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N-acyl or endocannnabanoid or NAPE

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https://www.readbyqxmd.com/read/28644004/the-intricate-effects-of-alpha-amino-and-lysine-modifications-on-arginine-methylation-on-the-n-terminal-tail-of-histone-h4
#1
Melody D Fulton, Jing Zhang, Maomao He, Meng-Chiao Ho, Y George Zheng
Chemical modifications on the DNA and nucleosomal histones tightly control the gene transcription program in eukaryotic cells. The "histone code" hypothesis proposes that the frequency, combination, and location of post-translational modifications (PTMs) on the core histones compose a complex network of epigenetic regulation. Currently, there are at least 23 different types and over 450 histone PTMs discovered, and the PTMs on lysine and arginine residues account for a crucial part of the histone code. Although significant progress has been achieved in recent years, the molecular basis for the histone code is far from being fully understood...
June 23, 2017: Biochemistry
https://www.readbyqxmd.com/read/28641003/synthesis-and-anti-inflammatory-evaluation-of-2-aminobenzaldehydes-via-ir-iii-catalyzed-c-h-amidation-of-aldimines-with-acyl-azides
#2
Saegun Kim, Prashant Chakrasali, Hyo Sun Suh, Neeraj Kumar Mishra, Taeyoung Kim, Sang Hoon Han, Hyung Sik Kim, Byung-Moo Lee, Soo Bong Han, In Su Kim
The aldimine-directed C-H amidation of various arenes with N-acyl azides as amidation surrogates under cationic iridium(III) catalysis is described. This transformation efficiently provides a range of 2-aminobenzaldehydes derivatives with excellent site-selectivity and functional group compatibility. The resulting 2-aminobenzaldehyde framework provides facile access to a range of biologically interesting heterocycles. In addition, all synthetic compounds were screened for anti-inflammatory activity against interleukin-1β (IL-1β) and tumor necrosis factor alpha (TNF-α) with lipopolysaccharide (LPS)-induced RAW264...
June 22, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28639122/targeting-prostate-specific-membrane-antigen-psma-with-f-18-labeled-compounds-the-influence-of-prosthetic-groups-on-tumor-uptake-and-clearance-profile
#3
Vincent Bouvet, Melinda Wuest, Justin J Bailey, Cody Bergman, Nancy Janzen, John F Valliant, Frank Wuest
PURPOSE: Prostate-specific membrane antigen (PSMA) is an important biomarker expressed in the majority of prostate cancers. The favorable positron emission tomography (PET) imaging profile of the PSMA imaging agent 2-(3-(1-carboxy-5-[(6-[(18)F]fluoro-pyridine-3-carbonyl)-amino]-pentyl)-ureido)-pentane-dioic acid [(18)F]DCFPyL in preclinical prostate cancer models and in prostate cancer patients stimulated the development and validation of other fluorine-containing PSMA inhibitors to further enhance pharmacokinetics and simplify production methods...
June 21, 2017: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
https://www.readbyqxmd.com/read/28638683/low-prevalence-of-obesity-in-beh%C3%A3-et-s-disease-is-associated-with-high-obestatin-level
#4
Süleyman Serdar Koca, Murat Kara, Metin Özgen, Ramazan Dayanan, Caner Feyzi Demir, Kader Aksoy, Nevin İlhan, Emir Dönder, Ahmet Işık
OBJECTIVE: Chronic inflammatory diseases are associated with altered body composition. Ghrelin has anti-inflammatory effects, and its level is altered in obesity and inflammatory diseases. The aim of the study was to evaluate the prevalence of obesity and ghrelin and obestatin levels in patients with Behçet's disease (BD). MATERIAL AND METHODS: One hundred and forty-three (143) patients with BD and 112 healthy controls (HC) were enrolled. Participants were subdivided according to the body mass index (BMI) as lean (<18...
