Improved delivery through biological membranes. 38. Brain-specific chemical delivery systems for .beta.-lactam antibiotics. Synthesis and properties of some dihydropyridine and dihydroisoquinoline derivatives of benzylpenicillin

1989 ◽  
Vol 32 (8) ◽  
pp. 1774-1781 ◽  
Author(s):  
Emil Pop ◽  
Whei Mei Wu ◽  
Efraim Shek ◽  
Nicholas Bodor
Keyword(s):  
Biological Membranes ◽  
Delivery Systems ◽  
Beta Lactam ◽  
Specific Chemical ◽  
Beta Lactam Antibiotics ◽  
Chemical Delivery Systems ◽  
Derivatives Of

Semisynthetic .beta.-lactam antibiotics. 1. Acylation of 6-aminopenicillanic acid with activated derivatives of .alpha.-sulfophenylacetic acid

1972 ◽  
Vol 15 (11) ◽  
pp. 1105-1108 ◽  
Author(s):  
Shiro Morimoto ◽  
Hiroaki Nomura ◽  
Toshihiro Ishiguro ◽  
Takeshi Fugono ◽  
Kihachiro Maeda
Keyword(s):  
Beta Lactam ◽  
Beta Lactam Antibiotics ◽  
Derivatives Of

Improved Delivery through Biological Membranes. Synthesis and Antiviral Activity of a Series of Ribavirin Chemical Delivery Systems: 2′ and 3′ Derivatives

1991 ◽  
Vol 2 (6) ◽  
pp. 337-355 ◽  
Author(s):  
M. Deyrup ◽  
R. Sidwell ◽  
R. Little ◽  
P. Druzgala ◽  
N. Bodor ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Intravenous Administration ◽  
Murine Model ◽  
Viral Encephalitis ◽  
Biological Membranes ◽  
Delivery Systems ◽  
Redox Systems ◽  
Isomeric Pair ◽  
Vehicle Treatment ◽  
Chemical Delivery Systems

Ribavirin was chemically manipulated to provide a number of derivatives in which a 1,4-dihydrotrigonellinate species was attached to either the 2′ or 3′-position. In addition, a variety of other modifications was used to augment the lipophilicity and stability of the ribavirin redox systems. Prepared compounds were tested in a murine model of viral encephalitis. Intravenous administration of an isomeric pair of derivatives (1-[3′-O-(N-methyl-3-carbonyl-1,4-dihydropyridine)-2′-O-benzoyl-β-D-ribofuranosyl]-1,2,4-triazole-3-carboxamide/1-[2′-O-(N-methyl-3-carbonyl-1,4-dihydropyridine)-3′-O-benzoyl-β-D-ribofuranosyl]-1,2,4-triazole-3-carboxamide) resulted in 43% survival compared with 0% for vehicle treatment and resulted in a decrease in brain viral titres by 10-fold.

In Vitro and In Vivo Evaluations of Dihydroquinoline- and Dihydroisoquinoline-based Targetor Moieties for Brain-specific Chemical Delivery Systems

2002 ◽  
Vol 10 (1) ◽  
pp. 63-71 ◽  
Author(s):  
Nicholas Bodor ◽  
Hassan H. Farag ◽  
M. Dulce C. Barros ◽  
Whei-Mei Wu ◽  
Peter Buchwald
Keyword(s):  
Delivery Systems ◽  
Specific Chemical ◽  
Chemical Delivery Systems
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