# US 4,396,628 A · Antiviral activities of dansylcadaverine and closely related compounds

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- Number: US 4,396,628 A
- Document ID: US4396628A
- Status: Granted
- Kind: A
- Application number: 06/352,599
- Filed: 1982-02-26
- Granted: 1983-08-02
- Earliest claimed: 1981-06-18
- Assignees: The United States of America as represented by the Department of Health and Human Services
- Inventors: Ira H. Pastan; Mark C. Willingham
- Web page: https://patentgrep.com/patent/US4396628A

## CPC

- A61K 31/18: Sulfonamides (compounds containing a para-N-benzene-sulfonyl-N- group A61K31/63)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

The entry of animal viruses into their host cells proceeds via a specialized internalization pathway involving clathrin coated regions of the plasma membrane. In the present invention, there has been examined the effect of dansylcadaverine compared with amantadine and other antiviral agents as to the entry of vesicular stomatitis virus (VSV) into mouse cells. It was found that both compounds inhibit VSV entry. Both compounds inhibit the uptake of .alpha..sub.2 macroglobulin (.alpha.2M), a protein that binds to specific membrane receptors and follows the same route of internalization. Dansylcadaverine is 20 fold more potent than amantadine to the blocking virus and also to the .alpha..sub.2 macroglobulin uptake.

## Claims

### Claim 1

A method of inhibiting and blocking the effective entry of vesicular stomatitis virus (VSV) and .alpha..sub.2 macroglobulin (.alpha..sub.2 M) into mouse cells comprising administering thereto an effective blockading amount of ##STR2## R.sub.1 =--(CH.sub.2)--.sub.3-7 R.sub.2 =--CH.sub.3
R.sub.3 =CH.sub.3
in a pharmaceutically-acceptable carrier.

### Claim 2 (depends on 1)

A method according to claim 1, wherein the compound utilized R.sub.1 =--(CH.sub.2).sub.5, R.sub.2 and R.sub.3 =CH.sub.3.

### Claim 3 (depends on 1)

A method according to claim 1, wherein the concentration of the compound utilized is about 50 .mu.M to 500 .mu.M.