78582-38-4Relevant academic research and scientific papers
Chemiluminescent acridinium-9-carboxamide boronic acid probes: Application to a homogeneous glycated hemoglobin assay
Adamczyk, Maciej,Chen, Yon-Yih,Johnson, Donald D.,Mattingly, Phillip G.,Moore, Jeffrey A.,Pan, You,Reddy, Rajarathnam E.
, p. 1324 - 1328 (2006)
Chemiluminescent acridinium-9-carboxamide probes containing 1, 3, 9, and 27 phenylboronic acids were prepared and their chemiluminescent properties evaluated. The relative chemiluminescent signal from the probes varied from 4 to 0.83 × 1019 cou
Structural Studies on 4,5-Disubstituted 2-Aminoimidazole-Based Biofilm Modulators that Suppress Bacterial Resistance to β-Lactams
Su, Zhaoming,Yeagley, Andrew A.,Su, Rui,Peng, Lingling,Melander, Christian
, p. 2030 - 2039 (2013/01/15)
A library of 4,5-disubstituted 2-aminoimidazole triazole amide (2-AITA) conjugates has been successfully assembled. Upon biological screening, this class of small molecules was discovered as enhanced biofilm regulators through non-microbicidal mechanisms against methicillin-resistant Staphylococcus aureus (MRSA) and multidrug-resistant Acinetobacter baumannii (MDRAB), with active concentrations in the low micromolar range. The library was also subjected to synergism and resensitization studies with β-lactam antibiotics against MRSA. Lead compounds were identified that suppress the antibiotic resistance of MRSA by working synergistically with oxacillin, a β-lactam antibiotic resistant to penicillinase. A further structure-activity relationship (SAR) study on the parent 2-AITA compound delivered a 2-aminoimidazole diamide (2-AIDA) conjugate with significantly increased synergistic activity with oxacillin against MRSA, decreasing the MIC value of the β-lactam antibiotic by 64-fold. Increased anti-biofilm activity did not necessarily lead to increased suppression of antibiotic resistance, which indicates that biofilm inhibition and resensitization are most likely occurring via distinct mechanisms.
Semi-synthesis and biological evaluation of analogues of UK-2A, a novel antifungal antibiotic from Streptomyces sp. 517-02
Usuki, Yoshinosuke,Mitomo, Koichi,Adachi, Noriko,Ping, Xu,Fujita, Ken-Ichi,Sakanaka, Osamu,Iinuma, Katsuharu,Iio, Hideo,Taniguchi, Makoto
, p. 2011 - 2014 (2007/10/03)
Several analogues of UK-2A, a novel antifungal antibiotic isolated from Streptomyces sp. 517-02, were semi-synthesized for structure-activity studies. In vitro antifungal activities of these compounds against Saccharomyces cerevisiae IFO 0203 were evaluat
Synthesis of mimics to thymidine and 5-(2''-thienyl)-2'-deoxyuridine triphosphates
Wellmar,Hornfeldt,Gronowitz,Johansson
, p. 1059 - 1076 (2007/10/03)
Dicarboxylic acid 5'-monoesters of thymidine and 5-(2-thienyl)- 2''deoxyuridine have been synthesised and evaluated as triphosphate mimics. Glutaric (25, 29), adipic (26, 30), pimelic (27, 31) and trans-1,4- cyclohexane dicarboxylic acids (28, 32) were em
Convenient Synthesis of Alcohol O-Hemiesters using Isopropenyl Esters as Acylating Reagents: Synthesis of Hydrophilic Oxaunomycin 10-O-Hemiester Derivatives
Kita, Yasuyuki,Maeda, Hiroshi,Takahashi, Fumie,Fukui, Seiji
, p. 2639 - 2650 (2007/10/02)
Various types of alcohol O-hemiesters 7a-m were synthesized conveniently in good yield by reaction with isopropenyl esters 4a-f in the presence of a catalytic amount of conc.H2SO4 or toluene-p-sulfonic acid followed by selective deprotection of the terminal esters.This method was applied to a preparation of hydrophilic oxaunomycin 10-O-hemiester derivatives 14a,b and 19a-c.
Salts of erythromycin A esters
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, (2008/06/13)
Highly water-soluble erythromycin A derivatives wherein the desosamine moiety is quaternized with an acyloxy-, benzoyloxy- or alkoxycarbonyl-(or carboxy)-acylmethyl iodide, bromine or chloride and esterified in the 2-position with loweralkyl or --(CH
