698982-50-2Relevant academic research and scientific papers
Ultrasound and water-mediated synthesis of bis-thiazoles catalyzed by Fe(SD)3 as Lewis acid-surfactant-combined catalyst
Parvizi, Jafar,Mahmoodi, Nosrat O.,Ghanbari Pirbasti, Fateme
, p. 140 - 150 (2017/11/20)
Preparation of bis-aminothiazoles under different conditions including synthesis in EtOH under ultrasound irradiation and also in water in the presence of Fe(SD)3 as Lewis acid-surfactant-combined catalyst (LASC) under ultrasound irradiation has been studied. The results were compared with the traditional reflux method. Also, the results confirmed the efficiency of the synthesis in water and under ultrasound irradiation technique. Moreover, the antibacterial activity of products was investigated using the well-diffusion method against bacterial strains including Micrococcus luteus, Escherichia coli, Pseudomonas aeruginosa and Bacillus subtilis. All of the products showed good antibacterial activity against M. luteus and E. coli. Most of the products showed antibacterial activity higher than erythromycin against M. luteus, E. coli, and B. subtilis.
Rational Design and Synthesis of Novel Dimeric Diketoacid-Containing Inhibitors of HIV-1 Integrase: Implication for Binding to Two Metal Ions on the Active Site of Integrase
Long, Ya-Qiu,Jiang, Xiao-Hua,Dayam, Raveendra,Sanchez, Tino,Shoemaker, Robert,Sei, Shizuko,Neamati, Nouri
, p. 2561 - 2573 (2007/10/03)
Discovery of diketoacid-containing compounds as HIV-1 integrase (IN) inhibitors played a major role in validating this enzyme as an important target for the development of therapeutics against HIV infection. In fact, S-1360, the first clinically used IN inhibitor containing a triazole ring as a bioisostere of a carboxylic acid moiety belongs to this class of compounds. To understand the role of divalent metal-chelating in the inhibition of IN (J. Med. Chem. 2002, 45, 5661-5670), we designed and synthesized a series of novel dimeric diketo-containing compounds with the notion that such dimeric compounds may simultaneously bind to two divalent metal ions on the active site of IN. We rationalized that the two diketo subunits separated by uniquely designed linkers can potentially chelate two metal ions that are either provided from one IN active site or two active sites juxtaposed together in a higher order tetramer. Herein, we show that all the new compounds are highly potent against purified IN with varied selectivity for strand transfer, and that some of the analogues exert potent inhibition of the cytopathic effect of HIV-1 in infected CEM cells. This study represents the first attempt to rationally target two divalent metal ions on the active site of IN and may have potential implications for the design of second generation diketoacid-containing class of inhibitors.
