- Homocoupling of bromotriazole derivatives on metal complex catalysts
-
Homocoupling of 4-bromo-1,2,3-triazoles upon treatment with stoichiometric amount of bis(pinacolato)diboron on a palladium catalyst gives 4,4-bi-1,2,3-triazoles in up to 95% yields.
- Afanas?ev,Tsyplenkova,Seliverstov,Sosonyuk,Proskurnina,Zefirov
-
-
Read Online
- Convenient and efficient synthesis of disubstituted piperazine derivatives by catalyst-free, atom-economical and tricomponent domino reactions
-
One-pot, atom-economical, catalyst-free and tri-component domino reactions are applied to the diversity-oriented synthesis (DOS) of disubstituted piperazine derivatives under mild conditions with moderate to high yields. This protocol exhibits potential a
- Dong, Hong-Ru,Chen, Zi-Bao,Li, Rong-Shan,Dong, Heng-Shan,Xie, Zhi-Xiang
-
-
Read Online
- Primary discovery of 1-aryl-5-substituted-1H-1,2,3-triazole-4-carboxamides as promising antimicrobial agents
-
Three series of novel 1H-1,2,3-triazole-4-carboxamides: 1-aryl-5-alkyl/aryl-1H-1,2,3-triazole-4-carboxamides, 1-aryl-5-amino-1H-1,2,3-triazole-4-carboxamides and 1,2,3-triazolo[1,5-a]quinazoline-3-carboxamides were synthesized via base-mediated click azide reactions. Compounds were evaluated for their antimicrobial activities against primary pathogens: Gram-positive and Gram-negative bacterial strains Escherichia coli, Klebsiella pneumonia, Acinetobacter baumannii, Pseudomonas aeruginosa, Staphylococcus aureus, as well as fungal strain Cryptococcus neoformans var. grubii and Candida albicans. Compounds exhibiting moderate to good activities were selected for SAR analysis. Several 5-methyl-1H-1,2,3-triazole-4-carboxamides 4d, 4l, 4r, showed potent antibacterial effect against S. aureus. On the contrary, 5-amino-1H-1,2,3-triazole-4-carboxamide 8b and [1,2,3]triazolo[1,5-a]quinazoline-3-carboxamide 9a were active against pathogenic yeast C. albicans. Thus, compound 4l under 1 μM demonstrated 50% growth inhibition against S. aureus. At the same concentration, the compound 9a killed approx. 40% of C. albicans cells. In general, these compounds demonstrated selective action and no significant impact on the viability of human keratinocytes of HaCaT line.
- Finiuk, Nataliya,Klyuchivska, Olha,Manko, Nazar,Matiychuk, Vasyl,Obushak, Mykola,Pokhodylo, Nazariy,Stoika, Rostyslav
-
-
- DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis
-
Visceral leishmaniasis (VL) is a parasitic disease endemic across multiple regions of the world and is fatal if untreated. Current therapies are unsuitable, and there is an urgent need for safe, short-course, and low-cost oral treatments to combat this ne
- Bello, Davide,Braillard, Stéphanie,Caljon, Guy,Carvalho, Sandra,Corpas-Lopez, Victoriano,Freund, Yvonne,Gilbert, Ian H.,Glossop, Paul A.,Jacobs, Robert T.,Lukac, Iva,Maes, Louis,Mowbray, Charles E.,Nare, Bakela,Pandi, Bharathi,Patterson, Stephen,Speake, Jason,Van Den Kerkhof, Magali,Wall, Richard J.,Whitlock, Gavin A.,Wyllie, Susan,Yardley, Vanessa,Zuccotto, Fabio
-
p. 16159 - 16176
(2021/11/16)
-
- Picolinamide compound containing triazole or quinolinone structure and application of picolinamide compound
-
The invention provides a picolinamide compound containing a triazole or quinolinone structure and application of the picolinamide compound. According to a technical scheme in the invention, extensiveresearch is conducted on the picolinamide compound, and
- -
-
Paragraph 0104; 0123-0124
(2020/01/12)
-
- 1,2,3-triazole based Cu2+ colorimetric sensor: Synthesis and characterization
-
A new simple organic scaffold based on 1,2,3-triazole fused imidazole derivative (L) was designed and synthesized and structure was confirmed by usual spectral techniques. The chromogenic properties of L toward different metal ions were investigated in mi
- Senthilkumaran,Senthil
-
p. 361 - 366
(2020/01/03)
-
- Design, synthesis and anticancer activity evaluation of aziridine-1,2,3-triazole hybrid derivatives
-
New 1-aryl-4-[(aziridine-1-yl)diarylmethyl]-5-methyl-1H-1,2,3-triazole derivatives 7a-i were synthesized by a one-pot reaction of diaryl-(1-aryl-5-methyl-1H-1,2,3-triazol-4-yl)methanols 6a-i derived from 1-aryl-5-methyl-1H-1,2,3-triazole-4-carboxylic acid
- Dong, Hong-Ru,Wu, Jian-Guo
-
p. 109 - 112
(2018/04/25)
-
- NOVEL OXABOROLE ANALOGS AND USES THEREOF
-
This application describes compounds, compositions, and methods which are useful in treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a parasite.
