scholarly journals Synthesis and in vitro Antitumor Effect of New Vindoline Derivatives Coupled with Amino Acid Esters

Heterocycles ◽  
2013 ◽  
Vol 87 (11) ◽  
pp. 2299 ◽  
Author(s):  
Csaba Szántay ◽  
Péter Keglevich ◽  
László Hazai ◽  
Álmos Gorka-Kereskényi ◽  
Lilla Péter ◽  
...  
Keyword(s):  
Amino Acid ◽  
Antitumor Effect ◽  
Amino Acid Esters ◽  
Acid Esters

scholarly journals FURTHER STUDIES ON THE ROLE OF PROTEASES IN THE ALLERGIC REACTION

1961 ◽  
Vol 113 (2) ◽  
pp. 359-380 ◽  
Author(s):  
Georges Ungar ◽  
Takuso Yamura ◽  
Jacqueline B. Isola ◽  
Sidney Kobrin
Keyword(s):  
Amino Acid ◽  
Guinea Pig ◽  
Proteolytic Activity ◽  
Guinea Pigs ◽  
Protease Activity ◽  
Amino Acid Esters ◽  
Protein Substrates ◽  
Protease Activation ◽  
Acid Esters

Protease activity was measured through the hydrolysis of synthetic amino acid esters in body fluids and tissues of guinea pigs, rats, mice, and humans. Significant in vitro activation was observed in serum and lung slices of sensitized guinea pigs on addition of the specific antigen. Increased proteolytic activity was also seen in reverse anaphylaxis. More marked activation occurred when guinea pig serum was treated with peptone and guinea pig or rat serum was treated with agar. Protease activation was demonstrated in specimens of human skin under the influence of a poison ivy extract or croton oil added in vitro. Urinary protease activity of guinea pigs increased significantly during the first hours of anaphylactic shock and very markedly in peptone shock. Peptone shock, elicited in mice pretreated with H. pertussis, was accompanied by a considerable increase in protease activity in the peritoneal fluid as compared with non-pretreated mice which were insensitive to peptone. Proteolytic activity resulting from the activation procedures was due to a number of proteases. The dominant substrate affinity and inhibition patterns suggest that serum and urine proteases are similar to but not identical with plasmin. Anaphylactic activation exhibited patterns different from those resulting from the action of anaphylactoid agents. Tissue enzymes are either of cathepsin- or chymotrypsin-type or mixtures of both. Some of the activated enzymes, although remarkably effective in hydrolyzing amino acid esters, show no activity on protein substrates. This does not justify, however, their designation as "esterases." They probably belong to the class of specific proteases acting only on a single or a small number of functionally significant protein substrates. There is at present sufficient evidence to prove not only that protease activation does occur in anaphylaxis and anaphylactoid conditions but also that it is an important component of the chain of reactions leading to the allergic response.

Highly water-soluble derivatives of the anesthetic agent propofol: in vitro and in vivo evaluation of cyclic amino acid esters

2003 ◽  
Vol 20 (1) ◽  
pp. 17-26 ◽  
Author(s):  
Cosimo Altomare ◽  
Giuseppe Trapani ◽  
Andrea Latrofa ◽  
Mariangela Serra ◽  
Enrico Sanna ◽  
...  
Keyword(s):  
Amino Acid ◽  
Water Soluble ◽  
Anesthetic Agent ◽  
Amino Acid Esters ◽  
In Vivo Evaluation ◽  
Derivatives Of ◽  
Acid Esters

Amino Acid Ester Prodrugs of Acyclovir

1992 ◽  
Vol 3 (3) ◽  
pp. 157-164 ◽  
Author(s):  
L. M. Beauchamp ◽  
G. F. Orr ◽  
P. de Miranda ◽  
T. Bumette ◽  
T. A. Krenitsky
Keyword(s):  
Amino Acid ◽  
Parent Compound ◽  
Parent Drug ◽  
Amino Acid Ester ◽  
Amino Acid Esters ◽  
Simplex Virus ◽  
Ester Prodrug ◽  
Acid Esters

Eighteen amino acid esters of the antiherpetic drug, acyclovir, were synthesized as potential prodrugs for oral administration. The esters were examined for in vitro antiviral activity against herpes simplex virus Type 1 (HSV-1). They were found to have less potency than the parent compound. Their efficiencies as prodrugs were evaluated in rats by measuring the urinary recovery of acyclovir. Ten prodrugs produced greater amounts of the parent drug in the urine. The L-amino acid esters were better prodrugs than the corresponding D- or D, L-isomers, suggesting the involvement of a stereoselective transporter. The L-valyl ester, 256U87, was the best prodrug. Sixty three per cent of its administered dose was excreted as acyclovir in the urine, a considerable improvement over acyclovir itself, for which this value was 19%. Since 256U87 was stable in aqueous solutions, its conversion to acyclovir in vivo was probably enzyme catalyzed. This L-valyl ester prodrug of acyclovir is now undergoing clinical evaluation.

Asymmetric Preparation of anti-β-Hydroxyα-amino Acid Esters

Synfacts ◽  
2006 ◽  
Vol 2006 (12) ◽  
pp. 1253-1253
Author(s):  
Y. Hamada ◽  
K. Makino ◽  
M. Iwasaki
Keyword(s):  
Amino Acid ◽  
Amino Acid Esters ◽  
Acid Esters

Antiviral activity of glycyrrhizic acid conjugates with amino acid esters against Zika virus

2021 ◽  
Vol 294 ◽  
pp. 198290
Author(s):  
Lidia A. Baltina ◽  
Mann-Jen Hour ◽  
Ya-Chi Liu ◽  
Young-Sheng Chang ◽  
Su-Hua Huang ◽  
...  
Keyword(s):  
Amino Acid ◽  
Antiviral Activity ◽  
Zika Virus ◽  
Glycyrrhizic Acid ◽  
Amino Acid Esters ◽  
Acid Esters
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