2101-86-2Relevant articles and documents
Cu(i)-catalyzed microwave-assisted synthesis of 1,2,3-triazole linked with 4-thiazolidinones: A one-pot sequential approach
Kumar, Yogesh,Matta, Akanksha,Kumar, Prashant,Parmar, Virinder S.,Van Der Eycken, Erik V.,Singh, Brajendra K.
, p. 1628 - 1639 (2015)
A novel copper(i) catalyzed, microwave-assisted one-pot, four-component sequential reaction between a propargyloxybenzaldehyde, a substituted phenyl azide, a substituted aniline and thioglycolic acid has been developed for the synthesis of 3-phenyl-2-[4-{
Synthesis of new anticancer and anti-inflammatory isoxazolines and aziridines from the natural (-)-deltoin
Znati, Mansour,Debbabi, Meriem,Romdhane, Anis,Ben Jannet, Hichem,Bouajila, Jalloul
, p. 1700 - 1712 (2018)
Objectives: This work describes the synthesis, the bioactivity and the structure–activity relationship of new derivatives from a natural coumarin. Methods: (-)-Deltoin 1 and the corresponding isoxazolines and aziridines were characterized by spectroscopic
Selective chemical modification of DNA with alkoxy- and benzyloxyamines
Gjonaj, Lorina,Roelfes, Gerard
, p. 6059 - 6065 (2015)
A new method for the selective chemical modification of DNA at cytosine nucleobases using alkoxy- and benzyloxyamines is presented. It is shown that in particular benzyloxyamines are effective DNA modifying agents, giving rise to almost exclusive formatio
Anti-leishmanial and cytotoxic activities of amino acid-triazole hybrids: Synthesis, biological evaluation, molecular docking and in silico physico-chemical properties
Masood, Mir Mohammad,Hasan, Phool,Tabrez, Shams,Ahmad, Md. Bilal,Yadava, Umesh,Daniliuc, Constantin G.,Sonawane, Yogesh A.,Azam, Amir,Rub, Abdur,Abid, Mohammad
, p. 1886 - 1891 (2017)
According to WHO, leishmaniasis is a major tropical disease, ranking second after malaria. Significant efforts have been therefore invested into finding potent inhibitors for the treatment. In this work, eighteen novel 1,2,3-triazoles appended with L-amin
A mild TCEP-based para-azidobenzyl cleavage strategy to transform reversible cysteine thiol labelling reagents into irreversible conjugates
Maruani, Antoine,Alom, Shamim,Canavelli, Pierre,Lee, Maximillian T. W.,Morgan, Rachel E.,Chudasama, Vijay,Caddick, Stephen
, p. 5279 - 5282 (2015)
It has recently emerged that the succinimide linkage of a maleimide thiol addition product is fragile, which is a major issue in fields where thiol functionalisation needs to be robust. Herein we deliver a strategy that generates selective cysteine thiol
Immobilization of vitamin B1 on the magnetic dialdehyde starch as an efficient carbene-type support for the copper complexation and its catalytic activity examination
Abbaspour, M.,Mohammadi Ziarani, G.,Rafiee, F.
, (2021/11/16)
Since the starch biopolymer is an available and inexpensive matrix with modifiable functionality and stabilization capability for metal ions, in this report, we oxidized it to dialdehyde form for the further functionalization with vitamin B1 as a green σ-donor and π-acceptor carbene type ligand. Immobilization of vitamin B1 on this biopolymer was done through imine bond formation between NH2 groups of aminopyrimidine segment of vitamin B1 and aldehyde functional groups of starch oxide. Thiazolium heterocycle part in this biomolecule provided a carbene type precursor for the metal complexation. After the magnetization process by using of Fe3O4 nanoparticles that lead to quick and facile magnetic separation and metal catalyst recycling, copper ions immobilized on the magnetic support (5.9 wt% Cu, 0.93 mmol/g). The prepared copper N-heterocyclic carbene complex (Fe3O4@DAS@VB1@CuCl nanocomposite) was characterized by FT-IR, SEM, EDX, XRD, VSM, TGA and ICP-OES analysis and then its catalytic activity investigated in azidonation of arylboronic acids and also one-pot coupling reaction of the synthesized aryl azides with phenylacetylene. 1,4-Diaryl 1,2,3-triazoles were obtained in excellent yields (≥90%) at proper reaction times (30–200 min). The magnetic catalyst was recovered by a magnetic field and reused in azidation reaction up to 7 cycle.
