5973-84-2Relevant academic research and scientific papers
Chelating competency and electrochemical response of a heterocyclic phenylhydrazone and its copper chelate
Raphael, Vinod P.,Thomas K, Joby,ShajU,Kuriakose, Nimmy
, p. 2099 - 2104 (2014)
Heterocyclic compound 3-acetylpyridine phenylhydrazone (APPH) and its copper chelate were synthesized and characterized by spectral, elemental, magnetic and conductance measurements. Investigations showed that APPH behaved as bidentate ligand during chela
Microwave-Assisted Synthesis and Antimicrobial Activity of Novel Pyrazole–Indanone Hybrid Analogs
Sundergoud, Sh.,Swamy, M. Kumara,Veerasomaiah, P.,Venkatesh, N.
, p. 1635 - 1639 (2020/10/22)
Abstract: A simple and efficient microwave-assisted protocol has been developed for the synthetic of a series of novel pyrazole–indanone hybrid analogs. The target compounds have been synthesized by the Claisen–Schmidt condensation of different 1,3-diphenyl-1H-pyrazole-4-carbaldehydes with 2,3-dihydro-1H-inden-1-one in the presence of potassium hydroxide. The compounds were characterized by IR, 1H and 13C NMR, and mass spectra and were found to exhibit potent antimicrobial activity in vitro.
Design and Synthesis of Imidazole and Triazole Pyrazoles as Mycobacterium Tuberculosis CYP121A1 Inhibitors
Kishk, Safaa M.,McLean, Kirsty J.,Sood, Sakshi,Smith, Darren,Evans, Jack W.D.,Helal, Mohamed A.,Gomaa, Mohamed S.,Salama, Ismail,Mostafa, Samia M.,de Carvalho, Luiz Pedro S.,Levy, Colin W.,Munro, Andrew W.,Simons, Claire
, p. 995 - 1011 (2019/08/06)
The emergence of untreatable drug-resistant strains of Mycobacterium tuberculosis is a major public health problem worldwide, and the identification of new efficient treatments is urgently needed. Mycobacterium tuberculosis cytochrome P450 CYP121A1 is a p
Design, synthesis and biological evaluation of novel 1,3-diarylpyrazoles as cyclooxygenase inhibitors, antiplatelet and anticancer agents
Inceler, Nazan,Ozkan, Yesim,Turan, Nilufer Nermin,Kahraman, Deniz Cansen,Cetin-Atalay, Rengul,Baytas, Sultan Nacak
supporting information, p. 795 - 811 (2018/05/31)
With the aim of achieving new compounds possessing both anti-inflammatory and antiplatelet activities, we synthesized (E)-3-[3-(pyridin-3/4-yl)-1-(phenyl/sulfonylmethylphenyl)-1H-pyrazol-4-yl]acrylamides, and evaluated their COX-1 and COX-2 inhibitory and
Synthesis, docking, in vitro and in vivo antidiabetic activity of pyrazole-based 2,4-thiazolidinedione derivatives as PPAR-γ modulators
Naim, Mohd. Javed,Alam, Ozair,Alam, Md. Jahangir,Shaquiquzzaman, Mohammad,Alam, Md. Mumtaz,Naidu, Vegi Ganga Modi
, (2018/02/12)
The design, synthesis, structure–activity relationship, and biological activity of 2,4-thiazolidinedione derivatives as peroxisome proliferator-activated receptor-γ (PPAR-γ) modulators for antidiabetic activity are reported. Fifteen 2,4-thiazolidinedione
Synthesis and biological evaluation of novel pyrazolic chalcone derivatives as novel hepatocellular carcinoma therapeutics
Hawash, Mohammed M.A.,Kahraman, Deniz Cansen,Eren, Fikriye,Cetin Atalay, Rengul,Baytas, Sultan Nacak
, p. 12 - 26 (2017/02/23)
Despite having the second highest mortality associated with cancer, currently Sorafenib is the only FDA-approved chemotherapeutic agent available for liver cancer patients which can only improve survival for few months. In this study, various pyrazolic ch
