N-thiolated beta-lactams: a new family of anti-Bacillus agents.
This report describes the evaluation of N-thiolated beta-lactam antibiotics as potential anti-Bacillus agents. N-Thiolated beta-lactams are a new family of antibacterials that previously have been found to selectively inhibit the growth of Staphylococcus bacteria over many other genera of microbes. From the data presented herein, these lactams similarly inhibit a variety of Bacillus species, including Bacillus anthracis. The preliminary structure-activity studies suggest that there is a need to balance the lipophilic character of the C3/C4 groups in order to obtain optimal anti-Bacillus activity. Elongation or extensive branching of the organothio substituent diminishes antibacterial effects, with the sec-butylthio derivative providing the strongest activity.
Department of Chemistry, 4202 East Fowler Avenue, CHE 207, University of South Florida, Tampa, FL 33620, USA. eturos@shell.cas.usf.edu
Edward
E
Turos
Timothy E
TE
Long
Bart
B
Heldreth
J Michelle
JM
Leslie
G Suresh Kumar
GS
Reddy
Yang
Y
Wang
Cristina
C
Coates
Monika
M
Konaklieva
Sonja
S
Dickey
Daniel V
DV
Lim
Eduardo
E
Alonso
Javier
J
Gonzalez
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001407:Bacillus / Q000187:drug effects*; D001408:Bacillus anthracis / Q000187:drug effects; D024881:Drug Resistance, Bacterial; D016106:Methicillin Resistance; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship; D013438:Sulfhydryl Compounds / Q000737:chemistry; D047090:beta-Lactams / Q000138:chemical synthesis* / Q000494:pharmacology*
D000900:Anti-Bacterial Agents; D013438:Sulfhydryl Compounds; D047090:beta-Lactams