181872-56-0Relevant academic research and scientific papers
NADP-dependent glutamate dehydrogenases in a dimorphic zygomycete Benjaminiella poitrasii: Purification, characterization and their evaluation as an antifungal drug target
Deshpande, Mukund V.,Kulkarni, Anand M.,Pathan, Ejaj K.,Prasanna, Nallaballe V. L.,Ramana, Chepuri V.
, (2020/08/21)
Background: It has been reported that the genes coding for NADP-dependent glutamate dehydrogenases (NADP-GDHs) showed a cause-effect relationship with Yeast-Hypha (Y[sbnd]H) reversible transition in a zygomycete Benjaminiella poitrasii. As Y[sbnd]H transition is significant in human pathogenic fungi for their survival and proliferation in the host, the NADP-GDHs can be explored as antifungal drug targets. Methods: The yeast-form specific BpNADPGDH I and hyphal-form specific BpNADPGDH II of B. poitrasii were purified by heterologous expression in E. coli BL-21 cells and characterized. The structural analogs of L-glutamate, dimethyl esters of isophthalic acid (DMIP) and its derivatives were designed, synthesized and screened for inhibition of NADP-GDH activity as well as Y[sbnd]H transition in B. poitrasii, and also in human pathogenic Candida albicans strains. Results: The BpNADPGDH I and BpNADPGDH II were found to be homo-hexameric proteins with native molecular mass of 282 kDa and 298 kDa, respectively and subunit molecular weights of 47 kDa and 49 kDa, respectively. Besides the distinct kinetic properties, BpNADPGDH I and BpNADPGDH II were found to be regulated by cAMP-dependent- and Calmodulin (CaM) dependent- protein kinases, respectively. The DMIP compounds showed a more pronounced effect on H-form specific BpNADPGDH II and inhibited Y[sbnd]H transition as well as growth in B. poitrasii and C. albicans strains. Conclusion: The present study will be useful to design and develop antifungal drugs against dimorphic human pathogens using glutamate dehydrogenase as a target. Significance: Glutamate dehydrogenases can be explored as a target against human pathogenic fungi.
Syntheses of amide based anion receptors and investigation of their associations with anions and their molecular structures using proton NMR titration and DFT methods
Navakhun, Korakot,Sawangsri, Ranu,Ruangpornvisuti, Vithaya
, p. 32 - 40 (2014/02/14)
The synthesized disubstituted isophthalamide and pyridine-2,6dicarboxamide derivatives of nine compounds were prepared. Their association constants with tetrabutylammonium fluoride (TBA·F), tetrabutylammonium chloride (TBA·Cl), tetrabutylammonium bromide
Synthesis and NMR binding studies towards rational design of a series of electron-withdrawing diamide receptors/organocatalysts
Kinsella, Michael,Duggan, Patrick G.,Muldoon, Jimmy,Eccles, Kevin S.,Lawrence, Simon E.,Lennon, Claire M.
supporting information; experimental part, p. 1125 - 1132 (2011/04/15)
A related series of bisamides have been evaluated for rational correlation between anion complexation and organocatalysis: remarkable enhancement of hydrogen bonding to anions was observed along with significant increases in catalytic activity in the Bayl
Isophthalic acid-derived dicarbothioamides as novel metal-free catalysts in hydrogen bond-promoted reactions
Guizzetti, Stefania,Benaglia, Maurizio,Puglisi, Alessandra,Raimondi, Laura
experimental part, p. 3731 - 3742 (2009/12/09)
The synthesis of N,N'-diaryl-1,3-benzene-dicarbothioamides was accomplished in only two steps with good yields, and their ability to act as hydrogen-bond donors in Diels-Alder reactions was evaluated. These new organocatalysts were indeed able to promote the cycloaddition of cyclopentadiene to ,-unsaturated aldehydes. In the attempt to control the absolute stereochemistry of the reaction, chiral catalysts were also prepared by simple condensation of isophthalic acid and-amino acid derivatives. Molecular mechanics calculations were performed to elucidate the mode of action of these metal-free catalytic systems and to find a rationale for the achieved enantioselectivity.