June 2017: European Journal of Rheumatology
https://www.readbyqxmd.com/read/28633201/rapid-start-up-of-denitrifying-granular-sludge-by-dosing-with-semi-starvation-fluctuation-c-n-ratio-strategy
#5
Wenyu Niu, Jianbo Guo, Jing Lian, Yuanyuan Song, Caicai Lu, Haibo Li, Yi Han, Pengna Yin
This study cultivated denitrifying granular sludge in three UASB reactors by the semi-starvation fluctuation C/N ratio strategy (reactor 1 (R1): constant C/N ratio; R2: regular fluctuation C/N ratio; and R3: semi-starvation fluctuation C/N ratio (SSF)). Microbial aggregates appeared in R1, R2 and R3 on days 28, 14 and 6, respectively. Compared with the results in R1 and R2, the guanosine tetraphosphate (ppGpp) concentration was highest, the acyl homoserine lactones (AHLs) concentration quickly reached a certain threshold, and more protein (PN) of extracellular polymeric substances (EPS) secretion resulted in the rapid formation of denitrifying granular sludge in R3...
June 1, 2017: Bioresource Technology
https://www.readbyqxmd.com/read/28632928/n-acylsulfonamides-synthetic-routes-and-biological-potential-in-medicinal-chemistry
#6
REVIEW
Alessandra Ammazzalorso, Barbara De Filippis, Letizia Giampietro, Rosa Amoroso
Sulfonamide is a common structural motif in naturally occurring and synthetic medicinal compounds. The rising interest in sulfonamides and N-acyl derivatives is attested by the large number of drugs and lead compounds identified in last years, explored in different fields of medicinal chemistry and showing biological activity. Many acylsulfonamide derivatives were designed and synthesized as isosteres of carboxylic acids, being the characteristics of these functional groups very close. Starting from chemical routes to N-acylsulfonamides, this review explores compounds of pharmaceutical interest, developed as enzymatic inhibitors or targeting receptors...
June 20, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28631313/salivary-gingival-crevicular-fluid-and-serum-levels-of-ghrelin-and-chemerin-in-patients-with-periodontitis-and-overweight
#7
H F R Jentsch, N Arnold, V Richter, J Deschner, T Kantyka, S Eick
BACKGROUND AND OBJECTIVE: Nutrition and body weight are modifying factors for periodontitis. The purpose of this study was to quantify two molecules (ghrelin and chemerin), released in association with food intake and obesity, in periodontally healthy and diseased individuals with respect to different body mass categories. MATERIAL AND METHODS: The two main groups (patients with chronic periodontitis and periodontally healthy/gingivitis volunteers) were subdivided into groups of subjects with normal weight [body mass index (BMI) <25] and groups of overweight/obese subjects (BMI ≥25)...
June 20, 2017: Journal of Periodontal Research
https://www.readbyqxmd.com/read/28628892/structural-characterization-of-wall-and-lipidated-polysaccharides-from-clostridium-perfringens-atcc-13124
#8
Evgeny Vinogradov, Annie Aubry, Susan M Logan
Cell surface polysaccharides produced by C. perfringens ATCC 13124 were analyzed using NMR, chemical and immunological methods. Two distinct polymers were identified. The more abundant PS1 had a structure based on a polymer of β-mannosamine with a number of modifications, including varying levels of substitution at O-6 with PEtN, N-acetylation, and different linkages between monosaccharides. The shortest variant of PS1 represented a lipoteichoic acid. It contained only 1-4-linkages between ManNAc residues, minor branching α-Ribf, and glucosyl-glycerol at the reducing end, which was acylated with linear saturated fatty acids C16, C18, and C20 (dominant)...
June 15, 2017: Carbohydrate Research
https://www.readbyqxmd.com/read/28628337/buckling-under-pressure-curvature-based-lipid-segregation-and-stability-modulation-in-cardiolipin-containing-bilayers
#9
Kevin J Boyd, Nathan N Alder, Eric R May
Mitochondrial metabolic function is affected by the morphology and protein organization of the mitochondrial inner membrane (MIM). Cardiolipin (CL) is a unique tetra-acyl lipid that is involved in the maintenance of the highly-curved shape of the MIM as well as spatial organization of the proteins necessary for respiration and oxidative phosphorylation. Cardiolipin has been suggested to self-organize into lipid domains due to its inverted conical molecular geometry, though the driving forces for this organization are not fully understood...
June 19, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/28621955/regioselective-three-component-reaction-of-pyridine-n-oxides-acyl-chlorides-and-cyclic-ethers
#10
D Heulyn Jones, Steven T Kay, Jayde A McLellan, Alan R Kennedy, Nicholas C O Tomkinson
A novel three-component reaction of pyridine N-oxides, acyl chlorides, and cyclic ethers is described. Treatment of an electron-deficient pyridine N-oxide with an acyl chloride in the presence of a cyclic ether at 25-50 °C leads to a substituted pyridine as a single regioisomer in up to 58% isolated yield. Isotopic-labeling experiments and substrate scope support the reaction proceeding through a carbene intermediate.
