A new class of cephalosporin compounds having benzopyran, benzothiopyran, and derivatives thereof, in the side chain portion of the cephalosporin molecule.

FtsZ, the bacterial analog of tubulin, is a promising new target for developing new antibiotics. It has been shown that polyphenols inhibit the GTPase activity of FtsZ, thereby inhibiting Z-ring formation during mitosis. The present invention provides novel polyphenols compounds, which can be accessed by the synthesis of dichamametin and 2''-hydroxy-5'-benzylisouvarinol-B as described herein. These novel compounds are useful in treating infections, particularly infections caused by gram-positive organisms. Methods of preparing the inventive compounds are also provided. The compounds are prepared by the benzylation of pinocembrin or chrysin core structure. Pharmaceutical compositions and method of using the compounds to treat disease are also provided. These compounds may be screened for antimicrobial activity as well as other biological activities such as anti-neoplastic, anti-inflammatory, immunosuppressive, and cytotoxic activity.

7-substituted cephalosporin compounds

Synthesis of Inhibitors of FtsZ

Novel cephem compounds represented by a formula [I] and pharmacologically admissible salts or capable of physiologically hydrolyzable nontoxic esters thereof are disclosed. ##STR1## [wherein R1 indicates a straight-chain or branched lower alkyl group, which may be substituted by carboxyl group which may be protected, trityl group, hydrogen atom or fluorine-substituted lower alkyl group, R2 indicates a hydrogen atom, metal atom, protective group for carboxyl group or ester residue producible hydrolyzable ester in vivo, R3, R4, R5 and R6, which may be identical or different, indicate hydrogen atoms, halogen atoms, straight-chain or branched lower alkyl groups, which may be substituted, mercapto groups, which may be substituted, lower alkylamino groups, hydroxyl groups, which may be protected, lower alkoxy groups, lower alkanoyl groups, lower alkoxycarbonyl groups, or lower alkylenedioxy groups, which may be substituted, being maybe formed with R3 and R4, R7 indicates a hydrogen atom, cyano group, halogen atom or COOR8 (R8 is hydrogen or lower alkyl group), R9 indicates an amino group, which may be protected, Z indicates N or CH, and n indicates 0 or 1]. Preparation processes for them and antibacterial agents containing them as effective ingredients are also claimed.

Cephem compounds, and antibacterial agents

N-(Substituted chromone-3-carbonyl)phenylglycine derivatives. These derivatives are useful intermediates for cephem compounds which are excellent as antibacterial agents.

7-substituted cephalosporin compounds

Citations

Synthesis of Inhibitors of FtsZ

Cephem compounds, and antibacterial agents

N-(Substituted chromone-3-carbonyl)-phenylglycine derivatives