NUCLEOTIDE DIMERS AS ANTI-HIV AGENTS

Award Information
Agency: Department of Health and Human Services
Branch: N/A
Contract: N/A
Agency Tracking Number: 11065
Amount: $490,796.00
Phase: Phase II
Program: SBIR
Awards Year: 1990
Solicitation Year: N/A
Solicitation Topic Code: N/A
Solicitation Number: N/A
Small Business Information
Baker Cummins Pharmaceuticals
8800 Nw 36th St, Miami, FL, 33178
DUNS: N/A
HUBZone Owned: N
Woman Owned: N
Socially and Economically Disadvantaged: N
Principal Investigator
 () -
Business Contact
Phone: () -
Research Institution
N/A
Abstract
A SERIES OF COMPOUNDS THAT ARE EITHER HOMODIMERS OR HETERODIMERS OF SPECIFIC DIDEOXYNUCLEOSIDES HAVE BEEN SYNTHESIZED. IN VARIOUS ASSAYS, THE PHOSPHATE-LINKED DIMERSOF SUCH ANTIVIRAL MONOMERIC DIDEOXYNUCLEOSIDES POSSESS GREATER ACTIVITY THAN THE COMBINED ACTIVITY OF THE DIDEOXYNUCLEOSIDES ADMINISTERED ALONE. PRELIMINARY PHARMACOKINETIC DATA OBTAINED FOR ONE OF THE AGENTS AFTER INTRAVENOUS ADMINISTRATION TO RATS INDICATED THAT IT CROSSEDTHE BLOOD-BRAIN BARRIER WITH A DISTRIBUTION THAT COMPARED FAVORABLY TO AZT. IT IS PLANNED TO EXPAND THE SERIES OF DIMERIC COMPOUNDS BY SYNTHESIZING DRUGS THAT INCLUDE THE FOLLOWING NUCLEOSIDES: DDA, DDI, DDC, DDG, AND AZT. SINCE THE LIPOPHILICITY AND, THEREFORE, THE CNS BIOAVAILABILITY OF THE SPECIFIC AGENTS APPEARS TO BE GREATER FOR THE ESTERIFIED ANALOG OF THE NUCLEOSIDE DIMER TRIESTER, A SERIES OF TRIESTERS WILL BE PREPARED TO EXAMINE THE IMPACT OF SUCH SUBSTITUTION ON ANTIVIRAL ACTIVITY AND CYTOTOXICITY. BASED ON THE IN VITRO RESULTS THAT ARE OBTAINED, THE IN VIVO DISTRIBUTION AND METABOLISM OF THE MOST ACTIVE COMPOUNDS WILL BE EXAMINED. THE INFORMATION OBTAINED FROM THESE EXPERIMENTS WILL LEAD TO THE CHOICE OF SPECIFIC COMPOUNDS TO BE STUDIED IN PHASE II.

* information listed above is at the time of submission.

Agency Micro-sites

SBA logo
Department of Agriculture logo
Department of Commerce logo
Department of Defense logo
Department of Education logo
Department of Energy logo
Department of Health and Human Services logo
Department of Homeland Security logo
Department of Transportation logo
Environmental Protection Agency logo
National Aeronautics and Space Administration logo
National Science Foundation logo
US Flag An Official Website of the United States Government