June 16, 2017: Organic Letters
https://www.readbyqxmd.com/read/28620585/identification-of-a-large-family-of-slam-dependent-surface-lipoproteins-in-gram-negative-bacteria
#11
Yogesh Hooda, Christine C L Lai, Trevor F Moraes
The surfaces of many Gram-negative bacteria are decorated with soluble proteins anchored to the outer membrane via an acylated N-terminus; these proteins are referred to as surface lipoproteins or SLPs. In Neisseria meningitidis, SLPs such as transferrin-binding protein B (TbpB) and factor-H binding protein (fHbp) are essential for host colonization and infection because of their essential roles in iron acquisition and immune evasion, respectively. Recently, we identified a family of outer membrane proteins called Slam (Surface lipoprotein assembly modulator) that are essential for surface display of neisserial SLPs...
2017: Frontiers in Cellular and Infection Microbiology
https://www.readbyqxmd.com/read/28617515/synthesis-of-n-acetoxy-n-arylamides-via-diacetoxyiodobenzene-promoted-double-acylation-reaction-of-hydroxylamines-with-aldehydes
#12
Huaiyuan Zhang, Yingpeng Su, Ke-Hu Wang, Danfeng Huang, Jun Li, Yulai Hu
A facile and efficient synthesis of N-acetoxy-N-arylamides through double acylations of hydroxylamines with aldehydes and diacetoxyiodobenzene is reported. The yields of the products are good to excellent.
June 15, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28615134/synthesis-and-biological-evaluation-of-5-fatty-acylamido-1-3-4-thiadiazole-2-thioglycosides
#13
Srikanth Vudhgiri, Dhevendar Koude, Dileep Kumar Veeragoni, Sunil Misra, R B N Prasad, Ram Chandra Reddy Jala
In the present study, the synthesis of 1, 3, 4-thiadiazole-based thioglycosides were accomplished in good yields with employing a convergent synthetic route. The starting material 5-amino-1, 3, 4-thiadiazole-2-thiol and followed by a series of 5-fatty-acylamido-1, 3, 4-thiadiazole-2-thiols (4a-4j) were synthesized with different fatty acid chlorides. The glycosylation of compounds 4a-4j were achieved with trichloroacetimidate methodology. Antimicrobial and cytotoxicity activities of title compounds were evaluated...
June 3, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28614759/structure-activity-relationship-study-and-optimisation-of-2-aminopyrrole-1-benzyl-4-5-diphenyl-1h-pyrrole-3-carbonitrile-as-a-broad-spectrum-metallo-%C3%AE-lactamase-inhibitor
#14
Ross P McGeary, Daniel T C Tan, Christopher Selleck, Marcelo Monteiro Pedroso, Hanna E Sidjabat, Gerhard Schenk
A SAR study on derivatives of 2-amino-1-benzyl-4,5-diphenyl-1H-pyrrole-3-carbonitrile 5a revealed that the 3-carbonitrile group, vicinal 4,5-diphenyl and N-benzyl side chains of the pyrrole are important for the inhibitory potencies of these compounds against members representing the three main subclasses of metallo-β-lactamases (MBLs), i.e. IMP-1 (representing the B1 subgroup), CphA (B2) and AIM-1 (B3). Coupling of 5a with a series of acyl chlorides and anhydrides led to the discovery of two N-acylamide derivatives, 10 and 11, as the two most potent IMP-1 inhibitors in this series...
June 3, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28610914/an-increase-level-of-acylation-stimulating-protein-is-correlated-with-metabolic-risk-markers-in-north-indian-obese-women
#15
Supriya Mishra, Vani Gupta, Sameeksha Mishra, Vandana Gupta, Abbas Ali Mahdi, Rekha Sachan
BACKGROUND AND AIMS: The present study was to investigate the association between serum acylation stimulating protein (ASP) level with metabolic risk factors in North Indian obese women. METHODS: This is a case control study, total n=322 women aged between 20 and 45 years (n=162 with metabolic syndrome & n=160 without metabolic syndrome) were recruited for the study according to National Cholesterol Education Program Treatment Panel (NCEPATP) guidelines. Serum ASP level were determined by enzyme linked immunosorbent assay...
