scholarly journals 2-(3,4-Dihydroxyphenyl)-4-(2-(4-nitrophenyl)hydrazono)-4H-chromene-3,5,7-triol

Molbank ◽  
10.3390/m1144 ◽  
2020 ◽  
Vol 2020 (3) ◽  
pp. M1144 ◽  
Author(s):  
Alessandra Gianoncelli ◽  
Alberto Ongaro ◽  
Giuseppe Zagotto ◽  
Maurizio Memo ◽  
Giovanni Ribaudo
Keyword(s):  
Mass Spectrometry ◽  
Molecular Modeling ◽  
Natural Compound ◽  
Folk Medicine ◽  
Single Step ◽  
Pde5 Inhibitors ◽  
Molecular Modeling Studies ◽  
Potential Activity ◽  
Phosphodiesterase 5 ◽  
Hydrazone Derivative

On the basis of the knowledge from traditional herbal and folk medicine, flavonoids are among the most studied chemical classes of natural compounds for their potential activity as phosphodiesterase 5 (PDE5) inhibitors. We here describe the preparation of a semi-synthetic hydrazone derivative of quercetin, 2-(3,4-dihydroxyphenyl)-4-(2-(4-nitrophenyl)hydrazono)-4H-chromene-3,5,7-triol, that was obtained via a single-step modification of the natural compound. The product was characterized by NMR, mass spectrometry and HPLC. Preliminary molecular modeling studies suggest that this compound could efficiently interact with PDE5.

scholarly journals Mass spectrometry and molecular modeling studies on the inclusion complexes between alendronate and β-cyclodextrin

2013 ◽  
Vol 78 (1-4) ◽  
pp. 437-443 ◽  
Author(s):  
Joanna Biernacka ◽  
Katarzyna Betlejewska-Kielak ◽  
Janina Witowska-Jarosz ◽  
Ewa Kłosińska-Szmurło ◽  
Aleksander P. Mazurek
Keyword(s):  
Mass Spectrometry ◽  
Molecular Modeling ◽  
Inclusion Complexes ◽  
Modeling Studies ◽  
Molecular Modeling Studies

scholarly journals Synthesis, Molecular Modeling, and Biological Evaluation of Novel Tetrahydro-β-Carboline Hydantoin and Tetrahydro-β-Carboline Thiohydantoin Derivatives as Phosphodiesterase 5 Inhibitors

2011 ◽  
Vol 2011 ◽  
pp. 1-9 ◽  
Author(s):  
Ashraf H. Abadi ◽  
Jochen Lehmann ◽  
Gary A. Piazza ◽  
Mohammad Abdel-Halim ◽  
Mohamed S. M. Ali
Keyword(s):  
Amino Acid ◽  
Molecular Modeling ◽  
Absolute Configuration ◽  
Biological Evaluation ◽  
Economic Advantage ◽  
Pde5 Inhibitors ◽  
Pde5 Inhibition ◽  
Chiral Carbon ◽  
Hydantoin Derivatives ◽  
Phosphodiesterase 5

Two series of fused tetrahydro-β-carboline hydantoin and tetrahydro-β-carboline thiohydantoin derivatives with a pendant 2,4-dimethoxyphenyl at position 5 were synthesized, and chiral carbons at positions 5 and 11a swing from R,R to R,S, S,R, and S,S. The prepared analogues were evaluated for their capacity to inhibit phosphodiesterase 5 (PDE5) isozyme. The R absolute configuration of C-5 in the β-carboline hydantoin derivatives was found to be essential for the PDE5 inhibition. Chiral carbon derived from amino acid even if of the S configuration (L-tryptophan) may lead to equiactive or more active isomers than those derived from amino acid with the R configuration (D-tryptophan). This expands the horizon from which efficient PDE5 inhibitors can be derived and may offer an economic advantage. The thiohydantoin derivatives were less active than their hydantoin congeners.

Characterization of hemoglobin Würzburg (α2ß2 4(A1)Thr→Asn), a new electrophoretically silent variant, by mass spectrometry and molecular modeling studies

2006 ◽  
Vol 1115 (1-2) ◽  
pp. 118-124 ◽  
Author(s):  
Emmanuel Bissé ◽  
Nathalie Zorn ◽  
Stéphanie Boussert ◽  
Thomas Epting ◽  
Alain Van Dorsselaer ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Molecular Modeling ◽  
Modeling Studies ◽  
Molecular Modeling Studies

Chromatography, mass spectrometry, and molecular modeling studies on ammodytoxins

2012 ◽  
Vol 402 (9) ◽  
pp. 2737-2748 ◽  
Author(s):  
Marija Brgles ◽  
Branimir Bertoša ◽  
Wolfgang Winkler ◽  
Tihana Kurtović ◽  
Günter Allmaier ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Molecular Modeling ◽  
Modeling Studies ◽  
Chromatography Mass Spectrometry ◽  
Molecular Modeling Studies

The Effect of PDE5 Inhibitors on the Male Reproductive Tract

2020 ◽  
Vol 26 ◽  
Author(s):  
Nikolaos Sofikitis ◽  
Aris Kaltsas ◽  
Fotios Dimitriadis ◽  
Jens Rassweiler ◽  
Nikolaos Grivas ◽  
...  
Keyword(s):  
Male Infertility ◽  
Reproductive Tract ◽  
Tunica Albuginea ◽  
Scientific Data ◽  
Secretory Function ◽  
Pde5 Inhibitors ◽  
Male Reproductive Tract ◽  
Review Study ◽  
Phosphodiesterase 5

The therapeutic range of cyclic nucleotide phosphodiesterase 5 inhibitors (PDE5) inhibitors is getting wider in the last years. This review study focuses on the potential employment of PDE5 inhibitors as an adjunct tool for the therapeutic management of male infertility. The literature tends to suggest a beneficial effect of PDE5 inhibitors on Leydig and Sertoli cells secretory function. It also appears that PDE5 inhibitors play a role in the regulation of the contractility of the testicular tunica albuginea and the epididymis. Moreover scientific data suggest that PDE5 inhibitors enhance the prostatic secretory function leading to an improvement in sperm motility. Other studies additionally demonstrate a role of PDE5 inhibitors in the regulation of sperm capacitation process. Placebo-controlled, randomized, blind studies are necessary to unambiguously incorporate PDE5 inhibitors as an adjunct tool for the pharmaceutical treatment of semen disorders and male infertility.

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