- A chiral oxazoline for catalytic enantioselective Nozaki-Hiyama-Kishi allylation and vinylation of aldehydes
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Asymmetric allylation and vinylation of aldehydes with allyl halides and vinyl halides have been achieved using the chromium(II)-oxazoline catalyst. The catalyst promotes the highly efficient enantioselective Nozaki–Hiyama-Kishi (NHK) allylation of aldehydes using allyl bromide, producing the corresponding homoallylic alcohols in good yields (up to 84%) and a high level of enantioselectivity (up to 98% ee). Meanwhile, the NHK vinylation of aldehydes produce desired allylic alcohols in satisfactory yields (up to 88%) and a high level of enantioselectivity (up to 97% ee). We developed a reliable and milder protocol for preparing chiral homoallylic and allylic alcohols.
- Chen, Chinpiao,Kumbhar, Sharad V.
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- Hydrophobicity-oriented drug design (HODD) of new human 4-hydroxyphenylpyruvate dioxygenase inhibitors
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Involved in the tyrosine degradation pathway, 4-hydroxyphenylpyruvate dioxygenase (HPPD) is an important target for treating type I tyrosinemia. To discover novel HPPD inhibitors, we proposed a hydrophobicity-oriented drug design (HODD) strategy based on the interactions between HPPD and the commercial drug NTBC. Most of the new compounds showed improved activity, compound d23 being the most active candidate (IC50 = 0.047 μM) with about 2-fold more potent than NTBC (IC50 = 0.085 μM). Therefore, compound d23 is a potential drug candidate to treat type I tyrosinemia.
- Ndikuryayo, Ferdinand,Kang, Wei-Ming,Wu, Feng-Xu,Yang, Wen-Chao,Yang, Guang-Fu
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- CLASS OF NEAR INFRARED MOLECULAR PROBES FOR BIOLOGICAL APPLICATIONS
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Methods for preparing 2,5-Bis(benzoxazol-2′-yl)benzene-1,4-diol derivatives (Zinhbo derivatives) are provided. Zinhbo derivatives are used to detect zinc ions and have particular application in vivo and in vitro. Zinhbo derivatives upon excitation give a florescence response emission that can be used to determine the presence of zinc cation in solution. Zinhbo derivatives complexed with zinc cations upon excitation can produce a florescence response emission in the visible and near infrared range. Zinhbo derivatives complexed with zinc cations exhibit a large stoke shift between the excitation and emission wavelengths.
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Paragraph 0098
(2014/10/16)
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- BIS(FLUOROALKYL)-1,4-BENZODIAZEPINONE COMPOUNDS AND PRODRUGS THEREOF
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Disclosed are compounds of Formula (I) and/or salts thereof: wherein R1 is —CH2CH2CF3; R2 is —CH2CH2CF3 or —CH2CH2CH2CF3; R3 is H, —CH3, or Rx; R4 is H or Ry; Ring A is phenyl or pyridinyl; and Rx, Ry, Ra, Rb, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer; or as prodrugs of such compounds.
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Paragraph 0314-0315
(2014/04/03)
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- A versatile synthesis of bis[2-(2'-hydroxylphenyl)benzoxazole] derivatives as zinc sensors
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A versatile synthetic route has been developed to prepare 2, 5-bis(benzoxazole-2-yl)benzene-1,4-diol derivatives 2. Although one of the derivatives (2b) has recently been shown to exhibit an excellent response to Zn2+ cations, the low yielding synthetic route will likely prevent its wide application. This report describes an improved synthetic procedure to obtain 2, thereby making this class of compounds available for biologically relevant studies. An effective synthesis has been developed for 2-aminophenol derivative 6, which bears a carboxylate group in the desired position. The strategy allows construction of bis(benzoxazole) compound 5, where the built-in ester group can be easily converted to either a hydroxymethyl or a bromomethyl group to introduce the zinc-chelating ligand. The Royal Society of Chemistry 2013.
- Wang, Junfeng,Pang, Yi
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p. 10208 - 10212
(2013/09/02)
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- Aminophenoxazinones as inhibitors of indoleamine 2,3-dioxygenase (IDO). synthesis of exfoliazone and chandrananimycin A
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A range of 2-aminophenoxazin-3-ones has been prepared by oxidative cyclocondensation of 2-aminophenols, including the natural products exfoliazone and chandrananimycin A, both synthesized for the first time. The compounds were evaluated for their ability
- Pasceri, Raffaele,Siegel, David,Ross, David,Moody, Christopher J.
