145162-51-2Relevant academic research and scientific papers
Boron carbonitride photocatalysts for direct decarboxylation: The construction of C(sp3)-N or C(sp3)-C(sp2) bonds with visible light
Shi, Jiale,Wang, Rong,Wang, Xinchen,Yuan, Tao,Zheng, Meifang
supporting information, p. 3945 - 3949 (2021/06/17)
A metal-free protocol is established for the decarboxylative N-H or C(sp2)-H functionalization of acidsviametal-free boron carbon nitride (BCN) photocatalysis, delivering the desired products under ambient conditions. This methodology is applicable to the late-stage modification of pharmaceutical molecules and gram-scale experiments as well as in the recovery and reuse of the photocatalysts without the loss of reactivity. The developed photochemical reaction system fulfills the requirements of green and sustainable chemistry.
NEW THIENOPYRIMIDINE DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Page/Page column 132; 167, (2015/07/15)
Compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R12, X, A and n are as defined in the description.
Suzuki-miyaura cross-coupling of potassium trifluoro(N -methylheteroaryl) borates with aryl and heteroaryl halides
Molander, Gary A.,Ryu, Daweon,Hosseini-Sarvari, Mona,Devulapally, Rammohan,Seapy, Dave G.
, p. 6648 - 6656 (2013/07/26)
The synthesis of potassium trifluoro(N-methylheteroaryl)borates and their use in cross-coupling reactions with various aryl and heteroaryl halides to construct N-methyl heteroaryl-substituted aromatic and heteroaromatic compounds are reported.
Non-nucleoside inhibitors of BasE, an adenylating enzyme in the siderophore biosynthetic pathway of the opportunistic pathogen Acinetobacter baumannii
Neres, Jo?o,Engelhart, Curtis A.,Drake, Eric J.,Wilson, Daniel J.,Fu, Peng,Boshoff, Helena I.,Barry, Clifton E.,Gulick, Andrew M.,Aldrich, Courtney C.
, p. 2385 - 2405 (2013/05/08)
Siderophores are small-molecule iron chelators produced by bacteria and other microorganisms for survival under iron limiting conditions such as found in a mammalian host. Siderophore biosynthesis is essential for the virulence of many important Gram-negative pathogens including Acinetobacter baumannii, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Escherichia coli. We performed high-throughput screening against BasE, which is involved in siderophore biosynthesis in A. baumannii, and identified 6-phenyl-1-(pyridin-4- ylmethyl)-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid 15. Herein we report the synthesis, biochemical, and microbiological evaluation of a systematic series of analogues of the HTS hit 15. Analogue 67 is the most potent analogue with a KD of 2 nM against BasE. Structural characterization of the inhibitors with BasE reveals that they bind in a unique orientation in the active site, occupying all three substrate binding sites, and thus can be considered as multisubstrate inhibitors. These results provide a foundation for future studies aimed at increasing both enzyme potency and antibacterial activity.
Synthesis and structure-activity relationship of a novel series of heterocyclic sulfonamide γ-secretase inhibitors
Pu, Jun,Kreft, Anthony F.,Aschmies, Suzan H.,Atchison, Kevin P.,Berkowitz, Joshua,Caggiano, Thomas J.,Chlenov, Micheal,Diamantidis, George,Harrison, Boyd L.,Hu, Yun,Huryn, Donna,Steven Jacobsen,Jin, Mei,Lipinski, Kerri,Lu, Peimin,Martone, Robert L.,Morris, Koi,Sonnenberg-Reines, June,Riddell, Dave R.,Sabalski, Joan,Sun, Shaiu-Ching,Wagner, Erik,Wang, Yiqun,Xu, Zheng,Zhou, Hua,Resnick, Lynn
body text, p. 4708 - 4717 (2009/10/23)
γ-Secretase inhibitors have been shown to reduce the production of β-amyloid, a component of the plaques that are found in brains of patients with Alzheimer's disease. A novel series of heterocyclic sulfonamide γ-secretase inhibitors that reduce β-amyloid levels in cells is reported. Several examples of compounds within this series demonstrate a higher propensity to inhibit the processing of amyloid precursor protein compared to Notch, an alternative γ-secretase substrate.
HETEROCYCLIC MODULATORS OF TGR5
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Page/Page column 63; 81, (2008/12/06)
The present invention relates to heterocyclic compounds useful as modulators of TGR5 and methods for the treatment of prevention of metabolic, cardiovascular, and inflammatory diseases.
4-Methoxybenzyl (PMB), a versatile protecting group for the regiospecific lithiation and functionalization of pyrazoles
Subramanyam
, p. 761 - 774 (2007/10/02)
The use of 4-methoxybenzyl (PMB) protecting group for the regiospecific metallation/functionalisation of pyrazole is reported.
Porphyrins with four azole substituents in meso positions: X-ray crystal structure of meso-tetrakis-(1-benzylpyrazol-4-yl)-porphyrin at 200 K
Werner, Andreas,Sanchez-Migallon, Ana,Fruchier, Alain,Elguero, Jose,Fernandez-Castano, Cristina,Foces-Foces, Concepcion
, p. 4779 - 4800 (2007/10/02)
Several new porphyrins have been prepared in improved yields using an established method which was adapted to formylpyrazoles bearing on the pyrazole N1-nitrogen protective groups. The deprotection of N-para-methoxybenzyl and SEM protected meso
Discovery of 6,11-ethano-12,12-diaryl-6,11-dihydrobenzo[b]quinolizinium cations, a novel class of N-methyl-D-aspartate antagonists
Subramanyam,Mallamo,Dority Jr.,Earley,Kumar,Aimone,Ault,Miller,Luttinger,DeHaven-Hudkins
, p. 21 - 27 (2007/10/02)
6,11-Ethano-12,12-diaryl-6,11-dihydrobenzo[b]quinolizinium cations 8, a novel class of N-methyl-D-aspartate (NMDA) antagonists acting at the phencyclidine site, have been identified. Structure-activity relationship studies around the lead compound 8a led
Research in the Azole Series. Synthesis and 13C NMR Study of Pyrazole-4-carboxaldehydes
Echevarria, Aurea,Elguero, Jose,Meutermans, Wim
, p. 957 - 960 (2007/10/02)
Ten new pyrazoles have been prepared and their 13C nmr chemical shifts compared with those of twelve other pyrazoles, some of them prepared purposely for this study.The chemical shifts are discussed statistically assuming that they are additive.A formyl group in the position 4 of the pyrazole ring produces a large effect on carbon C4 (SCS = 17.3 ppm) and medium effects on carbons C3 (SCS = 1.9 ppm) and C5 (SCS = 3.8 ppm).The azines derived from pyrazole-4-carboxaldehydes are of the E,E-configuration.