June 10, 2017: Diabetes & Metabolic Syndrome
https://www.readbyqxmd.com/read/28610318/two-new-species-of-trimma-pisces-gobiidae-from-fiji-south-western-pacific-ocean
#16
Richard Winterbottom
Two new species of Trimma are described from Fiji. Trimma bathum n. sp. lacks scales on the cheeks, opercle and predorsal midline, has 18-19 unbranched pectoral fin rays, an unbranched 5th pelvic fin ray that is 40-56% the length of the 4th ray, 17-18 gill rakers on the outer surface of the first gill arch, a U-shaped interorbital and a narrow slit-like postorbital trench, a low, median fleshy ridge extending half-way towards the orbit from the origin of the first dorsal fin, and, when freshly collected, a pink head and body with most body scales having an orange-brown spot or short bar at their centres...
May 24, 2017: Zootaxa
https://www.readbyqxmd.com/read/28609982/description-of-a-new-species-of-i-cnemaspis-i-squamata-gekkonidae-from-knuckles-range-of-sri-lanka
#17
Sudesh Batuwita, Sampath Udugampala
A new species of Cnemaspis Strauch is described from Knuckles Range of Sri Lanka. This new species had been previously confused with Cnemaspis podihuna Deraniyagala. Cnemaspis kandambyi sp. nov. closely resembles C. podihuna and C. molligodai Wickramasinghe & Munindradasa. Cnemaspis kandambyi sp. nov. differs from C. podihuna by having 7-8 (versus 3-6) unpored scales in each side of the precloacal-femoral pores row, lacking (versus having) an internasal scale, body (axilla to groin) relatively long 47.7-48...
April 12, 2017: Zootaxa
https://www.readbyqxmd.com/read/28609876/a-new-physoschistura-from-a-salween-affluent-in-western-yunnan-teleostei-nemacheilidae
#18
Marco Endruweit
Physoschistura absumbra, new species, is described from the watershed of the Salween in Cangyuan County, Yunnan Province, China. The combination of a complete lateral line, a continuous lower jaw, and the absence of a suborbital lobe distinguishes it from all other congeners. Further diagnostic characters are a long (dorsally 23-25% SL, laterally 26-28% SL) and deep head (at nape 13-14% SL), a shallow body (15-17% SL), a deep caudal peduncle (13-14% SL), 9-12 rather regular flank bars, a complete basicaudal bar, and a maximum adult size of about 44 mm SL...
May 9, 2017: Zootaxa
https://www.readbyqxmd.com/read/28599915/multiplex-polymerase-chain-reaction-for-identification-of-escherichia-coli-escherichia-albertii-and-escherichia-fergusonii
#19
Rebecca L Lindsey, L Garcia-Toledo, D Fasulo, L M Gladney, N Strockbine
Escherichia coli, Escherichia albertii, and Escherichia fergusonii are closely related bacteria that can cause illness in humans, such as bacteremia, urinary tract infections and diarrhea. Current identification strategies for these three species vary in complexity and typically rely on the use of multiple phenotypic and genetic tests. To facilitate their rapid identification, we developed a multiplex PCR assay targeting conserved, species-specific genes. We used the Daydreamer™ (Pattern Genomics, USA) software platform to concurrently analyze whole genome sequence assemblies (WGS) from 150 Enterobacteriaceae genomes (107 E...
June 6, 2017: Journal of Microbiological Methods
https://www.readbyqxmd.com/read/28598636/formal-3-4-annulation-of-%C3%AE-%C3%AE-unsaturated-acyl-azoliums-access%C3%A2-to-enantioenriched-n-h-free-1-5-benzothiazepines
#20
Chao Fang, Tao Lu, Jindong Zhu, Kewen Sun, Ding Du
An unprecedented formal [3 + 4] annulation of α,β-unsaturated acyl azoliums with 2-aminobenzenethiols has been utilized to synthesize enantioenriched N-H-free 1,5-benzothiazepines, which are recognized as privileged structures in numerous biologically active scaffolds. This protocol offers a rapid and direct pathway to access the target compounds with high enantioselectivities and has been applied in the concise synthesis of chiral drug (R)-thiazesim.
June 9, 2017: Organic Letters
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