4385-76-6Relevant academic research and scientific papers
Mesomorphic properties of 4-(4-pyridyl)-benzoic acid esters
Adomeniene, Ona,Adomenas, Povilas,Gleiznys, Antanas,Poloudina, Lidija,Gotoh, Yasuyuki
, p. 75 - 79 (2001)
Formerly unknown 4-(4-pyridyl)benzoic acid was synthesized and some of its esters were prepared, their mesomorphic properties were examined. Alkyl-esters of the said acid are nonmesomorphic, while three-ring aryl esters form monotropic smectic A state. Esters aren't stable, they hydrolize easily.
Suzuki cross-coupling reactions using reverse-phase glass beads in aqueous media
Lawson Daku, Kokovi M.,Newton, Roger F.,Pearce, Simon P.,Vile, Julia,Williams, Jonathan M. J.
, p. 5095 - 5098 (2003)
Reverse-phase glass beads have been employed in Suzuki reactions to provide, in aqueous media, a route to diverse polar substrates in good yield and with low levels of palladium leaching.
Structure-based drug optimization and biological evaluation of tetrahydroquinolin derivatives as selective and potent CBP bromodomain inhibitors
Bi, Xiaoyang,Chen, Yu,Sun, Zhongya,Lu, Wenchao,Xu, Pan,Lu, Tian,Ding, Hong,Zhang, Naixia,Jiang, Hualiang,Chen, Kaixian,Zhou, Bing,Luo, Cheng
supporting information, (2020/09/16)
CBP bromodomain could recognize acetylated lysine and function as transcription coactivator to regulate transcription and downstream gene expression. Furthermore, CBP has been shown to be related to many human malignancies including acute myeloid leukemia. Herein, we identified DC-CPin734 as a potent CBP bromodomain inhibitor with a TR-FRET IC50 value of 19.5 ± 1.1 nM and over 400-fold of selectivity against BRD4 bromodomains through structure based rational drug design guided iterative chemical modification endeavoring to discover optimal tail-substituted tetrahydroquinolin derivatives. Moreover, DC-CPin734 showed potent inhibitory activity to AML cell line MV4-11 with an IC50 value of 0.55 ± 0.04 μM, and its cellular on-target effects were further evidenced by c-Myc downregulation results. In summary, DC-CPin734 showing good potency, selectivity and anti AML activity could serve as a potent and selective in vitro and in vivo probe of CBP bromodomain and a promising lead compound for future drug development.
Preparing method of porous metal organic frame with small organic molecule fluorescent recognition function
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Paragraph 0027; 0034; 0035, (2017/04/29)
The invention discloses a preparing method of a porous metal organic frame with the small organic molecule fluorescent recognition function. The preparing method includes the following steps that 1, an organic ligand 5-(4-pyridine-4-yl-benzamido)-isophthalic acid (H2PYBI) is synthesized; 2, a Zn-MOF material is synthesized, wherein Zn(NO3)2.6H2O and H2PYBI are weighed, dissolved in solvent, heated in a reaction kettle for reaction and cooled to the room temperature after reaction is finished to obtain the Zn-MOF material; 3, activated complex is prepared, wherein the Zn-MOF material in the heating step 2 to remove guest molecules so as to obtain the activated complex. Compared with the prior art, the porous metal organic frame with the small organic molecule fluorescent recognition function has the structural advantages of high porosity, large specific surface area, regular pore passages and an adjustable skeleton, is high in heat stability and chemical stability and can be directly prepared into a device for detecting nitrobenzene.
PYRROLIDINE OR THIAZOLIDINE CARBOXYLIC ACID DERIVATIVES, PHARMACEUTICAL COMPOSITION AND METHODS FOR USE IN TREATING METABOLIC DISORDERSAS AS AGONISTS OF G- PROTEIN COUPLED RECEPTOR 43 (GPR43)
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Page/Page column 202, (2011/07/07)
The present invention is directed to novel compounds of formula (I) and their use in treating and/or preventing metabolic diseases.
BENZOXAZOLE CARBOXAMIDE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP)
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Page/Page column 74, (2009/08/16)
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.
