- Structure-activity relationship (SAR) studies on oxazolidinone antibacterial agents. 2.1) Relationship between lipophilicity and antibacterial activity in 5-thiocarbonyl oxazolidinones
-
5-Thiourea and 5-dithiocarbamate oxazolidinones were synthesized as a continuation of research on 5-thiocarbonyl oxazolidinone antibacterial agents considering the hydrophobic parameters of the molecule. The structure-activity relationship (SAR) study revealed that the antibacterial activity on 5-thiocarbonyl oxazolidinones was significantly affected by the lipophilicity, especially the calculated log P value and the balance between 5-hydrophilic (or hydrophobic) substituent and hydrophobic (or hydrophilic) substituents on the benzene ring. Some of 5-thiocarbonyl oxazolidinones were found to have good in vitro antibacterial activity against gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE).
- Tokuyama,Takahashi,Tomita,Tsubouchi,Yoshida,Iwasaki,Kado,Okezaki,Nagata
-
p. 353 - 360
(2007/10/03)
-
- THIOCARBAMIC ACID DERIVATIVES
-
Thiocarbamic acid derivatives represented by the following general formula or salts thereof which are useful as antibacterial agents: wherein R1 represents an alkyl group which may be substituted, or a cycloalkyl group which may be substituted; and R2, R3, and R4 independently represent hydrogen atom, a halogen atom, an alkyl group which may be substituted, an alkogyl group which may be substituted, an amino group which may be substituted, an alkanoyl group which may be substituted, a cycloalkyloxy group which has a heteroatom as a ring constituting atom and which may be substituted, or a saturated heterocyclic group which may be substituted; or any two of R2, R3, and R4 may bind to each other to form, together with the benzene ring, a condensed hydrocarbon ring which may be substituted.
- -
-
-