Amino Acid Ester Prodrugs of 2-Bromo-5,6-dichloro-1-(β-d-ribofuranosyl)benzimidazole Enhance Metabolic Stability in Vitro and in Vivo

2005 ◽  
Vol 314 (2) ◽  
pp. 883-890 ◽  
Author(s):  
Philip L. Lorenzi ◽  
Christopher P. Landowski ◽  
Xueqin Song ◽  
Katherine Z. Borysko ◽  
Julie M. Breitenbach ◽  
...  
Keyword(s):  
Amino Acid ◽  
Acid Ester ◽  
Amino Acid Ester ◽  
Metabolic Stability ◽  
Ester Prodrugs

scholarly journals Transdermal Delivery Systems for Ibuprofen and Ibuprofen Modified with Amino Acids Alkyl Esters Based on Bacterial Cellulose

2021 ◽  
Vol 22 (12) ◽  
pp. 6252
Author(s):  
Paula Ossowicz-Rupniewska ◽  
Rafał Rakoczy ◽  
Anna Nowak ◽  
Maciej Konopacki ◽  
Joanna Klebeko ◽  
...  
Keyword(s):  
Amino Acids ◽  
Amino Acid ◽  
Bacterial Cellulose ◽  
Acid Ester ◽  
Active Pharmaceutical Ingredient ◽  
Amino Acid Ester ◽  
Isopropyl Ester ◽  
Isopropyl Esters ◽  
Transdermal Application

The potential of bacterial cellulose as a carrier for the transport of ibuprofen (a typical example of non-steroidal anti-inflammatory drugs) through the skin was investigated. Ibuprofen and its amino acid ester salts-loaded BC membranes were prepared through a simple methodology and characterized in terms of structure and morphology. Two salts of amino acid isopropyl esters were used in the research, namely L-valine isopropyl ester ibuprofenate ([ValOiPr][IBU]) and L-leucine isopropyl ester ibuprofenate ([LeuOiPr][IBU]). [LeuOiPr][IBU] is a new compound; therefore, it has been fully characterized and its identity confirmed. For all membranes obtained the surface morphology, tensile mechanical properties, active compound dissolution assays, and permeation and skin accumulation studies of API (active pharmaceutical ingredient) were determined. The obtained membranes were very homogeneous. In vitro diffusion studies with Franz cells were conducted using pig epidermal membranes, and showed that the incorporation of ibuprofen in BC membranes provided lower permeation rates to those obtained with amino acids ester salts of ibuprofen. This release profile together with the ease of application and the simple preparation and assembly of the drug-loaded membranes indicates the enormous potentialities of using BC membranes for transdermal application of ibuprofen in the form of amino acid ester salts.

Amino Acid Ester Prodrugs of the Anticancer Agent Gemcitabine:  Synthesis, Bioconversion, Metabolic Bioevasion, and hPEPT1-Mediated Transport

2005 ◽  
Vol 2 (2) ◽  
pp. 157-167 ◽  
Author(s):  
Xueqin Song ◽  
Philip L. Lorenzi ◽  
Christopher P. Landowski ◽  
Balvinder S. Vig ◽  
John M. Hilfinger ◽  
...  
Keyword(s):  
Amino Acid ◽  
Acid Ester ◽  
Anticancer Agent ◽  
Amino Acid Ester ◽  
Ester Prodrugs

Synthesis of Stavudine Amino Acid Ester Prodrugs with Broad-Spectrum Chemotherapeutic Properties for the Effective Treatment of HIV/AIDS.

ChemInform ◽  
2004 ◽  
Vol 35 (26) ◽  
Author(s):  
Dharmarajan Sriram ◽  
Perumal Yogeeswari ◽  
Narasimharaghavan Srichakravarthy ◽  
Tanushree Ratan Bal
Keyword(s):  
Amino Acid ◽  
Effective Treatment ◽  
Broad Spectrum ◽  
Acid Ester ◽  
Amino Acid Ester ◽  
Ester Prodrugs ◽  
Hiv Aids

Amino Acid Ester Prodrugs of the Antiviral Agent 2-Bromo-5,6-dichloro-1-(β-d-ribofuranosyl)benzimidazole as Potential Substrates of hPEPT1 Transporter

2005 ◽  
Vol 48 (4) ◽  
pp. 1274-1277 ◽  
Author(s):  
Xueqin Song ◽  
Balvinder S. Vig ◽  
Philip L. Lorenzi ◽  
John C. Drach ◽  
Leroy B. Townsend ◽  
...  
Keyword(s):  
Amino Acid ◽  
Acid Ester ◽  
Antiviral Agent ◽  
Amino Acid Ester ◽  
Ester Prodrugs

scholarly journals Floxuridine Amino Acid Ester Prodrugs: Enhancing Caco-2 Permeability and Resistance to Glycosidic Bond Metabolism

2005 ◽  
Vol 22 (9) ◽  
pp. 1510-1518 ◽  
Author(s):  
Christopher P. Landowski ◽  
Xueqin Song ◽  
Philip L. Lorenzi ◽  
John M. Hilfinger ◽  
Gordon L. Amidon
Keyword(s):  
Amino Acid ◽  
Acid Ester ◽  
Amino Acid Ester ◽  
Glycosidic Bond ◽  
Ester Prodrugs

scholarly journals Kinetics and Mechanisms of Activation of α-Amino Acid Ester Prodrugs of Camptothecins

2006 ◽  
Vol 49 (14) ◽  
pp. 4344-4355 ◽  
Author(s):  
Lin Song ◽  
Robert Bevins ◽  
Bradley D. Anderson
Keyword(s):  
Amino Acid ◽  
Acid Ester ◽  
Amino Acid Ester ◽  
Ester Prodrugs
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