AMINO ACID PRODRUGS OF ACYCLOVIR: OCULAR HERPES INFECTIONS - Couverture souple

Katragadda, Suresh

 
9783639151367: AMINO ACID PRODRUGS OF ACYCLOVIR: OCULAR HERPES INFECTIONS
Couverture souple
ISBN 10 : 3639151364 ISBN 13 : 9783639151367
Editeur : VDM Verlag, 2009

Synopsis

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.

Les informations fournies dans la section « Synopsis » peuvent faire référence à une autre édition de ce titre.

Présentation de l'éditeur

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.

Biographie de l'auteur

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.

Les informations fournies dans la section « A propos du livre » peuvent faire référence à une autre édition de ce titre.

Éditeur
VDM Verlag
Date d'édition
2009
Langue
anglais
ISBN 10 
3639151364
ISBN 13 
9783639151367
Reliure
Broché
Nombre de pages
160
Coordonnées du fabricant
non disponible
Personne responsable
non disponible