33105-93-0Relevant academic research and scientific papers
Search for the pharamcophore of the K+ channel blocker, apamin
Demonchaux,Granellin,Dunn,Haylett,Jenkinson
, p. 915 - 920 (1991)
The suggestion that the arginine residues, 13Arg and 14Arg, in the octadecapeptide apamin 1 are critically important to its action in blocking Ca2+-dependent K+ channels (and hence part of the 'pharmacophore') has been investigated by examining small peptides containing Arg-Arg or Lys-Arg. Bisguanidine derivatives modelled on the Arg-Arg partial pharmacophore have also been synthesised and tested; in particular, N-(2-guanidinoethyl)-3[N1-(2-guanidinoethyl)carbamoyl]-trans-propena mide 11 and its higher homologue 12. None of the compounds showed more than weak activity (K(i) > 10-5 M) indicating that although the Arg-Arg fragment may be necessary, it is not a sufficient atom grouping for the pharmacophore.
Synthesis of diethylenetriaminepentaacetic acid conjugated inulin and utility for cellular uptake of liposomes
Essien,Lai,Hwang
, p. 898 - 901 (1988)
The synthesis, binding of radioactivity cations, liposomal encapsulation, and biodistribution of the oxidized-insulin reaction product with ethylenediamine and diethylenetriaminepentaacetic acid (4) are described. The four-step synthesis of the inulin derivative proceeded in a good overall yield of 72%. The complex of the inu7lin derivative with either 67Ga3+ or 111In3+ was stable in vivo and di not readily distribute into tissues, being excreted primarily in urine after intravenous administration to mice. The liposome-entrapped inulin derivative can be loaded with radioactive heavy metal cations by mobile ionophores in high radiochemical yields of 80-91%. Following the intravenous administration of the liposomal encapsulation of the indium-111-labeled inulin derivative, the entrapped compound had a biodistribution characteristic of liposomes and allowed an estimation of the extent of the intracellular uptake of liposomes. The ability of the inulin derivative to chelate many different types of metals will allow the use of this probe for studying subtle differences in tissue distribution resulting from different drug targeting or delivery protocols in the same animal by multiple labeling techniques. Moreover, the chelate-conjugated inulin permits studies of the applications of drug delivery systems in primates or human subjects by noninvasive techniques such as γ-scintigraphic or nuclear magnetic resonance imaging methods.
Synthesis and photoluminescence study of di-dendron dendrimers derived from mono-Boc-protected ethylenediamine cores
Zhao, Yili,Liu, Sen,Jiang, Wei,Chang, Yulei,Li, Yapeng,Fang, Xuexun,Wang, Jingyuan
, p. 264 - 270 (2011)
This work is focused on the synthesis and optical properties of cone-shaped structural feature di-dendron polyamidoamine dendrimers up to the third generation with mono-Boc-protected ethylenediamine (EDA) as a core. Strong UV absorbance spectra and fluorescence spectra from di-dendron dendrimers with different terminal groups (-NH2, -COOCH3) were studied under different conditions by varying experimental parameters such as concentration and pH. The optical density and fluorescence intensities increased when di-dendron dendrimers generation number increased from 0.5 to 3.0. It was confirmed that the concentration of di-dendron dendrimers plays an important role in fluorescence intensity. The increase in fluorescence intensity was linear in low concentration regions, but the intensity increased slowly in high concentration regions. The results also showed a rapid increase in fluorescence intensity at low pH. The formation of a fluorescence-emitting moiety had a close relationship to protonated tertiary amine groups in di-dendron dendrimers derived from mono-Boc-protected EDA cores. Furthermore, the formation of fluorescent chemical species was irreversible. Copyright
An inorganic phosphate (Pi) sensor triggers 'turn-on' fluorescence response by removal of a Cu2+ ion from a Cu 2+-ligand sensor: Determination of Pi in biological samples
Hatai, Joydev,Pal, Suman,Bandyopadhyay, Subhajit
, p. 4357 - 4360 (2012)
A fluorescent ligand that displays a high selectivity for Cu2+ has been synthesized. On complexation with Cu2+, the fluorescence of the ligand is quenched. Inorganic phosphate ions decomplex Cu2+ displaying a fluorescence enhancement that can even be seen with naked eyes. The method was successfully used in quantitative determination of inorganic phosphates in serum, urine, and saliva samples.