- -
-
-
- Discovery of novel pyrrolopyrimidine/pyrazolopyrimidine derivatives bearing 1,2,3-triazole moiety as c-Met kinase inhibitors
-
Six series of pyrrolo[2,3-d]pyrimidine and pyrazolo[3,4-d]pyrimidine derivatives bearing 1,2,3-triazole moiety were designed and synthesized, and some bio-evaluation was also carried out. As a result, four points can be summarized: Firstly, some of compounds exhibited excellent cytotoxicity activity and selectivity with the IC50 values in single-digit μm level. In particular, the most promising compound 16d showed equal activity to lead compound foretinib against A549, HepG2, and MCF-7 cell lines, with the IC50 values of 4.79?±?0.82, 2.03?±?0.39, and 2.90?±?0.43?μm, respectively. Secondly, the SARs and docking studies indicated that the in vitro antitumor activity of pyrrolo[2,3-d]pyrimidine derivatives bearing 1,2,3-triazole moiety was superior to the pyrazolo[3,4-d]pyrimidine derivatives bearing 1,2,3-triazole moiety. Thirdly, three selected compounds (16d, 18d, and 20d) were further evaluated for inhibitory activity against the c-Met kinase, and the 16d could inhibit the c-Met kinase selectively by experiments of enzyme-based selectivity. What is more, 16d could induce apoptosis of HepG2 cells and inhibitor the cell cycle of HepG2 on G2/M phase by acridine orange staining and cell cycle experiments, respectively.
- Wang, Linxiao,Liu, Xiaobo,Duan, Yongli,Li, Xiaojing,Zhao, Bingbing,Wang, Caolin,Xiao, Zhen,Zheng, Pengwu,Tang, Qidong,Zhu, Wufu
-
p. 1301 - 1314
(2018/05/14)
-
- Synthesis and antibacterial activity of di-heteryl substitued [1,2,4]triazolo [3,4-b] [1,3,4]thiadiazoles
-
A new series of 3-(5-methyl-1-phenyl-1H-4-pyrazolyl)-6-(5-methyl-1-aryl-1H-1,2,3-triazol-4-yl)[1,2,4]triazolo [3,4-b][1,3,4]thiadiazoles 12a-j have been prepared and assayed for their antibacterial activity against human pathogenic Gram-positive bacteria viz., Staphylococcus aureus, Bacillus subtilis and Gram-negative Escherichia coli. Among the screened compounds 12b, 12c and 12f, in which phenyl ring of triazole moiety bear 4-chloro, 4-nitro and 4-fluoro substituents respectively, showed high activity against all the micro-organisms employed. The activities of these compounds are almost equal to the standards.
- Sanjeeva Reddy,Vani Devi,Sunitha,Kalyani,Nagaraj
-
p. 590 - 597
(2017/01/18)
-
- Discovery of novel pyrrolo[2,3-b]pyridine derivatives bearing 1,2,3-triazole moiety as c-Met kinase inhibitors
-
A series of novel pyrrolo[2,3-b]pyridine derivatives bearing 1,2,3-triazole moiety were designed, synthesized, and evaluated for their c-Met kinase inhibitory activities and antiproliferative activities against 4 cancer cell lines (HT-29, A549, MCF-7, and PC-3) in vitro. Most compounds showed moderate to excellent potency, with the most promising analog 34 showing a c-Met IC50value of 1.68?nM. Structure–activity relationship studies indicated that electron-withdrawing groups (X?=?CF3, R1?=?F, R2?=?4-F) were required to decrease the higher electron density on the 5-atom linker to a proper degree to improve the inhibitory activity.
