426253-93-2Relevant academic research and scientific papers
NOVEL BETA-LACTAM COMPOUNDS AND PROECSS FOR PRODUCING THE SAME
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, (2008/06/13)
1. A β-lactam compound of the formula [1]; ???wherein R1 is a lower alkyl, a lower alkyl substituted by a hydroxy; R2 is a hydrogen, a lower alkyl; X is O, S, NH; m and n are 0 to 4, Y1 is a halogen, cyano, a hydroxy, an amino, a lower alkyloxy, a lower alkylamino, a carboxy, a carbamoyl, a lower alkyl, etc., Y2 is hydrogen, an alkyl, cyano, -C(R3)=NR4 (wherein R3 and R4 are hydrogen, an amino, an alkyl, etc., or R3 and R4 may combine each other together with the nitrogen atom to form a 5- to 7-membered heterocyclic group), or a pharmaceutically acceptable salt thereof, or a non-toxic ester thereof, which has an excellent antibacterial activity against Gram-positive bacteria, especially against MRSA and MRCNS.
New anti-MRSA and anti-VRE carbapenems: Synthesis and structure-activity relationships of 1β-metyl-2-(thiazol-2-ylthio)carbapenems
Sunagawa, Makoto,Itoh, Masanori,Kubota, Kubota,Sasaki, Akira,Ueda, Yutaka,Angehrn, Peter,Bourson, Anne,Goetschi, Erwin,Hebeisen, Paul,Then, Rudolf L.
, p. 722 - 757 (2007/10/03)
Discovery of novel antimicrobial agents effective against infections caused by drug-resistant pathogens is an important objective. In order to find a new parenteral carbapenem antibiotic, which has potent antibacterial activity especially against methicillin-resistant staphylococci, vancomycin-resistant enterococci and penicillin-resistant Streptococcus pneumoniae, a series of 1β-methylcarbapenems with thiazol-2-ylthio groups at the C-2 position have been synthesized. Structure-activity relationships were investigated which led to SM-197436 (27), SM-232721 (44) and SM-232724 (41), being selected for further evaluation.
