Synthesis of Certain 6‐(Arylthio)uracils and Related Derivatives as Potential Antiviral Agents.

Abstract

Pyrimidine derivatives R 0510Synthesis of Certain 6-(Arylthio)uracils and Related Derivatives as Potential Antiviral Agents. -New series of 6-(arylthio)uracils (V) and related derivatives such as piperazinylpyrazines (IX) and tricyclic pyrimidine derivatives (VII), (XIII) are synthesized and evaluated for their in vitro antiviral activity as well as cytotoxicity. Arylthiouracils (Vb) and (Vd) exhibit marginal activity against HIV-1. Moreover, compound (Vb) exhibits marginal activity against HSV-1. -(EL-EMAM*, A. A.; MASSOUD, M. A. M.; EL-BENDARY, E. R.; EL-SAYED, M. A.; Bull. Korean Chem.

5-Propyl-6-(p-tolylsulfanyl)pyrimidine-2,4(1H,3H)-dione

“…Data collection: APEX2 (Bruker, 2009); cell refinement: SAINT (Bruker, 2009); data reduction: SAINT; program(s) used to solve structure: SHELXTL (Sheldrick, 2008); program(s) used to refine structure: SHELXTL; molecular graphics: SHELXTL; software used to prepare material for publication: SHELXTL and PLATON (Spek, 2009 Pyrimidine-2,4-diones and their related derivatives have long been known for their diverse chemotherapeutic activities including antiviral activity against the HIV (Miyasaka et al, 1989;Tanaka et al, 1995;Hopkins et al, 1996;El-Emam et al, 2004), and HSV viruses (Russ et al, 2003). In addition, potent anticancer activity was observed for several pyrimidine-2,4-diones (Klein et al, 2001;Nencka et al, 2006).…”

Synthesis, antiviral, cytotoxicity and antitumor evaluations of A4 type of porphyrin derivatives

“…In addition to the above results, it was interesting to prepare 5-oxo-1-phenyl-4,5-dihydro-1H-pyrazole-3carbaldehyde (6) by the reaction of 3-methyl-1-phenyl-1Hpyrazol-5(4H)-one (5) [37][38][39][40][41] with selenium dioxide in dioxane to give a good yield of compound 6. When 5-oxo-1-phenyl-4,5-dihydro-1H-pyrazole-3-carbaldehyde (6) reacted with pyrrole, according to the above mentioned procedure, they afforded the corresponding porphyrin 7.…”

Crystal structure of 5-ethyl-6-[(3-methylphenyl)sulfanyl]pyrimidine-2,4(1H,3H)-dione, C13H14N2O2S

“…The chemotherapeutic e cacy of pyrimidine-related derivatives is related to their ability to inhibit vital enzymes responsible for DNA biosynthesis including dihydrofolate reductase (DHFR), thymidylate synthetase (TSase), thymidine phosphorylase (TPase) and reverse transcriptase (RTase). 1-[2-(Hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) and its derivatives have long been known for their potent activity against human immunode ciency viruses (HIV) [1][2][3][4][5][6][7]. In addition, numerous pyrimidine-related derivatives displayed marked activities against herpes simplex viruses (HSV) [8], and hepatitis B viruses (HBV) [9].…”