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NUCLEOTIDE DIMERS AS ANTI-HIV AGENTS

Award Information

Agency:
Department of Health and Human Services
Branch:
N/A
Award ID:
11065
Program Year/Program:
1990 / SBIR
Agency Tracking Number:
11065
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
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Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No
 
Phase 2
Fiscal Year: 1990
Title: NUCLEOTIDE DIMERS AS ANTI-HIV AGENTS
Agency: HHS
Contract: N/A
Award Amount: $490,796.00
 

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.

Principal Investigator:


0

Business Contact:

Small Business Information at Submission:

Baker Cummins Pharmaceuticals
8800 Nw 36th St Miami, FL 33178

EIN/Tax ID:
DUNS: N/A
Number of Employees: N/A
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No