SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL GUANINE ANALOGUES

Santhosha S. Poojary, Devaraju Kesagodu*, Ranjini P., Rekha N. D., Dhondiba Vishwanath, Chaitra Mallu M. and Basavaraju Y. B.

ABSTRACT

The novel substituted and potent guanines were synthesized in high yields. Guanine analogues especially acyclovir and valaciclovir for the treatment of herpes virus infections, have dominated the antiviral therapy for several decades. Valaciclovir is the L-valyl ester prodrug of acyclovir. It is used in the treatment of Herpes simplex virus and Vericella zoster virus. Herpes virus infections, especially those caused by HSV-1 and HSV-2 are the most common viral infections. In the present work, a series of novel substituted benzyl derivatives of Valacyclovir were efficiently synthesized and the structure of the compounds was confirmed by analytical spectral data. The synthesized new compounds were evaluated for their antibacterial, antifungal and antioxidant activities. Analogues synthesized in the present work exhibits strong to moderate activity. The antibacterial activity was compared with control, (gentamycin, fluconazole, and valaciclovir) 6e and 6f showed antibacterial, compound 6a and 6d showed antifungal acivity. The activity of the synthetic compounds is not significant when compared to the reference compounds gentamycin and flucanozole.

Keywords: Acyclovir, Valacyclovir, HSV-1, HSV-2, Vericella zoster.