Triazole [5, 4-d] pyrimidone tricyclic compounds as well as preparation method and application thereof
-
Paragraph 0064; 0067-0070; 0075, (2021/07/09)
The invention relates to triazole [5, 4-d] pyrimidone tricyclic compounds as well as a preparation method and application thereof.The triazole [5, 4-d] pyrimidone tricyclic compounds are prepared by following steps: taking different substituted anilines a
Structural and Activity Relationships of 6-Sulfonyl-8-Nitrobenzothiazinones as Antitubercular Agents
Chiarelli, Laurent R.,Fan, Dongguang,Han, Quanquan,Lu, Yu,Qiao, Chunhua,Shi, Rui,Stelitano, Giovanni,Wang, Bin,Huszár, Stanislav,Miku?ová, Katarína,Savková, Karin
supporting information, p. 14526 - 14539 (2021/10/26)
The benzothiazinone (BTZ) scaffold compound PBTZ169 kills Mycobacterium tuberculosis by inhibiting the essential flavoenzyme DprE1, consequently blocking the synthesis of the cell wall component arabinans. While extraordinarily potent against M. tuberculosis with a minimum inhibitory concentration (MIC) less than 0.2 ng/mL, its low aqueous solubility and bioavailability issues need to be addressed. Here, we designed and synthesized a series of 6-methanesulfonyl substituted BTZ analogues; further exploration introduced five-member aromatic heterocycles as linkers to attach an aryl group as the side chain. Our work led to the discovery of a number of BTZ derived compounds with potent antitubercular activity. The optimized compounds 6 and 38 exhibited MIC 47 and 30 nM, respectively. Compared to PBTZ169, both compounds displayed increased aqueous solubility and higher stability in human liver microsomes. This study suggested that an alternative side-chain modification strategy could be implemented to improve the druglike properties of the BTZ-based compounds.
Selective CDK4/6 inhibition of novel 1,2,3-triazole tethered acridinedione derivatives induces G1/S cell cycle transition arrest via Rb phosphorylation blockade in breast cancer models
Praveenkumar,Gurrapu, Nirmala,Kolluri, Prashanth Kumar,Shivaraj,Subhashini,Dokala, Appaji
, (2021/10/12)
CDK4 & CDK6 are essential regulators of initial cell cycle phases and are always considered an exciting choice for anti-cancer therapy. In the present study, we presented the structure-based rational design & synthesis of a new class of 1,2,3-triazole tet
Design and synthesis of novel diosgenin-triazole hybrids targeting inflammation as potential neuroprotective agents
Huang, Yi,Huang, Weiwei,Yang, Guixiang,Wang, Rui,Ma, Lei
supporting information, (2021/05/21)
Alzheimer's disease is a progressive neurodegenerative disease, and its incidence is expected to increase as the global population ages. Recent studies provide increasing evidence that inflammation plays a key role in the pathogenesis and progression of AD. Diosgenin, an active ingredient in Dioscorea nipponica Makino, is a promising bioactive lead compound in the treatment of Alzheimer's disease, which exhibited anti-inflammatory activity. To search for more efficient anti-Alzheimer agents, a series of novel diosgenin-triazolyl hybrids were designed, synthesized, and their neuroprotective effects against oxygen-glucose deprivation-induced neurotoxicity and LPS-induced NO production were evaluated. Most of these new hybrids displayed better activities than DIO. In particular, the promising compound L6 not only demonstrated an excellent neuroprotective effect but also showed the best anti-inflammatory activity. The structure-activity relationship study illustrated that the introduction of benzyl or phenyl triazole did improve the activity, and the introduction of benzyl triazole was better than that of phenyl triazole. The results we obtained showed that the diosgenin skeleton could be a promising structural template for the development of new anti-Alzheimer drug candidates, and compound L6 has the potential to be an important lead compound for further research.
