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Infection with herpes simplex virus (HSV) is the single most frequent cause of corneal opacities. Current available therapy for HSV keratitis involves the use of trifluorothymidine, idoxuridine and vidarabine. However, one of major problems associated with these drugs is their cytotoxicity. Acyclovir (ACV) with its selective mechanism of action can cause less cytotoxicity but its poor permeability across cellular barrier limits its utility. Thus, the development of a safe, long- acting, effective and stable topical antiviral drops that require less frequent dosing would represent a significant improvement. Recently design of prodrugs targeted to membrane transporters for improved efficacy and absorption proved highly successful. valacyclovir (VACV) is such a prodrug that increased the oral bioavailability of ACV by 3-5 fold in humans. Recently the presence of these transport systems on the corneal epithelium has been established in our laboratory. A series of novel water soluble amino acid ester prodrugs of ACV were thus synthesized. In conclusion more permeable, less cytotoxic Ser-acyclovir (SACV) exhibited excellent antiviral activity against HSV viruses.
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About the Author:
Suresh Katragadda, PhD: Graduated with PhD in Pharmaceutical Sciences at University of Missouri Kansas City (UMKC). Working as a NCD scientist I at Vertex Pharmaceuticals Inc., Boston. Ashim K. Mitra, PhD: Graduated with PhD in Pharmaceutical Chemistry at University of Kansas. Professor and Chair at Division of Pharmaceutical Sciences, UMKC.
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- PublisherVDM Verlag
- Publication date2009
- ISBN 10 3639151364
- ISBN 13 9783639151367
- BindingPaperback
- Number of pages160
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AMINO ACID PRODRUGS OF ACYCLOVIR: OCULAR HERPES INFECTIONS
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Book Description Taschenbuch. Condition: Neu. This item is printed on demand - it takes 3-4 days longer - Neuware -Infection with herpes simplex virus (HSV) is the single most frequent cause of corneal opacities. Current available therapy for HSV keratitis involves the use of trifluorothymidine, idoxuridine and vidarabine. However, one of major problems associated with these drugs is their cytotoxicity. Acyclovir (ACV) with its selective mechanism of action can cause less cytotoxicity but its poor permeability across cellular barrier limits its utility. Thus, the development of a safe, long-acting, effective and stable topical antiviral drops that require less frequent dosing would represent a significant improvement. Recently design of prodrugs targeted to membrane transporters for improved efficacy and absorption proved highly successful. valacyclovir (VACV) is such a prodrug that increased the oral bioavailability of ACV by 3-5 fold in humans. Recently the presence of these transport systems on the corneal epithelium has been established in our laboratory. A series of novel water soluble amino acid ester prodrugs of ACV were thus synthesized. In conclusion more permeable, less cytotoxic Ser-acyclovir (SACV) exhibited excellent antiviral activity against HSV viruses. 160 pp. Englisch. Seller Inventory # 9783639151367
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AMINO ACID PRODRUGS OF ACYCLOVIR OCULAR HERPES INFECTIONS DESIGN OF AMINO ACID PRODRUGS OF ACYCLOVIR FOR IMPROVED BIOAVAILABILITY AND THERAPEUTIC UTILITY IN TREATING OCULAR HERPES INFECTIONS
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AMINO ACID PRODRUGS OF ACYCLOVIR: OCULAR HERPES INFECTIONS : DESIGN OF AMINO ACID PRODRUGS OF ACYCLOVIR FOR IMPROVED BIOAVAILABILITY AND THERAPEUTIC ACTIVITY: UTILITY IN TREATING OCULAR HERPES INFECTIONS
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Book Description Taschenbuch. Condition: Neu. nach der Bestellung gedruckt Neuware - Printed after ordering - Infection with herpes simplex virus (HSV) is the single most frequent cause of corneal opacities. Current available therapy for HSV keratitis involves the use of trifluorothymidine, idoxuridine and vidarabine. However, one of major problems associated with these drugs is their cytotoxicity. Acyclovir (ACV) with its selective mechanism of action can cause less cytotoxicity but its poor permeability across cellular barrier limits its utility. Thus, the development of a safe, long-acting, effective and stable topical antiviral drops that require less frequent dosing would represent a significant improvement. Recently design of prodrugs targeted to membrane transporters for improved efficacy and absorption proved highly successful. valacyclovir (VACV) is such a prodrug that increased the oral bioavailability of ACV by 3-5 fold in humans. Recently the presence of these transport systems on the corneal epithelium has been established in our laboratory. A series of novel water soluble amino acid ester prodrugs of ACV were thus synthesized. In conclusion more permeable, less cytotoxic Ser-acyclovir (SACV) exhibited excellent antiviral activity against HSV viruses. Seller Inventory # 9783639151367
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Book Description Kartoniert / Broschiert. Condition: New. Dieser Artikel ist ein Print on Demand Artikel und wird nach Ihrer Bestellung fuer Sie gedruckt. Autor/Autorin: Katragadda SureshSuresh Katragadda, PhD: Graduated with PhD in Pharmaceutical Sciences at University of Missouri Kansas City (UMKC). Working as a NCD scientist I at Vertex Pharmaceuticals Inc., Boston. Ashim K. Mitra, PhD: Graduated . Seller Inventory # 4962045
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