139413-76-6Relevant articles and documents
Structural exploration of cinnamate-based phosphonic acids as inhibitors of bacterial ureases
Ntatsopoulos, Vassilis,Macegoniuk, Katarzyna,Mucha, Artur,Vassiliou, Stamatia,Berlicki, ?ukasz
, p. 307 - 316 (2018/10/15)
The conjugated system of cinnamic acid, α-substituted with a phosphonoalkyl residue, was previously validated as a scaffold that provided one of the most potent organophosphorus inhibitors of bacterial urease. Following the idea of using Morita-Baylis-Hil
Allylic isothiouronium salts: The discovery of a novel class of thiourea analogues with antitumor activity
Ferreira, Misael,Assun??o, Laura Sartori,Silva, Adny Henrique,Filippin-Monteiro, Fabíola Branco,Creczynski-Pasa, Tania Beatriz,Sá, Marcus Mandolesi
, p. 151 - 158 (2017/02/26)
A series of 28 aryl- and alkyl-substituted isothiouronium salts were readily synthesized in high yields through the reaction of allylic bromides with thiourea, N-monosubstituted thioureas or thiosemicarbazide. The S-allylic isothiouronium salts substitute
Synthesis of 1-benzhydryl piperazine derivatives and evaluation of their ACE inhibition and antimicrobial activities
Santhoshi, Amlipur,Kumar, Singam Naveen,Sujitha, Pombala,Poornachandra, Yedla,Sadhu, Partha Sarathi,Kumar, C. Ganesh,Rao, Vaidya Jayathirtha
, p. 3207 - 3219 (2014/05/06)
This study presents the synthesis of 14 new 1,4-disubstituted piperazine derivatives from allyl bromides of Baylis-Hillman adduct and 4,4-disubstituted benzhydryl piperazines. All the synthesized compounds were further screened for in vitro ACE inhibitor and antimicrobial activities. Among the synthesized piperazine derivatives, compound 12h showed moderate ACE inhibitor activity as compared to the standard, angiotensin-converting enzyme inhibitor (Sigma). The kinetic data (K m, K i and V max values) of enzyme inhibition for compound 12h and ACE inhibitor standard were also determined. Similarly, all compounds were screened against different bacterial strains. Compounds 12a, 12b, 12d, 12h and 12i showed excellent to moderate activity against various tested bacterial strains. Compounds 12b and 12i showed broad spectrum of antibacterial activity against Pseudomonas aeruginosa, Staphylococcus aureus, S. aureus MLS 16, Escherichia coli, Bacillus subtilis and Klebsiella planticola, while compounds 12a, 12d and 12i showed promising activity against P. aeruginosa (MIC value of 8.96 μM), S. aureus (MIC value of 42.2 μM) and S. aureus MLS 16 (MIC value of 81.3 μM), respectively. The remaining compounds showed activity at a concentration of >491 μM.
