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Kap-Sun Yeung et al.
Bioorganic & medicinal chemistry letters, 23(1), 198-202 (2012-12-04)
A series of substituted carboxamides at the indole C7 position of the previously described 4-fluoro-substituted indole HIV-1 attachment inhibitor 1 was synthesized and the SAR delineated. Heteroaryl carboxamide inhibitors that exhibited pM potency in the primary cell-based assay against a
Elanur Aydın et al.
Toxicology and industrial health, 31(8), 764-772 (2013-04-05)
Carvone (CVN) is a monocyclic monoterpene found in the essential oils of Mentha spicata var. crispa (Lamiaceae) and Carum carvi L. (Apiaceae) plants and has been reported to have antioxidant, antimicrobial, anticonvulsant, and antitumor activities. The beneficial health properties of
Anita Toulmin et al.
Journal of medicinal chemistry, 51(13), 3720-3730 (2008-06-19)
Partition coefficients were measured for 47 compounds in the hexadecane/water ( P hxd) and 1-octanol/water ( P oct) systems. Some types of hydrogen bond acceptor presented by these compounds to the partitioning systems are not well represented in the literature
Kap-Sun Yeung et al.
Bioorganic & medicinal chemistry letters, 23(1), 203-208 (2012-12-04)
As part of the SAR profiling of the indole-oxoacetic piperazinyl benzamide class of HIV-1 attachment inhibitors, substitution at the C7 position of the lead 4-fluoroindole 2 with various 5- and 6-membered heteroaryl moieties was explored. Highly potent (picomolar) inhibitors of
Aleem Gangjee et al.
Bioorganic & medicinal chemistry, 21(4), 891-902 (2013-01-22)
A series of fourteen N(4)-(substituted phenyl)-N(4)-alkyl/desalkyl-9H-pyrimido[4,5-b]indole-2,4-diamines was synthesized as potential microtubule targeting agents. The synthesis involved a Fisher indole cyclization of 2-amino-6-hydrazinylpyrimidin-4(3H)-one with cyclohexanone, followed by oxidation, chlorination and displacement with appropriate anilines. Compounds 6, 14 and 15 had low
Madhumita Patel et al.
Advanced healthcare materials, 4(10), 1565-1574 (2015-06-03)
Neuronal differentiation of tonsil-derived mesenchymal stem cells (TMSCs) is investigated in a 3D hybrid system. The hybrid system is prepared by increasing the temperature of poly(ethylene glycol)-poly(l-alanine) aqueous solution to 37 °C through the heat-induced sol-to-gel transition, in which TMSCs
Origène Nyanguile et al.
Antimicrobial agents and chemotherapy, 52(12), 4420-4431 (2008-10-15)
The exogenous control of hepatitis C virus (HCV) replication can be mediated through the inhibition of the RNA-dependent RNA polymerase (RdRp) activity of NS5B. Small-molecule inhibitors of NS5B include nucleoside and nonnucleoside analogs. Here, we report the discovery of a
Xuan Li et al.
PloS one, 9(10), e111801-e111801 (2014-11-02)
Quorum sensing, bacterial cell-to-cell communication with small signal molecules, controls the virulence of many pathogens. In contrast to other vibrios, neither the VanI/VanR acylhomoserine lactone quorum sensing system, nor the three-channel quorum sensing system affects virulence of the economically important
Chika Saigo et al.
Drug design, development and therapy, 8, 1073-1082 (2014-08-22)
Indoxyl sulfate (IS), a putative low-molecular weight uremic toxin, is excreted in the urine under normal kidney function, but is retained in the circulation and tissues during renal dysfunction in acute kidney injury and chronic kidney disease. IS, which is
Cagdas Kara et al.
Asian-Australasian journal of animal sciences, 28(11), 1599-1605 (2015-11-19)
Twenty Holstein calves were used to investigate the effects of mannanoligosaccharides (MOS) supplementation in the whole milk on growth performance, faecal score, faecal pH, selected faecal bacterial populations and health during the preweaning period. Healthy calves selected by clinical examination
Martin Gilar et al.
Journal of chromatography. A, 1381, 110-117 (2015-01-22)
Sample introduction in microfluidic liquid chromatography often generates wide zones rather than peaks, especially when a large sample volume (relative to column volume) is injected. Formation of wide injection zones can be further amplified when the sample is dissolved in
Alan P Graves et al.
Journal of medicinal chemistry, 48(11), 3714-3728 (2005-05-27)
Molecular docking is widely used to predict novel lead compounds for drug discovery. Success depends on the quality of the docking scoring function, among other factors. An imperfect scoring function can mislead by predicting incorrect ligand geometries or by selecting
Ayrikim Adugna et al.
African health sciences, 15(2), 656-664 (2015-07-01)
Diarrheal disease and its complications remain a major cause of morbidity and mortality in children. The prevalence and antibiogram of E. coli as causative agents of diarrhea vary from region to region, and even within countries in the same geographical
Elvin D de Araujo et al.
The Journal of biological chemistry, 290(37), 22699-22714 (2015-07-23)
The sulfonylurea receptor 2B (SUR2B) forms the regulatory subunit of ATP-sensitive potassium (KATP) channels in vascular smooth muscle. Phosphorylation of the SUR2B nucleotide binding domains (NBD1 and NBD2) by protein kinase A results in increased channel open probability. Here, we
Magda Monari et al.
Chemistry (Weinheim an der Bergstrasse, Germany), 21(31), 11038-11049 (2015-06-03)
A new Michael-Michael cascade reaction between 2-(2-oxoindolin-3-ylidene)acetic esters 1 and nitroenoates 2, catalyzed by bifunctional thioureas, is investigated. The combination of the two Michael reactions results in a novel and facile [4+2] or [3+2] spiroannulation process, which is characterized by
Hannah Gaimster et al.
