13916-39-7Relevant articles and documents
1-(Carbamoylmethyl)-3H-indolium squaraine dyes: Synthesis, spectra, photo-stability and association with BSA
Wang, Bingshuai,Fan, Jiangli,Sun, Shiguo,Wang, Li,Song, Bo,Peng, Xiaojun
, p. 43 - 50 (2010)
Novel, squarylium dyes containing 1-(alkylcarbamoylmethyl)-2,3,3-trimethyl- 3H-indolium groups were synthesized and their UV/Vis and fluorescence spectra, aggregation, photo-stability and association with bovine serum albumin were studied. The absorption and emission max wavelengths of the dyes in different solvents were in the range 619-653?nm. Compared to a typical ethyl squarylium dye, the introduction of alkylcarbamoylmethyl groups reduced aggregation and improved molar extinction coefficient, fluorescence quantum yield and photo-stability in water. Moreover, the fluorescence intensity of the dyes increased upon the addition of BSA in pH 7.0 phosphate buffer solution. An excellent linear relationship (r2?=?0.9982) was obtained between fluorescence intensity and bovine serum albumin concentration.
Synthesis and characterization of amide-functionalized N-heterocyclic carbene-Pd complexes
Kamisue, Ryo,Sakaguchi, Satoshi
, p. 1910 - 1915 (2011)
Amide-functionalized N-heterocyclic carbene (NHC) precursors such as azolium compounds have been designed and synthesized. Reaction of PdCl 2(CH3CN)2 with the NHC-Ag complex derived from the azolium salt gave [(NHC)PdClsu
Synthesis and Biological Evaluation of 1,2,4-Triazole Thioethers as Both Potential Virulence Factor Inhibitors against Plant Bacterial Diseases and Agricultural Antiviral Agents against Tobacco Mosaic Virus Infections
Fang, Zi-Mian,Guo, Deng-Xuan,Ji, Jin,Liu, Li-Wei,Qi, Pu-Ying,Shao, Wu-Bin,Wang, Jin-Jing,Wang, Pei-Yi,Yang, Song,Zhou, Xiang
, p. 15108 - 15122 (2021/12/27)
Targeting the virulence factors of phytopathogenic bacteria is an innovative strategy for alleviating or eliminating the pathogenicity and rapid outbreak of plant microbial diseases. Therefore, several types of 1,2,4-triazole thioethers bearing an amide l
Quinazoline amide compound and application thereof
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Paragraph 0026; 0030-0032, (2020/05/01)
The invention discloses a quinazoline amide compound. The structural general formula of the quinazoline amide compound is shown as I, wherein R1 and R2 are H or Cl; R3 is selected from n-propyl and benzyl, and the compound shown in the general formula I has excellent biological activity on agricultural harmful mites and can be used for preventing and treating agricultural harmful mites.
Synthesis of E/Z N-(1-Chlorovinyl)formamide Using Vilsmeier–Haack Reaction
Tang, Linlin,Wang, Jingtao,Xia, Xiaojiao,Zuo, Hua,Choi, Kyung-Min,Shin, Dong-Soo
supporting information, p. 243 - 247 (2019/03/14)
Synthesis of a variety of novel Z/E N-(1-chlorovinyl)formamides through Vilsmeier–Haack reaction starting from 2-phenoxyethanamides with POCl3/DMF has been accomplished. The reactions introduced chlorine atom to the Cα-position and p
Rational Design, Synthesis, and Biological Activity of N-(1,4-Benzoxazinone)Acetamide Derivatives as Potent Platelet Aggregation Inhibitors
Xiang, Yi,Wang, Xiu-Hua,Yang, Quan,Tan, Jia-Lian,Jang, Hee-Jae,Zuo, Hua,Shin, Dong-Soo
supporting information, p. 146 - 155 (2018/01/27)
Inappropriate thrombus formation within blood vessels is the leading cause of mortality in the industrialized world. Platelet aggregation activated by thrombin may have close relationship with thrombosis. Based on our studies on the pharmacophoric role of 1,4-benzoxazine-3(4H)-one for desirable platelet aggregation inhibitory activity, we identified N-(4-ethyl-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-7-yl)-2-(4-methylpiperazin-1-yl)acetamide (BOAP-AM6) and N-(4-butyl-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-7-yl)-2-(4-(4-fluorophenyl)piperazin-1-yl)acetamide (BOAP-AM21) as platelet aggregation inhibitors with an IC50 of 8.93 and 8.67 μM, respectively, as potent as the positive control aspirin. A combination of structure–activity relationships studies and molecular modeling revealed that the molecule BOAP-AM6 interacted with the amino acid residue TYR166 and ARG214 in the binding site of GPIIb/IIIa receptor through hydrogen bond and compound BOAP-AM21 acted on the amino acid residue ASN215 and ALA218, both through the same approach as the reported potent molecules 7a and 7b.