Structural modifications of salicylates: Inhibitors of human CD81-receptor HCV-E2 interaction
Holzer, Marcel,Ziegler, Sigrid,Neugebauer, Alexander,Kronenberger, Bernd,Klein, Christian D.,Hartmann, Rolf W.
experimental part, p. 478 - 484 (2009/04/04)
Starting point of the present paper was the result of a virtual screening using the open conformation of the large extracellular loop (LEL) of the CD81-receptor (crystal structure: PDB-ID: 1G8Q). After benzyl salicylate had been experimentally validated to be a moderate inhibitor of the CD81-LEL-HCV-E2 interaction, further optimization was performed and heterocyclic-substituted benzyl salicylate derivatives were synthesized. The compounds were tested for their ability to inhibit the interaction of a fluorescence-labeled antibody to CD81-LEL using HUH7.5 cells. No compound showed an increase concerning the inhibition of the protein-protein interaction compared to benzyl salicylate.
Chemical Compounds
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Page/Page column 11, (2008/12/08)
There is provided compounds of Formula (I) and salts, solvates, and physiologically functional derivatives thereof: wherein R1 is hydrogen or C1-6alkyl; n is 1, 2, 3 or 4; R2 is aryl, optionally substituted by one or two groups selected from the group consisting of halogen, hydroxy, cyano, C1-4alkyl, C1-4alkoxy, C1-4alkanoyl, haloC1-4alkyl, haloC1-4alkoxy, aryl, aryloxy, C1-4alkoxycarbonyl, C1-4alkylsulfonyl and a group R3R4NSO2 (wherein R3 and R4 are independently hydrogen or C1-4alkyl) and a 5- or 6-membered heteroaryl group; or n is 0 and R1 and R2, together with the nitrogen atom to which they are joined, form a 5- or 6-membered monocyclic heterocyclic ring or a 9- or 10-membered bicyclic heterocyclic ring wherein at least the ring which contains the nitrogen atom to which R1 and R2 are joined is non-aromatic, and wherein the 5- or 6-membered monocyclic heterocyclic ring or the 9- or 10-membered bicyclic heterocyclic ring is optionally substituted by one or two groups selected from the group consisting of halogen, hydroxy, cyano, oxo, C1-4alkyl, C1-4alkanoyl, C1-4alkoxy, haloC1-4alkyl, haloC1-4alkoxy, aryl, aryloxy and C1-4alkoxycarbonyl; and X is indazolyl, pyrazolyl or a group: wherein G is CH or N; and Y1 and Y2 are independently hydrogen, halogen and a group NR5R6 (wherein R5 and R6 are independently hydrogen, C1-6alkyl or C2-6alkenyl).
Biarylcarboxybenzamide derivatives as potent vanilloid receptor (VR1) antagonistic ligands
Park, Hyeung-Geun,Choi, Ji-Yeon,Kim, Mi-Hyun,Choi, Sea-Hoon,Park, Mi-Kyung,Lee, Jihye,Suh, Young-Ger,Cho, Hawon,Oh, Uhtaek,Kim, Hee-Doo,Joo, Yung Hyup,Shin, Song Seok,Kim, Jin Kwan,Jeong, Yeon Su,Koh, Hyun-Ju,Park, Young-Ho,Jew, Sang-Sup
, p. 631 - 634 (2007/10/03)
Seventeen biarylcarboxybenzamide derivatives were prepared for the study of their agonistic/antagonistic activities to the vanilloid receptor (VR1) in rat DRG neurons. The replacement of the piperazine moiety of the lead compound 1 with phenyl ring showed quite enhanced antagonistic activity. Among the prepared derivatives, N-(4-tert-butylphenyl)-4-pyridine-2-yl-benzamide (2, IC 50 = 31 nM) and N-(4-tert-butylphenyl)-4-(3-methylpyridine-2-yl) benzamide (3g, IC50 = 31 nM), showed 5-fold higher antagonistic activity than 1 in 45Ca2+-influx assay.
New carboxamide compounds having melanin concentrating hormone antagonistic activity, pharmaceutical preparations comprising these compounds and process for their manufacture
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Page/Page column 73, (2010/02/09)
The present invention relates to carboxamide compounds of general formula I wherein the groups and residues A, B, W, X, Y, Z, R1, R2, R3 and k have the meanings given in claim 1. Moreover the invention relates to process for preparing the above mentioned carboxamides as well as pharmaceutical compositions containing at least one carboxamide according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.
