivators of chemical warfare agent inhibited acetylcholinesterase (AChE) with promising in vitro potential was developed by the covalent linkage of an oxime nucleophile and a peripheral site ligand. However, the complexity of these molecular structures thwarts their accessibility. We report the compatibility of various oxime-based compounds with the use of the Ugi multicomponent reaction in which four readily accessible building blocks are mixed together to form a product that links a reactivating unit and a potential peripheral site ligand...
November 13, 2017: Journal of Medicinal Chemistry
Arjun Gupta, Nivedita Arora, Ugis Gruntmanis
No abstract text is available yet for this article.
October 30, 2017: JAMA Internal Medicine
Eman M M Abdelraheem, Rudrakshula Madhavachary, Arianna Rossetti, Katarzyna Kurpiewska, Justyna Kalinowska-Tłuścik, Shabnam Shaabani, Alexander Dömling
An Ugi multicomponent reaction based two-step strategy was applied to generate medium-sized rings. In the first linear expansion phase, a series of diamines reacted with cyclic anhydrides to produce different lengths of terminal synthetic amino acids as the starting material for the second phase. The Ugi-4-center 3-component reaction was utilized to construct complex medium-sized rings (8-11) by the addition of isocyanides and oxo components. This method features mild conditions and a broad substrate scope.
November 17, 2017: Organic Letters
Ugis Sarkans, Mikhail Gostev, Awais Athar, Ehsan Behrangi, Olga Melnichuk, Ahmed Ali, Jasmine Minguet, Juan Camillo Rada, Catherine Snow, Andrew Tikhonov, Alvis Brazma, Johanna McEntyre
BioStudies ( ) is a new public database that organizes data from biological studies. Typically, but not exclusively, a study is associated with a publication. BioStudies offers a simple way to describe the study structure, and provides flexible data deposition tools and data access interfaces. The actual data can be stored either in BioStudies or remotely, or both. BioStudies imports supplementary data from Europe PMC, and is a resource for authors and publishers for packaging data during the manuscript preparation process...
October 23, 2017: Nucleic Acids Research
Chisato Kusunoki-Tsuji, Shin-Ichi Araki, Shinji Kume, Masami Chin-Kanasaki, Norihisa Osawa, Katsutaro Morino, Osamu Sekine, Satoshi Ugi, Atsunori Kashiwagi, Hiroshi Maegawa
AIM/INTRODUCTION: Diabetes and obesity are important health and economic concerns. We investigated the influence of obesity on diabetes control, the annual medical expenditures, and medications in Japanese patients with type 2 diabetes who were relatively lean in comparison to those in Western countries. MATERIALS AND METHODS: A total of 402 Japanese patients with type 2 diabetes were enrolled and their annual medical expenditures investigated. Obesity was defined as body mass index over 25 kg/m(2) , according to the obesity classifications from the Japan Society for the Study of Obesity...
October 25, 2017: Journal of Diabetes Investigation
Ji Hye Kim, Sun Young Lee, Hyun Gyung Kwon, Sang Pyo Lee, Jeong Hwan Kim, In Kyung Sung, Hyung Seok Park, Chan Sup Shim
Background/Aims: The serum anti-Helicobacter pylori (H. pylori) immunoglobulin G (IgG) and serum pepsinogen (PG) assays are widely used to screen for gastric cancer. An equivocal serology test finding indicates IgG titer between the positive and negative test findings. This study aims to evaluate the long-term follow-up result after an equivocal test finding on the serum anti-H. pylori IgG assay. Methods: Koreans aged 18 years or older with an equivocal serum anti-H...
October 25, 2017: Korean Journal of Gastroenterology, Taehan Sohwagi Hakhoe Chi
Natalia Estrada-Ortiz, Constantinos G Neochoritis, Aleksandra Twarda-Clapa, Bogdan Musielak, Tad A Holak, Alexander Dömling
Based on a combination of an Ugi four component reaction and a ring closing metathesis, a library of novel artificial macrocyclic inhibitors of the p53-MDM2 interaction was designed and synthesized. These macrocycles, alternatively to stapled peptides, target for the first time the large hydrophobic surface area formed by Tyr67, Gln72, His73, Val93, and Lys94 yielding derivatives with affinity to MDM2 in the nanomolar range. Their binding affinity with MDM2 was evaluated using fluorescence polarization (FP) assay and (1)H-(15)N two-dimensional HSQC nuclear magnetic resonance experiments...
October 12, 2017: ACS Medicinal Chemistry Letters
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