Desethylene ciprofloxacin is a major metabolite of ciprofloxacin . It is also a degradation product of ciprofloxacin that can be created through advanced oxygenation processes as a potential way to remove ciprofloxacin from wastewater. It is also created during degradation of ciprofloxacin by chlorination.
PD 117588 is a quinolone against bacterial isolates from cancer patients. PD 117558 has a broad antimicrobial spectrum with excellent activity against all Gram-positive isolates (including methicillin-resistant Staphylococcus aureus, coagulase-negative st
Ro 24-6392 is an ester-linked co-drug combining ciprofloxacin and desacetylcefotaxime. Ro 24-6392 demonstrats activity against a wide spectrum of aerobic bacteria.
ABT-719 is a 2-pyridinone antimicrobial agent that is more effective against Enterococcus faecalis strains than ciprofloxacin and vancomycin, which showed resistance to ciprofloxacin and vancomycin covering a range of MIC.
IMP-1700 is an inhibitor of bacterial DNA repair.1It potentiates the activity of the quinolone antibiotic ciprofloxacin against methicillin-resistantS. aureus(MRSA) with a combination index value of 0.7. IMP-1700 inhibits the ciprofloxacin-induced bacterial SOS response, a process that repairs DNA damage, in a reporter assay in a concentration-dependent manner. It is also active againstE. coli, as well as methicillin-resistant and -sensitive S. aureus, when used alone (EC50s = 0.5, 0.21, and 3.8 μM, respectively). 1.Lim, C.S.Q., Ha, K.P., Clarke, R.S., et al.Identification of a potent small-molecule inhibitor of bacterial DNA repair that potentiates quinolone antibiotic activity in methicillin-resistant Staphylococcus aureusBioorg. Med. Chem.27(20)114962(2019)
Piperazine (2HCl) is gamma-aminobutyric acid (GABA) agonists and its major effects appear to be on the central nervous system. Piperazine was the anthelmintic with the greatest number of reports of toxicoses and suspected toxicoses in cats. Piperazine neurotoxicity in cats and dogs usually was manifested by muscle tremors, ataxia, and or behavioral disturbances within 24 hours after estimated daily dose(s) between 20 and 110 mg kg[1]. For di-substituted derivatives, ciprofloxacin was selected and hybrids were synthesized via substitution at piperazinyl-N4. The reaction of piperazinyl-NH of ciprofloxacin with selected drugs resulted in pronounced growth inhibition of standard as well as resistant bacterial strains[2]. The parent piperazine 6 was found to exhibit a reasonable activity toward the HeLa and MDA MB 231 tumor cell lines (IC50= 9.2 and 8.4 μΜ, respectively)[3]. Piperazine adipate (10 mM) causes mortality of A. galli and H. gallinae after a maximum of 30 min exposure, inhibits malate oxidation by 78%, and inhibits aldolase activity in both parasites. Piperazine adipate (10 mM) also inhibits cholinesterase activity by 96% in Ascaridia galli (A. galli) and 93% in Heterakis gallinae (H. gallinae). Piperazine adipate inhibits oxaloacetate reduction by 26% and 55% in A. galli and H. gallinae, resepctively[4].
Quorum Sensing-IN-2(compound 23e)是一款不影响细菌生长的群体感应抑制剂,具有减少细菌致病性的功能。该化合物在抑制细菌感染方面表现出效力,同时具有极低的溶血活性。在铜绿假单胞菌PAO1引起的菌血症模型中,Quorum Sensing-IN-2与环丙沙星共同作用,显示了协同效应。