Anti-Viral Azide Containing Compounds

Abstract

Methods of using azide-modified biomolecules, such as fatty acids, carbohydrates and lipids, to treat a plant, an insect or an animal infected with a virus or to inhibit infectivity of a virus, such as the human immunodeficiency virus, are provided. Also provided are methods of labeling a virus, such as human immunodeficiency virus, with an azide-modified biomolecule, such as a fatty acid, a carbohydrate, or an isoprenoid lipid. Also, provided are methods of tracking a virus in vivo, with an azide-modified biomolecule, such as a fatty acid, a carbohydrate, or an isoprenoid lipid. The azide-modified biomolecules may be combined with a pharmaceutically acceptable excipient to produce a pharmaceutical composition, optionally containing another anti-viral agent and / or a delivery agent, such as a liposome.

Description

BACKGROUND[0001]Viral infections account for significant morbidity and mortality in humans and animals. In addition, viral infections also result in significant agricultural losses, with plant viruses causing an estimated $60 billion in lost crop yields throughout the world each year. Although significant resources have been dedicated to identifying compounds having anti-viral properties, viral infections continue to present a significant risk to human health and agriculture.[0002]In addition, the usefulness of most existing anti-viral treatments is limited by the development of multidrug resistance, poor efficacy, and / or toxicity. In fact, many anti-viral treatments are highly toxic and can cause serious side effects, including heart damage, kidney failure and osteoporosis. Other challenges include creating a drug that is broadly applicable in combating many different types of viral infections, which can be particularly important in the treatment of immunocompromised individuals.[0...

AI Technical Summary

Benefits of technology

[0026]Another aspect of the disclosure is directed a method of inhibiting the infectivity of a virus, the method comprising contacting a cell infected with the virus with an azide-modified

Problems solved by technology

Viral infections account for significant morbidity and mortality in humans and animals.

In addition, viral infections also result in significant agricultural losses, with plant viruses causing an estimated $60 billion in lost crop yields throughout the world each year.

Although significant resources have been dedicated to identifying compounds having anti-viral properties, viral infections continue to present a significant risk to human health and agriculture.

In addition, the usefulness of most existing anti-viral treatments is limited by the development of multidrug resistance, poor efficacy, and / or toxicity.

In fact, many anti-viral treatments are highly toxic and can cause serious side effects, including heart damage, kidney failure and osteoporosis.

Other challenges include creating a drug that is broadly applicable in combating many different types of viral infections, which can be particularly important in the treatment of immunocompromised individuals.

As of 2007, it was estimated that more than 33 million people were infected with HIV, and HIV associated diseases represent a major world health problem.

As the infection progresses, the immune system becomes weaker, leaving the infected person more susceptible to opportunistic infections and tumors, such as Kaposi's sarcoma, cervical cancer, lymphoma, and neurological disorders.

Certain antiretroviral drugs can delay the process even further.

Although much effort has been put forth into designing effective therapeutics against HIV, currently no curative anti-retroviral drugs against HIV exist.

Therefore, interfering with reverse transcriptase inhibits HIV's ability to replicate.

As a result, when the analogs are incorporated into a growing viral DNA chain, the incoming deoxynucleotide cannot form a phosphodiester bond with the analog that is needed to extend the DNA chain.

While beneficial, these antiretroviral drugs often exhibit toxic side effects such as bone marrow suppression, vomiting, and liver function abnormalities.

In addition, they are not curative, probably due to the rapid appearance of drug resistant HIV mutants (Lander, B. et al., 1989, Science 243:1731-1734).

Images