26774-38-9Relevant academic research and scientific papers
Synthesis, physicochemical characterization, cytotoxicity, antimicrobial, anti-inflammatory and psychotropic activity of new N-[1,3-(benzo)thiazol-2-yl]- ω-[3,4-dihydroisoquinolin-2(1H)-yl]alkanamides
Zablotskaya, Alla,Segal, Izolda,Geronikaki, Athina,Eremkina, Tatiana,Belyakov, Sergey,Petrova, Marina,Shestakova, Irina,Zvejniece, Liga,Nikolajeva, Vizma
, p. 846 - 856 (2013)
A series of new N-[(benzo)thiazol-2-yl]-2/3-[3,4-dihydroisoquinolin-2(1H)- yl]ethan/propanamide derivatives was synthesized and characterized by 1H, 13C NMR and IR spectroscopy and mass-spectrometry. A single crystal X-ray study of N
Silyl modification of biologically active compounds. 8. Trimethylsilyl ethers of hydroxyl-containing thiazole derivatives
Zablotskaya,Segal,Germane,Shestakova,Domracheva,Nesterova,Geronikaki,Lukevics
, p. 859 - 866 (2002)
Trimethylsilyl ethers of various hydroxyl-containing thiazole derivatives have been synthesized. The psychotropic activity (in vivo) and the cytotoxicity (in vitro on tumor cell lines HT-1080 and MG-22A) of these ethers and of their unsilylated precursors
Exploring DOXP-reductoisomerase binding limits using phosphonated N-aryl and N-heteroarylcarboxamides as DXR inhibitors
Bodill, Taryn,Conibear, Anne C.,Mutorwa, Marius K.M.,Goble, Jessica L.,Blatch, Gregory L.,Lobb, Kevin A.,Klein, Rosalyn,Kaye, Perry T.
supporting information, p. 4332 - 4341 (2013/07/27)
DOXP-reductoisomerase (DXR) is a validated target for the development of antimalarial drugs to address the increase in resistant strains of Plasmodium falciparum. Series of aryl- and heteroarylcarbamoylphosphonic acids, their diethyl esters and disodium salts have been prepared as analogues of the potent DXR inhibitor fosmidomycin. The effects of the carboxamide N-substituents and the length of the methylene linker have been explored using in silico docking studies, saturation transfer difference NMR spectroscopy and enzyme inhibition assays using both EcDXR and PfDXR. These studies indicate an optimal linker length of two methylene units and have confirmed the importance of an additional binding pocket in the PfDXR active site. Insights into the constraints of the PfDXR binding site provide additional scope for the rational design of DXR inhibitors with increased ligand-receptor interactions.
Substituted thiazoles VI. Synthesis and antitumor activity of new 2-acetamido- and 2 or 3-propanamido-thiazole analogs
El-Messery, Shahenda M.,Hassan, Ghada S.,Al-Omary, Fatmah A.M.,El-Subbagh, Hussein I.
experimental part, p. 615 - 625 (2012/09/21)
A novel series of 2-acetamido and 2 or 3-propanamido derivatives of 4- or 5-substituted-thiazoles was designed and synthesized. Structure elucidation of the new synthesized compounds was attained by the use of 1H & 13C NMR, and Mass
Synthesis and biological evaluation of new thiazolyl/benzothiazolyl-amides, derivatives of 4-phenyl-piperazine
Papadopoulou, Christina,Geronikaki, Athina,Hadjipavlou-Litina, Dimitra
, p. 969 - 973 (2008/09/18)
A series of thiazolyl-N-phenyl piperazines has been synthesised and tested for anti-inflammatory activity. Their RM values were determined as an expression of their lipophilicity. Theoretical calculation of their lipophilicity, as clog P and logPsk also performed. The effect of the synthesised compounds on inflammation, using the carrageenin induced mouse paw oedema model was studied. In general, the studied compounds were found to be potent anti-inflammatory agents (44-74.1%). Anti-inflammatory activity was influenced by some structural characteristics of the synthesised compounds. An attempt was made to correlate their biological activity with some physicochemical parameters using a quantitative structure-activity relationship approach (QSAR).
Aminothiazole derivatives with antidegenerative activity on cartilage
Panico, Anna Maria,Geronikaki, Athina,Mgonzo, Remi,Cardile, Venera,Gentile, Barbara,Doytchinova, Irini
, p. 2983 - 2989 (2007/10/03)
A series of 2-dialkylamino-N-(4-substituted thiazolyl-2)acetamides and 3-dialkylamino-N-(4-substituted thiazolyl-2)propionamides were synthesized and evaluated for their anti-inflammatory activity. Encouraging results led us to investigate the effect of t
Synthesis and biological evaluation of new 4,5-disubstituted-thiazolyl amides, derivatives of 4-hydroxy-piperidine or of 4-N-methyl piperazine
Geronikaki,Hadjipavlou-Litina,Chatziopoulos,Soloupis
, p. 472 - 479 (2007/10/03)
4,5-disubstituted-thizolyl amides, derivatives of 4-hydroxy-piperidine and of 4-N-methyl piperazine, were synthesized and tested as anti-inflammatory agents. Log P values were theoretically calculated and experimentally determined. These compounds were tested for antioxidant activity, as hydroxyl radical scavengers and for their ability to interact with stable 1,1-diphenyl-2-picryl hydrazyl free radical (DPPH). The effect of the synthesized compounds on inflammation, using the carrageenin induced mice paw edema model was studied. Both anti-inflammatory and antioxidant activities depended on some structural characteristics of the synthesized compounds.
