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Synthesis of the 7,8-dihydro-7-deazapurine derivatives and their antibiotic activity.
- Source :
-
Archives of pharmacal research [Arch Pharm Res] 1998 Apr; Vol. 21 (2), pp. 187-92. - Publication Year :
- 1998
-
Abstract
- The cis- and trans-diastereomers of the 7,8-dihydro-7-deazapurine derivatives were synthesized from the corresponding diastereomers of 4-trans-cyano-2-methyl-3-phenyl-5-oxopyrrolidine (5), which were reduced from the 2-cis- and 2-trans-diastereomers of 4-trans-cyano-2-hydroxymethyl-3-phenyl-5-oxopyrrolidine (2) via tosylation, iodination and following elimination, respectively. The prepared cis- and trans-diastereomers of 6-amino-2-mercapto-8-methyl-7-phenyl-7,8-dihydro-7(9H)-deazapurine (8) were transferred to the corresponding 2-methylthio-diastereomers 9 and following desulfurization with Raney-nickel leaded to the cis- and trans-diastereomers of 6-amino-8-methyl-7-phenyl-7,8-dihydro-7(9H)-deazapurine (10), respectively. The synthesized 7-deazapurine derivatives were tested for their antibiotic activity by the serial two-fold dilution method.
- Subjects :
- Anti-Bacterial Agents pharmacology
Bacillus subtilis drug effects
Escherichia coli drug effects
Microbial Sensitivity Tests
Purines pharmacology
Staphylococcus aureus drug effects
Structure-Activity Relationship
Anti-Bacterial Agents chemical synthesis
Bacteria drug effects
Purines chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 0253-6269
- Volume :
- 21
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Archives of pharmacal research
- Publication Type :
- Academic Journal
- Accession number :
- 9875429
- Full Text :
- https://doi.org/10.1007/BF02974026