PloS one, 10(9), e0136691-e0136691 (2015-09-04)
During the transition from exponential to stationary phase E. coli produces a substantial quantity of the small, aromatic signalling molecule indole. In LB medium the supernatant indole concentration reaches a maximum of 0.5-1 mM. At this concentration indole has been
Fernando Rodrigues de Sá Alves et al.
Mini reviews in medicinal chemistry, 9(7), 782-793 (2009-06-13)
The indole scaffold probably represents one of the most important structural subunits for the discovery of new drug candidates. The demonstration that many alkaloids contain the indole nucleus, the recognition of the importance of essential amino acid tryptophan in human
Nripendra Nath Biswas et al.
Organic & biomolecular chemistry, 13(3), 925-937 (2014-11-20)
Gram-negative bacteria such as Pseudomonas aeruginosa use N-acylated L-homoserine lactones (AHLs) as autoinducers (AIs) for quorum sensing (QS), a major regulatory and cell-to-cell communication system for social adaptation, virulence factor production, biofilm formation and antibiotic resistance. Some bacteria use indole
Rodolphe Beaud et al.
Angewandte Chemie (International ed. in English), 51(50), 12546-12550 (2012-11-06)
IRONic electrophilic indoles! The C3-regioselective hydroarylation of N-acetyl indoles with aromatic nucleophiles mediated by FeCl(3) features a rare example of the electrophilic reactivity of the indole core in a Friedel-Crafts reaction. This indole umpolung allows us straightforward access to the
Haoting Tian et al.
Environmental science & technology, 49(13), 7784-7792 (2015-06-02)
A new photoreduction pathway for nitro-aromatic compounds (NACs) and the underlying degradation mechanism are described. 1,3-Dinitrobenzene was reduced to 3-nitroaniline by the widely distributed aromatic molecule indole; the reaction is facilitated by montmorillonite clay mineral under both simulated and natural
Paula V Gonzalez et al.
Journal of medical entomology, 52(6), 1315-1321 (2015-09-10)
Aedes aegypti (L.) (Diptera: Culicidae) is the key vector of three important arboviral diseases: dengue, yellow fever, and chikungunya. Immature stages of this species inhabit human-made containers placed in residential landscapes. In this study, we evaluated a few compounds in
Yong-Gyun Jung et al.
Applied and environmental microbiology, 81(1), 211-219 (2014-10-19)
A variety of systems have been developed to study biofilm formation. However, most systems are based on the surface-attached growth of microbes under shear stress. In this study, we designed a microfluidic channel device, called a microfluidic agarose channel (MAC)
Changwu Yue et al.
World journal of microbiology & biotechnology, 31(4), 541-548 (2015-02-24)
The draft genome sequence of marine Streptomyces olivaceus strain FXJ 7.023 contains a cryptic Type III polyketide synthase (type III PKS) gene cluster, which is similar to the Streptomyces coelicolor THN biosynthesis gene cluster. A putative type III PKS (SoRppA)
Wenping Hua et al.
Molecular biology reports, 41(7), 4817-4825 (2014-04-08)
The dried root of Gentiana macrophylla is a well-known traditional Chinese herbal medicine for treating jaundice, hepatitis, and stomachic and choleretic ailments. However, natural sources are now in short supply. A lack of information about its genetic background has been
Hélène Gérard et al.
The Journal of organic chemistry, 78(18), 9233-9242 (2013-08-07)
The chemo-, regio-, and stereoselectivities of multicomponent [4 + 2]/[3 + 2] domino cycloaddition reactions involving nitroindole derivatives with vinylethers and acrylates are studied computationnally and compared to experimental results. In this process, the nitroarene first reacts as an electron-deficient
Anthony G Dodge et al.
Applied and environmental microbiology, 81(5), 1610-1615 (2014-12-21)
Abrin is a toxic protein produced by the ornamental plant Abrus precatorius, and it is of concern as a biothreat agent. The small coextracting molecule N-methyl-l-tryptophan (l-abrine) is specific to members of the genus Abrus and thus can be used
Suleyman Durmaz et al.
Pakistan journal of medical sciences, 31(5), 1067-1072 (2015-12-10)
To determine the clonal relationship of ESBL-producing and quinolone resistant E.coli strains and to investigate the risk factors for infections with these microorganisms. A total of 95 ESBL-producing and quinolone resistant E.coli strains isolated from various clinical specimens of inpatients
Vera I Safronova et al.
Archives of microbiology, 197(7), 889-898 (2015-05-28)
Eleven extra-slow-growing strains were isolated from nodules of the relict legume Vavilovia formosa growing in North Ossetia (Caucasus) and Armenia. All isolates formed a single rrs cluster together with the type strain Tardiphaga robiniae LMG 26467(T), while the sequencing of
W Neumann et al.
Dalton transactions (Cambridge, England : 2003), 44(4), 1748-1753 (2014-12-04)
Carbaboranes are increasingly used as pharmacophores to replace phenyl substituents in established drug molecules. In contrast to traditional organic chemistry, elaborate procedures to introduce functionality frequently fail in the case of carbaboranes and their chemistry is often hampered by degradation
Jean-Pierre H Perchellet et al.
Anticancer research, 34(4), 1643-1655 (2014-04-03)
Synthetic 6,7-annulated-4-substituted indole compounds, which elicit interesting antitumor effects in murine L1210 leukemia cells, were tested for their ability to inhibit human HL-60 tumor cell proliferation, disrupt mitosis and cytokinesis, and interfere with tubulin and actin polymerization in vitro. Various
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