280113-67-9Relevant academic research and scientific papers
Novel isoniazid embedded triazole derivatives: Synthesis, antitubercular and antimicrobial activity evaluation
Dixit, Prashant P.,Haval, Kishan P.,Haval, Nitin B.,Kasare, Sanghratna L.,Khedkar, Vijay M.,Patil, Pravin S.,Rekha, Estharla Madhu,Sriram, Dharmarajan
, (2020)
In the present study, a series of new isoniazid embedded triazole derivatives have been synthesized. These compounds were evaluated for their in vitro antitubercular and antimicrobial activities. Among the screened compounds, six have exhibited potent antitubercular activity against Mycobacterium tuberculosis H37Rv strain with MIC value 0.78 μg/mL, whereas, three compounds have displayed activity with MIC value ranging from 1.56 to 3.125 μg/mL. The cytotoxicity of the active compounds was studied against RAW 264.7 cell line by MTT assay and no toxicity was observed even at 25 μg/mL concentration. The five compounds have displayed good antimicrobial activities. Molecular docking have been performed against mycobacterial InhA enzyme to gain an insight into the plausible mechanism of action which could pave the way for our endeavor to identify potent antitubercular candidates. We believe that further optimization of these molecules may lead to potent antitubercular agents.
Copper(I)-Catalyzed Intramolecular Cyclization of o-Propargyloxy Diketopiperazines to Access Diverse Diazabicyclic and Spiro-Diketopiperazinochromanes
Armaghan, Mahsa,Balalaie, Saeed,Bijanzadeh, Hamid Reza,Frank, Walter,Manavi, Bita,Rominger, Frank,Tejeneki, Hossein Zahedian
supporting information, p. 4190 - 4196 (2021/08/06)
In this report, two distinctive intramolecular cyclizations of o-propargyloxy diketopiperazines (achieved from a one-pot Ugi post-transformation) is achieved via a copper(I)-catalyzed intramolecular reaction of azomethine ylide and alkyne moiety. The presence of internal alkyne in the starting materials directed the reaction towards through [3+2]-cycloaddition, while terminal alkyne led to a spirocyclization reaction between azomethine ylide and terminal unsaturated C?C bond. This method offering an opportunity for the synthesis of challenging Diazabicyclics and Spiro-Diketopiperazinochromanes in high yields with exclusive diastereoselectivity. (Figure presented.).
CuI/Cu(OSO2CF3)2 catalysed convenient approach to dichromenopyridines and triazole-thiazole appended chromone derivatives
Yerrabelly, Jayaprakash Rao,Porala, Subbanarasimhulu,Kasireddy, Venkateshwar Reddy,Ghojala, Venkat Reddy,Rebelli, Pradeep
, p. 3781 - 3790 (2021/11/01)
A variety of new pentacyclic dichromenopyridines have been synthesized from 2-amino chromone and O-propargyloxy salicilaldehydes through intramolecular Povarov reaction using CuI/Cu(OSO2CF3)2 as a Lewis acid catalyst. The
Synthesis, characterization, PASS prediction and in silico ADME studies of ester and ether linked 1,4-disubstituted 1,2,3-triazoles derivatives via click approach
Krishnaswamy,Raghuram Shetty,Roopa,Banu, Salma,Preritha,Rajeshwari,Ravikumar,Pruthviraj,Aruna Kumar,Sreenivasa
, p. 1857 - 1864 (2020/09/02)
In the present investigation, we focused our interest on the synthesis of pharmacophoric units (quinoline and 1,2,3-triazole) linked through ester (3a-b) and (substituted aromatic ring and 1,2,3-triazole) linked through an ether (3c-h). The synthesis invo
Synthesis and spectral study of a new family of 2,5-diaryltriazoles having restricted rotation of the 5-aryl substituent
Tsyrenova, Biligma,Nenajdenko, Valentine
, (2020/02/11)
Efficient synthesis of 2,5-diaryl substituted 4-azido-1,2,3-triazoles by the reaction of sodium azide with dichlorosubstituted diazadienes was demonstrated. The optical properties of the prepared azidotriazoles were studied to reveal a luminescence maximu
Synthesis of coumarin-sulfonamide derivatives and determination of their cytotoxicity, carbonic anhydrase inhibitory and molecular docking studies
Zengin Kurt, Belma,Sonmez, Fatih,Ozturk, Dilek,Akdemir, Atilla,Angeli, Andrea,Supuran, Claudiu T.
, (2019/09/30)
Carbonic anhydrases isoforms CA IX, and XII are known to be highly expressed in various human tissues and malignancies. CA IX is a prominent target for especially colorectal cancers, because it is overexpressed in colorectal cancer and this overexpression
Coumarin-1,2,3-triazole hybrid derivatives: Green synthesis and DFT calculations
Nouraie, Pegah,Moradi Dehaghi, Shahram,Foroumadi, Alireza
, p. 386 - 394 (2019/01/19)
A series of new 1,2,3-triazole-coumarin hybrid system are synthesized from the click reaction between 3-azido coumarin and different aromatic terminal alkyne derivatives in a green manner. All compounds are characterized by IR, NMR and UV–VIS spectroscopy
Gold-catalyzed formation of aryl-fused pyrazolooxazepines via intramolecular regioselective 7-exo-dig cyclization
Guduru, Ravinder,Mangina, N. S. V. M. Rao,Sridhar, Balasubramanian,Karunakar, Galla V.
supporting information, p. 2809 - 2817 (2019/03/12)
An efficient method was developed for the synthesis of substituted aryl-fused pyrazolooxazepines from ortho-O-propargyl aryl pyrazoles by gold catalysis. In this organic transformation a new C-N bond was formed regioselectively via 7-exo-dig cyclization.
“On water” cascade synthesis of benzopyranopyrazoles and their macrocycles
Muthusamy, Sengodagounder,Gangadurai, Chinnakuzhanthai
supporting information, p. 1501 - 1505 (2018/03/21)
Reported herein is an intramolecular 1,3-dipolar cycloaddition strategy for rapid entry into benzopyranopyrazoles (BPP) on water medium as “open flask chemistry” approach. The in situ generation of diazo functionality in two-step sequence from the appropr
Synthesis and biological properties of novel 1-methyl-2-(2-(prop-2-yn-1-yloxy)benzylidene) hydrazine analogues
Kivrak, Arif,Yilmaz, Can,Konus, Metin,Koca, Halil,Aydemir, Selahattin,Oagaz, Jeger Ali
, p. 306 - 316 (2018/06/11)
1-Methyl-2-(2-(prop-2-yn-1-yloxy)benzylidene)hydrazine analogues were readily prepared in good yields by the reaction of 2-(prop-2-yn-1-yloxy)benzaldehydes and methyl hydrazine. The reaction tolerates a variety of substituents on the 2-hydroxybenzaldehyde
