149267-91-4Relevant academic research and scientific papers
The continuous-flow synthesis of carbazate hydrazones using a simplified computer-vision controlled liquid–liquid extraction system
O'Brien, Matthew,Cooper, Dennis A.,Mhembere, Panashe
supporting information, p. 5188 - 5191 (2016/11/13)
A computer-vision controlled liquid–liquid extraction system was used in the continuous-flow synthesis of a series of carbazate hydrazones. The system uses open-source software components (Python, OpenCV) and is simpler and potentially more economical, in terms of hardware, than one we have described previously.
Synthesis of 5-aryl-3H-[1,3,4]oxadiazol-2-ones from N′-(chloro-aryl- methylene)-tert-butylcarbazates using basic alumina as an efficient and recyclable surface under solvent-free condition
Debnath, Kamalesh,Pathak, Sudipta,Pramanik, Animesh
, p. 896 - 899 (2013/02/25)
The synthesis of biologically important 5-aryl-3H-[1,3,4]oxadiazol-2-ones has been carried out by heating the easily synthesized N′-(chloro-aryl- methylene)-tert-butylcarbazates on basic alumina surface under solvent-free condition. The dual characteristic of basic alumina as a solid support as well as a nucleophile is successfully exploited in these reactions. The method provides special attributions such as reduced reaction times, easier work-up procedures, and good to excellent yields as well as increased purity of products and most importantly environmentally friendly protocols. The basic alumina is easily recovered and utilized for further reactions several times without serious loss of activity.
Thrombin inhibitors built on an azaphenylalanine scaffold
Zega, Anamarija,Mlinsek, Gregor,Solmajer, Tomaz,Trampus-Bakija, Alenka,Stegnar, Mojca,Urleb, Uros
, p. 1563 - 1567 (2007/10/03)
A series of azaphenylalanine derivatives were investigated as novel thrombin inhibitors based on the prodrug principle. By systematic structural modifications we have identified optimal groups for this series that led us to potent inhibitors of thrombin i
Design and structure-activity relationship of thrombin inhibitors with an azaphenylalanine scaffold: Potency and selectivity enhancements via P2 optimization
Zega,Mlinsek,Sepic,Golic Grdadolnik,Solmajer,Tschopp,Steiner,Kikelj,Urleb
, p. 2745 - 2756 (2007/10/03)
Theoretical and structural studies followed by the directed synthesis and in vitro biological tests lead us to novel noncovalent thrombin pseudopeptide inhibitors. We have incorporated an azapeptide scaffold into the central part of the classical tripeptide D-Phe-Pro-Arg inhibitor structure thus eliminating one stereogenic center from the molecule. A series of compounds has been designed to optimize the occupancy of the S2 pocket of thrombin. Increased hydrophobicity at P2 provides an enhanced fit into this active site S2 pocket. In the present paper, we also report on the structure of these inhibitors in solution and conformational analysis of inhibitors in the active site in order to asses the consequences of the replacement of the central α-CH by a nitrogen functionality. In vitro biological testing of the designed inhibitors shows that elimination of R, S stereoisomerism and restriction of conformational freedom influences the binding of inhibitors in a favorable fashion.
Antiretroviral hydrazine derivatives
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, (2008/06/13)
The invention relates to compounds of formula STR1 and salts, pharmaceutical compositions, intermediates and processes of preparation thereof.
