139413-75-5Relevant academic research and scientific papers
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
Ir-Catalyzed Asymmetric Hydrogenation of α-Alkylidene β-Lactams and Cyclobutanones
Xia, Jingzhao,Nie, Yu,Yang, Guoqiang,Liu, Yangang,Gridnev, Ilya D.,Zhang, Wanbin
supporting information, p. 612 - 618 (2018/06/22)
Chiral β-lactams and cyclobutanones are present in numerous natural and pharmaceutical products. The stereoselective construction of chiral four-membered cyclic compounds is an ongoing challenge for the chemical community. Herein, we report a highly stere
Efficient synthesis of N-allylated 2-nitroiminoimidazolidine analogues from Baylis–Hillman bromides
Kumar, Sriramoju Bharath,Pavan Kumar, Chebolu Naga Sesha Sai,Santhoshi, Amlipur,Kumar, Koochana Pranay,Murthy,Jayathirtha Rao, Vaidya
, p. 131 - 136 (2017/01/11)
Various Baylis–Hillman–derived new N-allylated 2-nitroiminoimidazolidine analogs were efficiently prepared using potassium carbonate as base. Simple workup procedure, excellent yields, and mild reaction conditions are the salient features of this method. All the synthesized compounds are screened for their larvicidal activity on fourth instar mosquito larvae, Culex quinquefasciatus.
Design, synthesis and evaluation of 3-arylidene azetidin-2-ones as potential antifungal agents against Alternaria solani Sorauer
Delong, Wang,Yongling, Wu,Lanying, Wang,Juntao, Feng,Xing, Zhang
, p. 6661 - 6673 (2017/11/17)
A new concise and facile method was explored to synthesize a collection of new 3-arylidene azetidin-2-ones, which could be regarded as the derivatives of the hybrid scaffold of bioactive natural cinnamamide and heterocycle azetidi-2-one. The structures of
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
An efficient synthesis of dihydrobenzo[c]azepines from Morita-Baylis-Hillman adducts via Pictet-Spengler reaction
Moon, Hye Ran,Kim, Su Yeon,Roh, Hwa Jung,Kim, Jae Nyoung
supporting information, p. 680 - 684 (2016/05/19)
Various dihydrobenzo[c]azepines were synthesized in good yields via Pictet-Spengler cyclization protocol from tosylamide derivatives of Morita-Baylis-Hillman adducts and 1,3,5-trioxane. The synthesis was carried out in the presence of easily removable mon
Synthesis of thio-heterocyclic analogues from Baylis-Hillman bromides as potent cyclooxygenase-2 inhibitors
Santhoshi, Amlipur,Mahendar, Budde,Mattapally, Saidulu,Sadhu, Partha Sarathi,Banerjee, Sanjay Kumar,Jayathirtha Rao, Vaidya
, p. 1952 - 1957 (2014/04/17)
A series of thio-substituted pyrimidine, benzoxazole, benzothiazole and triazole analogues were synthesized from Baylis-Hillman bromides in a clean and efficient way. The synthesized twenty new compounds were subjected to in vitro COX-1 and COX-2 inhibito
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.
Multicomponent cascade assembly for quinolinopyranpyrazole architectures
Bakthadoss, Manickam,Devaraj, Anthonisamy,Kannan, Damodharan
, p. 1505 - 1513 (2014/03/21)
A highly efficient, multicomponent protocol for the construction of functionalized quinolinopyranpyrazole scaffolds with high stereoselectivity has been developed through the application of a domino reaction. All the quinolinopyranpyrazoles were synthesiz
Multicomponent Cascade Assembly for Quinolinopyranpyrazole Architectures
Bakthadoss, Manickam,Devaraj, Anthonisamy,Kannan, Damodharan
, p. 1505 - 1513 (2015/10/05)
A highly efficient, multicomponent protocol for the construction of functionalized quinolinopyranpyrazole scaffolds with high stereoselectivity has been developed through the application of a domino reaction. All the quinolinopyranpyrazoles were synthesiz