- Tang, Qidong,Wang, Linxiao,Tu, Yayi,Zhu, Wufu,Luo, Rong,Tu, Qidong,Wang, Ping,Wu, Chunjiang,Gong, Ping,Zheng, Pengwu
-
p. 1680 - 1684
(2016/07/27)
-
- Synthesis and anticancer activity evaluation of new 1,2,3-triazole-4- carboxamide derivatives
-
Anticancer screening of several novel 1,2,3-triazoles has been performed. The 1,2,3-triazole derivatives were synthesized from available starting materials according to the convenient synthetic procedures using a multicomponent reaction which gave a wide
- Pokhodylo, Nazariy,Shyyka, Olga,Matiychuk, Vasyl
-
p. 2426 - 2438
(2014/05/06)
-
- Discovery and biological evaluation of novel 6,7-disubstituted-4-(2-fluorophenoxy)quinoline derivatives possessing 1,2,3-triazole-4-carboxamide moiety as c-Met kinase inhibitors
-
A series of 6,7-disubstituted-4-(2-fluorophenoxy)quinoline derivatives possessing 1,2,3-triazole-4-carboxamide moiety were designed, synthesized and evaluated for their in vitro biological activities against c-Met kinase and five typical cancer cell lines (A549, H460, HT-29, MKN-45 and U87MG). Most compounds showed moderate to excellent antiproliferative activity. In this study, a promising compound 34, with a c-Met IC50 value of 1.04 nM, was identified as a multitargeted receptor tyrosine kinase inhibitor. The SAR analyses indicated that compounds with halogen group, especially fluoro group, at 4-position on the phenyl ring (moiety B) have potent antitumor activity, and methylation on the 5-atom linker played an important role in the c-Met enzymatic activity.
- Zhou, Shunguang,Liao, Huimin,Liu, Mingmei,Feng, Guobing,Fu, Baolin,Li, Ruijuan,Cheng, Maosheng,Zhao, Yanfang,Gong, Ping
-
p. 6438 - 6452
(2015/02/02)
-
- Synthesis and characterization of some new 1,2,4-triazines containing 1,2,3-triazole
-
A series of 3-(1 -aryl-1 H-1,2,3-triazol-4-yl)-6-phenyl-1,2,4-triazines were synthesized by the reaction of 1-aryl-1tf-1,2,3-triazole-4-carbohydrazide with 2-bromo-1- phenylethanone and sodium acetate in refluxed EtOH and AcOH. Their structures were chara
- Wang, Yan-Fei,Dong, Hong-Ru,Li, Rong-Shan,Dong, Heng-Shan
-
-
- Chemoselective reaction of aryl azides with ethyl 3-oxo-4- (triphenylphosphor- anylidene) butanoate
-
The reaction of aryl azides with ethyl 3-oxo-4-(triphenylphosphoranylidene) butanoate has been studied under different conditions and it was found that the reaction occurs chemoselectively to form one of two possible isomers. Novel (1H-1,2,3-triazol-5-yl)
- Pokhodylo,Matiychuk,Obushak
-
scheme or table
p. 1469 - 1472
(2010/07/08)
-
- Synthesis of 1,2,4- and 1,3,4-oxadiazoles from 1-aryl-5-methyl-1H-1,2,3- triazole-4-carbonyl chlorides
-
5-Substituted 2-(1-aryl-5-methyl-1H-1,2,3-triazol-4-yl)-1,3,4-oxadiazoles were synthesized by reaction of 1-aryl-5-methyl-1H-1,2,3-triazole-4-carbonyl chlorides with the corresponding 5-substituted 1H-tetrazoles. 5-Methyl-1-phenyl-1H-1,2,3-triazole-4-carb
- Obushak,Pokhodylo,Pidlypnyi,Matiichuk
-
scheme or table
p. 1522 - 1527
(2009/06/28)
-
- 1H and 13C NMR - Spectroscopy of substituted 1,2,3-triazoles
-
1-Aryl-4-carboxy-5-methyl-1,2,3-triazoles were prepared by the condensation of aryl azides with ethyl acetoacetate. The structures of these compounds were characterized by MS, IR and 1H and 13C NMR spectroscopy. The measured and calc
- Sun, Xiao-Wen,Xu, Peng-Fei,Zhang, Zi-Yi
-
p. 459 - 460
(2007/10/03)
-