Synthesis, cytotoxicity, and molecular properties prediction of novel 1,3-diarylpyrazole derivatives
Baytas, Sultan Nacak,Inceler, Nazan,Yilmaz, Akin
, p. 4893 - 4908 (2013/09/23)
A novel combinatorial library of ester and amide derivatives of 1,3-diarylpyrazoles was designed and synthesized. Anticancer activities of these compounds were assessed against MCF7, MDA-MB-231, HeLa, Raji, and HL60 human cancer cells by MTT assay. Out of
Open vessel and cooling while heating microwave-assisted synthesis of pyridinyl N-Aryl hydrazones
La Regina, Giuseppe,Gatti, Valerio,Piscitelli, Francesco,Silvestri, Romano
experimental part, p. 2 - 6 (2011/04/15)
We reported the first example of open vessel and cooling while heating microwave-assisted synthesis of pyridinyl N-aryl hydrazones. Compounds were prepared in excellent isolated yields (88-98%) in only 5 min, by reacting 4- and 2,4-(di)substituted phenylhydrazines, bearing both electron-donating (4-CH 3, 4-OCH3) and -withdrawing (4-Cl, 4-Br, 4-CF3, 4-NO2, 2,4-Cl2) groups with 2-, 3-, and 4-acetylpyridine. The method was successfully extended to other carbonyl compounds.
Combinatorial synthesis of substituted 3-(2-indolyl)piperidines and 2-phenyl indoles as inhibitors of ZipA-FtsZ interaction
Jennings, Lee D.,Foreman, Kenneth W.,Rush III, Thomas S.,Tsao, Desiree H.H.,Mosyak, Lidia,Kincaid, Scott L.,Sukhdeo, Mohani N.,Sutherland, Alan G.,Ding, Weidong,Kenny, Cynthia Hess,Sabus, Chantel L.,Liu, Hanlan,Dushin, Elizabeth G.,Moghazeh, Soraya L.,Labthavikul, Pornpen,Petersen, Peter J.,Tuckman, Margareta,Ruzin, Alexey V.
, p. 5115 - 5131 (2007/10/03)
The ZipA-FtsZ protein-protein interaction is a potential target for antibacterial therapy. The design and parallel synthesis of a combinatorial library of small molecules, which target the FtsZ binding area on ZipA are described. Compounds were demonstrat
3-Substituted-2-(heteroaryl) indoles
-
, (2008/06/13)
Disclosed as thromboxane synthetase inhibitors are the compounds of formula STR1 wherein R1 represents hydrogen or lower alkyl; Ar represents 3-pyridyl or 1-imidazolyl, each unsubstituted or substituted by lower alkyl, carboxy, lower alkoxycarbonyl or carbamoyl; R2 and R3 independently represent hydrogen, lower alkyl, halogen, trifluoromethyl, hydroxy, lower alkoxy, carboxy lower alkyl, lower alkoxycarbonyl lower alkyl, carboxy, lower alkoxycarbonyl, or lower alkyl-(thio, sulfinyl or sulfonyl), or R2 and R3 together on adjacent carbon atoms represent lower alkylenedioxy; A represents straight chain or branched alkylene of 3 to 12 carbon atoms in which the number of the carbon atoms separating the indole nucleus from group B is 3 to 12, straight chain or branched alkenylene of 2 to 12 carbon atoms, straight chain or branched alkynylene of 2 to 12 carbon atoms, lower alkylenephenylene-lower (alkylene or alkenylene), lower alkylenephenylene, lower alkylene-(thio or oxy)-lower alkylene, lower alkylene-(thio or oxy)-phenylene, or lower alkylene-phenylene-(thio or oxy)-lower alkylene; B represents carboxy, esterified carboxy, carbamoyl, mono- or di-lower alkylcarbamoyl, hydroxymethyl, cyano, hydroxycarbamoyl, 5-tetrazolyl or formyl; the imidazolyl and pyridyl N-oxide thereof; or a pharmaceutically acceptable salt thereof; as well as their synthesis, pharmaceutical compositions thereof, and methods of treatment utilizing such compounds.
