cas 17675-42-2, 4-AMINO-N-CYCLOHEXYLBENZAMIDE

Articles about 17675-42-2Total 9 be found

Discovery of memantyl urea derivatives as potent soluble epoxide hydrolase inhibitors against lipopolysaccharide-induced sepsis
Sepsis, a systemic inflammatory response, caused by pathogenic factors including microorganisms, has high mortality and limited therapeutic approaches. Herein, a new soluble epoxide hydrolase (sEH) inhibitor series comprising a phenyl ring connected to a
Bao, Xuefei,Chen, Guoliang,Du, Fangyu,Hammock, Bruce D.,Liu, Qiu,Liu, Zhongbo,Morisseau, Christophe,Sun, Wenjiao,Wang, Chao,Xiao, Wei,Yang, Hao,Zhang, Tan,Zhou, Jun
(2021)
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sEH inhibitor and preparation method and application thereof
The invention provides an sEH inhibitor and a preparation method and application thereof, and relates to the technical field of endogenous active substance regulation and control. The sEH inhibitor provided by the invention has a structure as shown in a f
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Paragraph 0234; 0236; 0239-0240

(2020/07/28)

Amido pyrimidine compound
The invention provides an amido pyrimidine compound with a novel structure as shown in a formula (I) and a preparation method and application of the amido pyrimidine compound. The amido pyrimidine compound is a compound shown as the formula (I), or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer or tautomer thereof and the like. The amido pyrimidine compound provided bythe invention has a relatively good proliferation inhibition effect on various cancer cells; according to the present invention, the compound has characteristics of low tumor cell inhibition concentration, significantly-improved compound activity, good tumor cell selectivity and good solubility, and is expected to be a specific drug for treatment of malignant tumor cell abnormal proliferation diseases caused by EGFR mutation.
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Paragraph 0215-0217

(2020/06/20)

PURINE AND 3-DEAZAPURINE ANALOGUES AS CHOLINE KINASE INHIBITORS
There are provided substituted purine and 3-deazapurine analogues, which modulate the activity of Choline Kinase (ChoK). The compounds of this invention are therefore useful in treating diseases caused by an altered choline metabolism, such as cancer, cell proliferative disorders, infectious diseases of different origin, immune-related disorders and neurodegenerative disorders. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
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(2018/02/28)

Synthesis and in vitro antiproliferative activity of novel pyrazolo[3,4-d]pyrimidine derivatives
A novel series of pyrazolo[3,4-d]pyrimidine derivatives were designed, synthesized and evaluated for their antiproliferative activity. Among the five compounds selected by NCI, compound 11a showed a distinctive pattern of selectivity on cell line panels and was further screened for a 5-log dose range, where it showed potent antiproliferative activity with median growth inhibition (GI50) equal to 1.71 μM against the CNS cancer SNB-75 cell line. The tested derivative showed remarkably the highest cell growth inhibition against non-small cell lung cancer HOP-62, CNS cancer SNB-75, breast cancer HS578T, and melanoma MALME-3M cell lines. Flow cytometric analysis revealed that compound 11a could significantly induce apoptosis in A549 cells in vitro at low micromolar concentrations. Further investigation showed that compound 11a induced significant cell cycle arrest at G0/G1 phase partly due to its ability to downregulate cyclin D1 and upregulate p27kip1 levels.
Abdou, Nermin S.,Serya, Rabah A. T.,Esmat, Ahmed,Tolba, Mai F.,Ismail, Nasser S. M.,Abouzid, Khaled A. M.
p. 1518 - 1534
(2015/08/18)

Structure-activity relationships in the binding of chemically derivatized CD4 to gp120 from human immunodeficiency virus
The first step in HIV infection is the binding of the envelope glycoprotein gp120 to the host cell receptor CD4. An interfacial "Phe43 cavity" in gp120, adjacent to residue Phe43 of gp120-bound CD4, has been suggested as a potential target for therapeutic intervention. We designed a CD4 mutant (D1D2F43C) for site-specific coupling of compounds for screening against the cavity. Altogether, 81 cysteine-reactive compounds were designed, synthesized, and tested. Eight derivatives exceeded the affinity of native D1D2 for gp120. Structure-activity relationships (SAR) for derivatized CD4 binding to gp120 revealed significant plasticity of the Phe43 cavity and a narrow entrance. The primary contacts for compound recognition inside the cavity were found to be van der Waals interactions, whereas hydrophilic interactions were detected in the entrance. This first SAR on ligand binding to an interior cavity of gp120 may provide a starting point for structure-based assembly of small molecules targeting gp120-CD4 interaction.
Xie, Hui,Ng, Danny,Savinov, Sergey N.,Dey, Barna,Kwong, Peter D.,Wyatt, Richard,Smith III, Amos B.,Hendrickson, Wayne A.
p. 4898 - 4908
(2008/03/11)

Alkoxy- and amidocarbonylation of functionalised aryl and heteroaryl halides catalysed by a Bedford palladacycle and dppf: A comparison with the primary Pd(II) precursors (PhCN)2PdCl2 and Pd(OAc) 2
The versatility of a Bedford-type palladacycle 1, namely [{Pd(-Cl){κ2-P,C-P(OC6H2-2,4- tBu2)(OC6H3-2,4-tBu 2)2}}2], as a primary Pd source, in combination with the ligand bis-1,1′-(diphenylphosphino)ferrocene (dppf) has been established in carbonylation reactions of aryl and heteroaryl bromides with methanol, piperidine and related nucleophiles. Palladacycle 1 has been compared with other primary Pd sources, e.g. (PhCN)2PdCl2 and Pd(OAc)2. The efficacy of the carbonylation processes appear to be linked to the [Pd] concentration, substrate: catalyst ratio, CO pressure and reaction temperature. In amidocarbonylation, double carbonylation is observed for certain organohalides. In the case of 2,5-dibromopyridine, regioselective amination (Hartwig-Buchwald type) also occurs as a side-reaction. This journal is The Royal Society of Chemistry.
Fairlamb, Ian J. S.,Grant, Stephanie,McCormack, Peter,Whittall, John
p. 859 - 865
(2007/10/03)

Anticonvulsant activity of some 4-aminobenzamides
A series of 4-aminobenzamides of some simple primary and secondary amines were prepared and evaluated for anticonvulsant effects. The compounds were tested in mice against seizures induced by electroshock and pentylenetetrazole (metrazole) and in the rotorod assay for neurologic deficit. For those N-alkyl amides tested, 4-amino-N-amylbenzamide was the most potent against maximal electroshock seizures (MES): ED50=42.98 mg/kg; however, the N-cyclohexylbenzamide showed the greatest protective index (PI=TD50/ED50), 2.8. The introduction of a second aromatic ring produced more potent compounds, with d,l-4-amino-N-(α-methylbenzyl)-benzamide showing the highest level of activity. This compound has an anti-MES ED50 of 18.02 mg/kg in mice when administered intraperitoneally (ip) and a TD50 of 170.78 mg/kg (PI=9.5) in the same species. These data compare quite favorably with those for phenobarbital and phenytoin in the same assays.
Clark,Wells,Sansom,et al.
p. 779 - 782
(2007/10/02)