Synthesis and antimicrobial and cytotoxic activities of pyrrole-containing analogs of trichostatin A

• Published in: Journal of medicinal chemistry 1990-10, Vol.33 (10), p.2845-2849
• Main Authors: Massa, S, Artico, Marino, Corelli, F, Mai, A, Di Santo, R, Cortes, S, Marongiu, M. E, Pani, A, La Colla, P
• Format: Article
• Language: English
• Subjects: Animals; Anti-Bacterial Agents - chemical synthesis; Anti-Bacterial Agents - chemistry; Antifungal Agents - chemical synthesis; Antifungal Agents - chemistry; Antiviral Agents - chemical synthesis; Antiviral Agents - chemistry; Cell Division - drug effects; Cell Survival - drug effects; Chemical Phenomena; Chemistry; Chemistry, Physical; Dose-Response Relationship, Drug; Exact sciences and technology; Heterocyclic compounds; Heterocyclic compounds with only one n hetero atom and condensed derivatives; Hydroxamic Acids - antagonists & inhibitors; Hydroxamic Acids - chemical synthesis; Hydroxamic Acids - chemistry; Organic chemistry; Preparations and properties; Pyrroles; Regression Analysis; Structure-Activity Relationship; Vero Cells
• ISSN: 0022-2623; 1520-4804
• DOI: 10.1021/jm00172a026

A number of aroylpyrroleacrylic acid derivatives were synthesized by standard procedures and evaluated for cytotoxicity in Vero cells and for capacity to inhibit the multiplication of viruses, bacteria, and fungi. While none of the test compounds showed any activity against bacteria and fungi, most of them inhibited the replication of some DNA viruses at concentrations allowing the exponential growth of uninfected cells. In particular three compounds (8, 9c, and 10h) showed an antiviral activity at doses that were from 4- to greater than 8-fold lower than the maximum nontoxic doses.