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p. 3310 - 3317
(2013/06/04)
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- Stabilization of unique valencies of cobalt, nickel and copper by complexation with the tridentate ligand 2-(2′-pyridyl)-8-hydroxyquinoline Dedicated to Prof. George Christou, on his 60th birthday, an extraordinary and enthusiastic inorganic chemist, and the most supportive mentor i could ever ask for (GM).
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The complexes of cobalt, copper and nickel ions with the known tridentate ligand 2-(2′-pyridyl)-8-hydroxyquinoline (HQP) were prepared and characterized. The structures of the complexes with Co(II), Cu(II) and Ni(III) were corroborated by crystal structure analyses. The structures of the complexes with Co(III) and Cu(I) were realized from NMR measurements in solution. It was found that HQP stabilizes high oxidation states of the complexed metal ions. The results also suggest that HQP binds Cu(II) and Cu(I) in two different modes; Cu(II) forms an octahedral complex with the three elements of the ligand, namely, the 8-hydroxyl the two nitrogens of bipyridine, while Cu(I) binds only to two nitrogens of the bipyridine, yielding a tetra-coordinated complex.
- Maayan, Galia,Dayagi, Yohai,Arad-Yellin, Rina,Shimon, Linda J.W.,Shanzer, Abraham
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p. 365 - 370
(2013/10/08)
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- BENZOXAZOLE CARBOXAMIDE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP)
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A compound having the structure set forth in Formula (I) or Formula (II): wherein the variables Y, R1, R2, R3, and R4 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.
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Page/Page column 55-56
(2009/08/16)
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- In pursuit of natural product leads: Synthesis and biological evaluation of 2-[3-hydroxy-2-[(3-hydroxypyridine-2-carbonyl)amino]phenyl]benzoxazole-4- carboxylic acid (A-33853) and its analogues: Discovery of N-(2-benzoxazol-2- ylphenyl)benzamides as novel
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The first synthesis and biological evaluation of antibiotic 31 (A-33853) and its analogues are reported. Initial screening for inhibition of L. donovani, T. b. rhodesiense, T. cruzi, and P. falciparum cultures followed by determination of IC50
- Tipparaju, Suresh K.,Joyasawal, Sipak,Pieroni, Marco,Kaiser, Marcel,Brun, Reto,Kozikowski, Alan P.
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supporting information; experimental part
p. 7344 - 7347
(2009/12/07)
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- SUBSTITUTED 2-AMINO-FUSED HETEROCYCLIC COMPOUNDS
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The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein: R1, R2, Z1, t, and ring A are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of JNK, such as diabetes, the method comprising administering to a mammal an effective amount of a compound of formula (I).
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Page/Page column 24; 72-73
(2008/06/13)
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- Dual inhibitors of adipocyte fatty acid binding protein and keratinocyte fatty acid binding protein
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Compounds that are dual aP2/k-FABP inhibitors are provided having the formula wherein A, B, X, Y, R1, R2 and R3 are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing dual aP2/k-FABP inhibitors alone or in combination with at least one other antidiabetic agent such as metformin, glyburide, troglitazone and/or insulin.
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- Benzamide analogs useful as PARP (ADP-ribosyltransferase, ADPRT) DNA repair enzyme inhibitors
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A range of 3-oxybenzamide compounds and related quinazolinone compounds are disclosed which can act as potent inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase or PARP enzyme (EC 2.4.2.30), and which thereby can provide useful therapeutic compounds for use in conjunction with DNA-damaging cytotoxic drugs or radiotherapy to potentiate the effects of the latter. The compounds disclosed include 3-benzyloxybenzamides, 3-oxybenzamides in which a chain of 5 or more methylene groups terminate in a halogen atom or in a purin-9-yl moiety, certain benzoxazole-4-carboxamide compounds and certain quinazolinone compounds. In formula X and Y together may form a bride -X-Y- that represents the grouping (a), (b) or (c )wherein R5 is H, alkyl, aryl or aralkyl.
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