Synthesis and acaricidal activities of scopoletin phenolic ether derivatives: Qsar, molecular docking study and in silico Adme predictions
Luo, Jinxiang,Lai, Ting,Guo, Tao,Chen, Fei,Zhang, Linli,Ding, Wei,Zhang, Yongqiang
, (2018/05/04)
Thirty phenolic ether derivatives of scopoletin modified at the 7-hydroxy position were synthesized, and their structures were confirmed by IR,1H-NMR,13C-NMR, MS and elemental analysis. Preliminary acaricidal activities of these compounds against female adults of Tetranychus cinnabarinus (Boisduval) were evaluated using the slide-dip method. The results indicated that some of these compounds exhibit more pronounced acaricidal activity than scopoletin, especially compounds 32, 20, 28, 27 and 8 which exhibited about 8.41-, 7.32-, 7.23-, 6.76-, and 6.65-fold higher acaricidal potency. Compound 32 possessed the the most promising acaricidal activity and exhibited about 1.45-fold higher acaricidal potency against T. cinnabarinus than propargite. Statistically significant 2D-QSAR model supports the observed acaricidal activities and reveals that polarizability (HATS5p) was the most important parameter controlling bioactivity. 3D-QSAR (CoMFA: q2 = 0.802, r2 = 0.993; CoMSIA: q2 = 0.735, r2 = 0.965) results show that bulky substituents at R4, R1, R2 and R5 (C6, C3, C4, and C7) positions, electron positive groups at R5 (C7) position, hydrophobic groups at R1 (C3) and R2 (C4), H-bond donors groups at R1 (C3) and R4 (C6) will increase their acaricidal activity, which provide a good insight into the molecular features relevant to the acaricidal activity for further designing novel acaricidal agents. Molecular docking demonstrates that these selected derivatives display different bide modes with TcPMCA1 from lead compound and they interact with more key amino acid residues than scopoletin. In silico ADME properties of scopoletin and its phenolic ether derivatives were also analyzed and showed potential to develop as good acaricidal candidates.
Evidence of single electron transfer from the enolate anion of an: N, N ′-dialkyldiketopiperazine additive in BHAS coupling reactions
Emery, Katie J.,Tuttle, Tell,Murphy, John A.
, p. 8810 - 8819 (2017/11/03)
A designed N,N′-dialkyldiketopiperazine (DKP) provides evidence for the role of DKP additives as initiators that act by electron transfer in base-induced homolytic aromatic substitution reactions, involving coupling of haloarenes to arenes.
C–C bond-forming reactions of ground-state aryl halides under reductive activation
Emery, Katie J.,Tuttle, Tell,Kennedy, Alan R.,Murphy, John A.
, p. 7875 - 7887 (2016/11/17)
Under basic conditions aryl halides can undergo SRN1 reactions, BHAS reactions and benzyne formations. Appropriate complex substrates afford an opportunity to study inherent selectivities. SRN1 reactions are usually favoured under ph
6-amino-4(3H)-quinazolinone derivatives and their synthesis method and use
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Paragraph 0139; 0140, (2016/12/22)
The invention discloses 6-amino-4(3H)-quinazolinone derivatives and their synthesis method and use and belongs to the technical field of drug synthesis. The invention also relates to a use of the 6-amino-4(3H)-quinazolinone derivatives with a general formula (I) and its synthesis method in medical science, wherein in the general formula (I), X represents (CH2)n-1, n=1 to 10 and R1, R2 and R3 represent different substituents. The invention discloses the compound structures and their synthesis method and external acetylcholinesterase inhibition activity. The 6-amino-4(3H)-quinazolinone derivatives can be further studied and developed to form novel drugs for treating Alzheimer disease.