62172-89-8Relevant academic research and scientific papers
ANTIBIOTIC RESISTANCE BREAKERS
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Page/Page column 125, (2019/01/05)
The invention relates to antibiotic compounds of formula (A1) and pharmaceutically acceptable salts, solvates, tautomers and combinations thereof, wherein X and L are optional linkers and one of RA or R1 comprises Ar1, wherein Ar1 is an antibiotic resistance breaker moiety which comprises an optionally substituted C6-10 aryl, C7-13 aralkyl, C5-10 heteroaryl, C6-13 heteroaralkyl, C5-10 heterocyclyl, C6-13 heterocyclalkyl, C3-10 carbocyclyl, C4-13 carbocyclalkyl, -C(=NR')-NR'R'' or –CH2- CH=CH2 group; wherein after administration of the compound to a bacterial infection this moiety reduces or prevents efflux. The invention also discloses pharmaceutical compositions comprising compounds of formula (A1) and the use of such compounds as medicaments, in particular, to treat bacterial infections, such as drug-resistant bacterial infections.
Dinickel complexes with anthyridine-based ligands
Huang, Da-Wei,Liu, Yi-Hung,Peng, Shie-Ming,Liu, Shiuh-Tzung
, p. 8265 - 8271 (2016/06/09)
Two new dinickel complexes with anthyridine-based ligands, 5-phenyl-2,8-bis(2-pyridinyl)-1,9,10-anthyridine (L2) and 5-phenyl-2,8-bis(6′-bipyridinyl)-1,9,10-anthyridine (L3), are reported. Complexation of Ni(OAc)2 with L2 and L3 in trifluoroacetic acid provided the corresponding dinickel complexes [{Ni2(L2)(H2O)6(CF3COO)2}(CF3COO)2] (2) and [Ni2(L3)(CF3COO)4(H2O)] (3), respectively. Both complexes were characterized by spectroscopic methods and further confirmed by X-ray crystallography. Structural analyses of 2 and 3 revealed the Ni?Ni distances in the complexes to be 5.4086(6) and 5.0138(7) ?, respectively. The catalytic activities of complexes 2 and 3 toward the reduction of carboxylic acids were evaluated. It appears that complex 3 shows a good catalytic activity toward the reduction of carboxylates into the corresponding alcohols by diphenylsilane.
Synthesis of heterosubstituted hexaarylbenzenes via asymmetric carbonylative couplings of benzyl halides
Potter, Robert G.,Hughes, Thomas S.
, p. 1187 - 1190 (2008/01/04)
Asymmetric carbonylative couplings of benzyl halldes have been shown to give heterosubstituted 1,3-diarylacetones In moderate to high yields. These asymmetric ketones were converted via Knoevenagel condensations to tetraarylcyclopentadienones, and further
Synthesis and Preliminary Biological Evaluation of 6-O-[11C]-[(methoxymethyl)benzyl]guanines, New Potential PET Breast Cancer Imaging Agents for the DNA Pepair Protein AGT
Liu, Xuan,Zheng, Qi-Huang,Fei, Xiangshu,Wang, Ji-Quan,Ohannesian, David W.,Erickson, Leonard C.,Stone, K. Lee,Hutchins, Gary D.
, p. 641 - 644 (2007/10/03)
Novel radiolabeled O6-benzylguanine derivatives, 6-O-[11C]-[(methoxymethyl)benzyl]guanines ([11C]p-O6-MMBG, 1a; [11C]m-O6-MMBG, 1b; ([11C]o-O6-MMBG, 1c), have been synthesized for evaluation as new potential positron emission tomography (PET) breast cancer imaging agents for DNA repair protein, O6-alkylguanine-DNA alkyltransferase (AGT).
Oxidation of benzylic alcohols and ethers to carbonyl derivatives by nitric acid in dichloromethane
Strazzolini, Paolo,Runcio, Antonio
, p. 526 - 536 (2007/10/03)
Nitric acid in dichloromethane may be successfully employed for the oxidation of benzylic alcohols and ethers to the corresponding carbonyl compounds. The proposed method proved to be of general applicability, affording very good yields of aldehydes and ketones and showing interesting chemoselectivity in many instances, allowing competitive aromatic nitration to be avoided, as well as - in the case of aldehydes - any further oxidation to carboxylic acids. The reaction probably proceeds by a radical mechanism, the active species in the oxidation process being NO2. Competitive formation of nitro esters was observed in some cases, whereas poor results were obtained with allylic and non-benzylic substrates. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2003.
Synthesis of radiolabeled O6-benzylguanine derivatives as new potential PET tumor imaging agents for the DNA repair protein O6-alkylguanine-DNA alkyltransferase
Zheng, Qi-Huang,Liu, Xuan,Fei, Xiangshu,Wang, Ji-Quan,Ohannesian, David W.,Erickson, Leonard C.,Stone, K. Lee,Martinez, Tanya D.,Miller, Kathy D.,Hutchins, Gary D.
, p. 1239 - 1252 (2007/10/03)
Novel radiolabeled O6-benzylguanine derivatives, 2-amino-6-O-[11C]-[(methoxymethyl)benzyloxy]-9-benzyl purines ([11C]p-O6AMBP, 1a; [11C]m-O6-AMBP, 1b; [11C]o-O6-AMBP, 1c), have been synthesized for evaluation as new potential positron emission tomography (PET) tumor imaging agents for the DNA repair protein, O6-alkylguanine-DNA alkyltransferase (AGT). The appropriate precursors for radiolabeling were obtained in three steps from starting material 2-amino-6-chloropurine with moderate to excellent chemical yields. Tracers were prepared by O-[11C]methylation of hydroxymethyl precursors using [11C]methyl triflate. Pure target compounds were isolated by solid-phase extraction (SPE) purification procedure in 45-60% radiochemical yields (decay corrected to the end of bombardment), and a synthesis time of 20-25 min. Copyright
Single-step, highly active, and highly selective nanoparticle catalysts for the hydrogenation of key organic compounds
Raja, Robert,Khimyak, Tetyana,Thomas, John Meurig,Hermans, Sophie,Johnson, Brian F. G.
, p. 4638 - 4642 (2007/10/03)
Pores for cluster catalysts: Nanoparticles of both Ru5Pt and Ru10Pt2, uniformly distributed along the inner walls of mesoporous silica, exhibit high catalytic performance in the single-step hydrogenation of dimethyl terephthalate (DMT, to 1,4-cyclohexanedimethanol (CHDM); see scheme), of benzoic acid (to cyclohexane carboxylic acid), and of naphthalene (in the presence of sulfur) to cisdecalin.
Methylation of Alcohols, Phenols, and Carboxylic Acids, and Selective Monomethylation of Diols and Dicarboxylic Acids with Dimethyl Sulfate by Use of Alumina
Ogawa, Haruo,Ichimura, Youko,Chihara, Teiji,Teratani, Shousuke,Taya, Kazuo
, p. 2481 - 2484 (2007/10/02)
Alcohols in cyclohexane give their methyl ethers in high yields by the use of a combination of dimethyl sulfate and alumina.Some diols and dicarboxylic acids adsorbed on alumina react with dimethyl sulfate and produce the corresponding monomethyl ethers and esters in high selectivities.
