Structure–activity relationships of pyrrole amidine antiviral antibiotics III: Preparation of distamycin and congocidine derivatives based on 2,5‐disubstituted pyrroles

Meir Bialer*, Boris Yagen, Raphael Mechoulam, Yechiel Becker

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

17 Scopus citations

Abstract

Isomers of distamycin A and tripyrrole congocidine containing 2,5‐disubstituted pyrroles were synthesized along with distamycin and congocidine homologs containing a single pyrrole ring. Selected compounds were evaluated for their cytotoxicity and antiviral activity. All of the tripyrrole derivatives tested in this series were nontoxic but were less active than distamycin A. The monopyrrole derivative, N‐methyl‐5‐nitropyrrole‐2‐carboxamido‐β‐propionamidine hydrochloride, was nontoxic and was almost as active antivirally as distamycin A.

Original languageEnglish
Pages (from-to)1334-1338
Number of pages5
JournalJournal of Pharmaceutical Sciences
Volume69
Issue number11
DOIs
StatePublished - Nov 1980

Keywords

  • Antibiotics—distamycin A and congocidine derivatives based on 2,5‐disubstituted pyrroles, synthesis and evaluation for cytotoxicity and antiviral activity, structure–activity relationships
  • Congocidine—derivatives based on 2,5‐disubstituted pyrroles, synthesis and evaluation for cytotoxicity and antiviral activity, structure–activity relationships
  • Distamycin—derivatives based on 2,5‐disubstituted pyrroles, synthesis and evaluation for cytotoxicity and antiviral activity, structure–activity relationships
  • Structure–activity relationships—distamycin A and congocidine derivatives based on 2,5‐disubstituted pyrroles, antiviral activity

Fingerprint

Dive into the research topics of 'Structure–activity relationships of pyrrole amidine antiviral antibiotics III: Preparation of distamycin and congocidine derivatives based on 2,5‐disubstituted pyrroles'. Together they form a unique fingerprint.

Cite this