Synthesis and Biological Evaluation of Lisofylline (LSF) Analogues as a Potential Treatment for Type 1 Diabetes.

ChemInform ◽  
2006 ◽  
Vol 37 (39) ◽  
Author(s):  
Peng Cui ◽  
Timothy L. Macdonald ◽  
Meng Chen ◽  
Jerry L. Nadler
Keyword(s):  
Type 1 Diabetes ◽  
Biological Evaluation ◽  
Potential Treatment ◽  
Synthesis And Biological Evaluation

scholarly journals Pyridazino[3,4-b][1,5]Benzodiazepin-5-Ones: Synthesis and Biological Evaluation

1997 ◽  
Vol 8 (4) ◽  
pp. 371-379 ◽  
Author(s):  
G Heinisch ◽  
E Huber ◽  
C Leitner ◽  
B Matuszczak ◽  
A Maurer ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Reverse Transcriptase Inhibitors ◽  
Inhibitory Potency ◽  
Substitution Pattern ◽  
Carboxylic Acid Chloride ◽  
Tricyclic Compounds ◽  
Immunodeficiency Virus ◽  
Synthesis And Biological Evaluation ◽  
Primary Aliphatic Amines

Starting from 3,6-dichloropyridazine-4-carboxylic acid chloride, a series of pyridazino[3,4- b][1,5]benzodiazepin-5-ones bearing various substituents in positions 3, 6, 8 and 11 was prepared via N-alkyl-3-alkylamino-6-chloro- N-(2-chloro-5-nitrophenyl)-pyridazine-4-carboxamides. The latter were smoothly accessible by treatment of N-alkyl-3,6-dichloro-N-(2-fluorophenyl)-pyridazine-4-carboxamides with primary aliphatic amines. The new tricyclic compounds, which are structurally related to nevirapine and congeners were screened as human immunodeficiency virus type 1 reverse transcriptase inhibitors; the influence of the substitution pattern on inhibitory potency is discussed.

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