76043-35-1Relevant academic research and scientific papers
Pyrazolo[5,1-c][1,2,4]triazoles: Antimicrobial, Antitumor Activities, and Computational Docking Studies
Farghaly, Thoraya A.,Abdallah, Magda A.,Mahmoud, Huda K.,El-Metwaly, Nashwa,Elaasser, Mahmoud
, p. 2859 - 2866 (2017/09/26)
A new series of pyrazolotriazoles 7a–l, 11, and 15a–c derived from the reaction of 3-amino-4-(arylhydrazono)-4,5-dihydropyrazol-5-one 3a,b with various types of hydrazonoyl chlorides 4, 10, 12, and 13 was being synthesized in existence of triethylamine. The spectral data were assured the postulated structures for all compounds. All 7-arylazopyrazolo[5,1-c][1,2,4]triazole derivatives 7a–l, 11, and 15a–c have been evaluated for their antimicrobial and antitumor activities, and the results show that some derivatives have good to mild utility as antitumor and antibacterial operators. Moreover, the computational studies using AutoDock tools 4.2 are confirming the results in biological activity.
Phenyl hydrazone bearing pyrazole and pyrimidine scaffolds: Design and discovery of a novel class of non-nucleoside reverse transcriptase inhibitors (NNRTIs) against HIV-1 and their antibacterial properties
Singh, Udaya Pratap,Bhat, Hans Raj,Verma, Amita,Kumawat, Mukesh Kumar,Kaur, Rajinder,Gupta,Singh, Ramendra K.
, p. 17335 - 17348 (2013/09/24)
A novel series of phenyl hydrazone bearing pyrazole and pyrimidine hybrid compounds has been designed using the molinspiration toolkit based on Lipinski's rule of five and developed via sequential reactions starting from the diazotization of different anilines and further active methylation with acetyl acetone, ethyl acetoacetate and ethyl cyanoacetate to generate hydrazono derivatives. The target hybrid compounds were synthesized on cyclisation of the resulting hydrazono derivatives with hydrazine, phenyl hydrazine and urea. These molecules have been subsequently tested for anti-HIV activity using TZM-bl cell lines. The MTT assay was also carried out for the cytotoxicity determination of the active compounds. Further, to exemplify the key structural features of the molecules, a molecular docking analysis of the most active compounds was performed at the NNIBP of the HIV-RT protein. The antibacterial activity of the target compounds was also determined against a panel of four Gram-positive and four Gram-negative human pathogens. All molecules showed a potent anti-HIV activity along with a prominent inhibition of bacterial organisms.
