162515-01-7Relevant articles and documents
PENAM DERIVATIVES
-
, (2008/06/13)
The present invention discloses compounds having the formula wherein one of R1 and R2 is ?COR4, ?CN, ?CH2R5. halogen. ?CH=CHR6 or Q and the other is hydrogen or lower alkyl or both R1 and R2 together form a gamma-lactam ring, R3 is hydrogen, lower alkyl. aryl-alkyl, allyl or a residue which is cleavable in vivo, R4 is hydrogen, lower alkyl, lower alkoxy. benzyloxy, amino, lower alkylamino or lower alkyl-lower alkoxyamino. R5 is hydroxy. ?OCONHR7. ?OCONH2 or a five- or six-membered hetero-aromatic ring which contains N,S and/or O and which is linked via a nitrogen atom, R6 is ?CN or CHO. R7 is ?COCH2Cl. Q is a five- or six-membered hetero-aromatic ring which contains N, S and/or O and n is 0, 1 or 2, and the pharmaceutically compatible salts thereof. These compounds are good beta-lactamase inhibitors. They can be used for the prevention or treatment of bacterial infections, optionally together with a beta-lactam antibiotic
Design, synthesis, and evaluation of 2β-alkenyl penam sulfone acids as inhibitors of β-lactamases
Richter, Hans G. F.,Angehrn, Peter,Hubschwerlen, Christian,Kania, Malgosia,Page, Malcolm G. P.,Specklin, Jean-Luc,Winkler, Fritz K.
, p. 3712 - 3722 (2007/10/03)
A general method for synthesis of 2β-alkenyl penam sulfones has been developed. The new compounds inhibited most of the common types of β- lactamase. The level of activity depended very strongly on the nature of the substituent in the 2β-alkenyl group. Th