Formation of a tris(catecholato) iron(iii) complex with a nature-inspired cyclic peptoid ligand
Oh, Jinyoung,Kang, Dahyun,Hong, Sugyeong,Kim, Sun H.,Choi, Jun-Ho,Seo, Jiwon
supporting information, p. 3459 - 3463 (2021/03/22)
Siderophore-mimicking macrocyclic peptoids were synthesized. Peptoid3with intramolecular hydrogen bonds showed an optimally arranged primary coordination sphere leading to a stable catecholate-iron complex. The tris(catecholato) structure of 3-Fe(iii) was determined with UV-vis, fluorescence, and EPR spectroscopies and DFT calculations. The iron binding affinity was comparable to that of deferoxamine, with enhanced stability upon air exposure.
BICYCLIC PEPTIDE LIGANDS AND USES THEREOF
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Paragraph 0495; 0496, (2020/05/14)
The present invention provides compounds, compositions thereof, and methods of using the same.
A cardiovascular drug fasudil hydrochloride intermediate simple synthesis of process
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Paragraph 0016-0018, (2019/05/15)
The invention discloses a cardiovascular drug fasudil hydrochloride intermediate simple synthesis process, taking ethylenediamine, BOC anhydride, DCM into the reaction bottle stirring, GC to intermediate state the reaction is complete, the reaction solution is concentrated under reduced pressure, concentrate, tetrahydrofuran to stir until completely dissolved, addition of sodium methoxide, thermal insulation stirring [...] 1, 3 - dibromo propane, thermal insulation to stir until the reaction is complete, the reaction solution is poured into ice water, extracted with ethyl acetate twice, combined with the organic phase, a washed, dried with anhydrous sodium sulfate, concentrated under reduced pressure to dry, taking concentrated intermediate, 40% sodium hydroxide, ethanol into the reaction bottle stirring, the reaction solution is heated to reflux, thermal insulation reaction to intermediate state hydrolysis, reverse the ice water, for two armor uncle ether extraction, the combined organic phase, a washed, dried with anhydrous sodium sulfate, concentrated under reduced pressure to dry, adding hexane stirring crystallization, to obtain the product, yield 87.0%, GC99%, raw materials of this invention is simple and easy, the product has high purity, simple and convenient operation, the work efficiency is high.
An investigation into the role of 2,6-lutidine as an additive for the RuCl3-NaIO4 mediated oxidative cleavage of olefins to ketones
Watson, David W.,Gill, Matthew,Kemmitt, Paul,Lamont, Scott G.,Popescu, Mihai V.,Simpson, Iain
supporting information, p. 4479 - 4482 (2018/11/23)
2,6-Lutidine has been identified as a beneficial additive for the oxidative cleavage of olefins to ketones by NaIO4 in the presence of catalytic RuCl3, improving the yield and shortening the reaction times. In the absence of 2,6-lutidine reactions stalled at the diol intermediate with incomplete conversion to the desired ketones. The reaction protocol described herein also avoids the use of harmful solvents such as CCl4 and DCE and is tolerant of a range of functional groups.
CHEMICAL BLOWING AGENT AND THERMALLY EXPANDABLE THERMOPLASTIC COMPOSITION
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Page/Page column 27; 28, (2016/07/05)
The present invention relates to a chemical blowing agent comprising at least one tertiary alkyl carbamate. The chemical blowing agent can be activated thermally and is suitable for foaming thermoplastic materials and can for example be incorporated into thermally expandable baffle and/or reinforcement elements which are used in automotive manufacturing and building insulation.
Efficient N-Boc protection of amines by a reusable heterogeneous solid acid nanocatalyst at room temperature
Veisi, Hojat,Sedrpoushan, Alireza,Ghazizadeh, Habibollah,Hemmati, Saba
, p. 1451 - 1461 (2016/04/26)
An efficient and rapid protocol for chemoselective N-Boc protection of various structurally different aryl, aliphatic, and heterocyclic amines is reported with (Boc)2O using mesoporous silica phenylsulfonic acid (SBA-15-Ph-SO3H) as a recyclable and heterogeneous solid acid nanocatalyst under solvent-free condition at ambient temperature. The catalyst can be easily recovered and reused for ten reaction cycles for protection of amines without considerable loss of activity. The advantages of this green method are simplicity, easy workup, chemoselectivity, short reaction time, and excellent yield.
