Suramin analogues with a 2-phenylbenzimidazole moiety as partial structure; potential anti HIV- and angiostatic drugs, 2: Sulfanilic acid-, benzenedisulfonic acid-, and naphthalenetrisulfonic acid analogues

Arch Pharm (Weinheim). 1998 Mar;331(3):97-103. doi: 10.1002/(sici)1521-4184(199803)331:3<97::aid-ardp97>3.0.co;2-f.

Abstract

The synthesis of suramin analogues bearing a 2-phenyl-benzimidazole moiety is described. Aminoarene sulfonic acids 2a-e are acylated with 3,4-dinitrobenzoyl chloride 3 yielding the amides 4a-e which are hydrogenated to the corresponding diamines 5a-e. These are treated with 3-nitrobenzaldehyde, yielding the azomethines 7a-e and their isomers 8a-e and 9a-e. Key step in the synthesis of the target compounds 12a-e is the oxidation of the azomethines with oxygen to the benzimidazoles 10a-e. These are hydrogenated to the amines 11a-e reacting with phosgene to yield the symmetric ureas 12a-e. Results of the anti-HIV, cytostatic, and antiangiogenic screening are presented.

MeSH terms

  • Anti-HIV Agents / chemical synthesis*
  • Anti-HIV Agents / pharmacology
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Benzenesulfonates / chemical synthesis
  • Benzenesulfonates / pharmacology
  • Cells, Cultured
  • Drug Evaluation, Preclinical
  • Humans
  • Naphthalenesulfonates / chemical synthesis
  • Naphthalenesulfonates / pharmacology
  • Sulfanilic Acids / chemical synthesis
  • Sulfanilic Acids / pharmacology
  • Suramin / analogs & derivatives*
  • Suramin / chemical synthesis
  • Suramin / pharmacology

Substances

  • Anti-HIV Agents
  • Antineoplastic Agents
  • Benzenesulfonates
  • Naphthalenesulfonates
  • Sulfanilic Acids
  • Suramin