Synthesis and antimicrobial and cytotoxic activities of pyrrole-containing analogues of trichostatin A.
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.
Massa
S
S
Dipartimento di Studi Farmaceutici, Università di Roma La Sapienza, Italy.
Artico
M
M
Corelli
F
F
Mai
A
A
Di Santo
R
R
Cortes
S
S
Marongiu
M E
ME
Pani
A
A
La Colla
P
P
D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry; D002455:Cell Division / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004305:Dose-Response Relationship, Drug; D006877:Hydroxamic Acids / Q000037:antagonists & inhibitors / Q000138:chemical synthesis / Q000737:chemistry; D011758:Pyrroles; D012044:Regression Analysis; D013329:Structure-Activity Relationship; D014709:Vero Cells
D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D000998:Antiviral Agents; D006877:Hydroxamic Acids; D011758:Pyrroles; C012589:trichostatin A