Disease relevance of Azactam

• Aztreonam, the first member of the monobactam class of monocyclic beta-lactam antibiotics, is highly active against most gram-negative aerobic bacteria, including Pseudomonas aeruginosa [1].
• Aztreonam, a new monobactam antibiotic with specific gram-negative aerobic activity, was used in combination with clindamycin in the treatment of 40 women with pelvic infection, including post-partum endometritis, pelvic inflammatory disease, and post-hysterectomy pelvic cellulitis [2].
• The studies suggest that monobactams are intrinsically active against both gram-positive and gram-negative bacteria; the activity spectrum of a given monobactam is determined by the binding to essential PBPs, which in turn is determined by the nature of the substituents on the beta-lactam nucleus [3].
• The new monobactam was inhibitory and bactericidal against the majority of diarrhea-causing members of the family Enterobacteriaceae at concentrations of less than and equal to 8 micrograms/ml [4].
• The activities of seven broad spectrum cephalosporins, four other beta-lactam antibiotics, and one monobactam against Chlamydia trachomatis were measured in a cell culture system [5].

High impact information on Azactam

• The refined structure of the acyl-enzyme formed with the monobactam inhibitor aztreonam at 2.5-A resolution defines the enzyme's active site and, along with molecular modelling, indicates a mechanism for beta-lactam hydrolysis [6].
• Cephalosporin C, the monobactam analog of penicillin G and (2,3)-alpha-methylene benzylpenicillin have been mapped at 2.3 A resolution in the form of acyl-enzyme complexes bound to serine 62 [7].
• The observed substituent effects due to the presence of the 3-formylamino and the SO(3) groups attached to the beta-lactam ring are crucial factors determining the hydrolysis of monobactam antibiotics [8].
• Aztreonam, a new monobactam, has several advantages over gentamicin including less toxicity, more dependable blood levels and good coverage of N. gonorrhoeae and the Enterobacteriaceae [9].
• In vitro antimicrobial activity of tigemonam, a new orally administered monobactam [10].

Chemical compound and disease context of Azactam

• Tigemonam, a new monobactam with excellent activity against gram-negative bacteria, was evaluated for in vivo efficacy and absorption after oral administration to laboratory animals [11].
• Aztreonam, a synthetic monobactam antimicrobial agent specifically active against aerobic, gram-negative microorganisms, was studied in combination with the extended-spectrum penicillins azlocillin and piperacillin against 46 strains of Pseudomonas aeruginosa [12].
• MM 42842, a new member of the monobactam family produced by Pseudomonas cocovenenans. I. Identification of the producing organism [13].
• SQ 28,332, a new monobactam produced by a Flexibacter sp. Taxonomy, fermentation, isolation, structure determination and biological properties [14].
• Minimal inhibitory concentrations of the monobactam carumonam (RO 17-2301) and twelve other antimicrobials were determined using agar dilution against 140 recent non-replicate clinical isolates of Pseudomonas aeruginosa [15].

Biological context of Azactam

• Multiple-dose pharmacokinetics of the monobactam azthreonam (SQ 26,776) in healthy subjects [16].
• Immunology of the monobactam aztreonam [17].
• Oral bioavailability of the monobactam aztreonam (SQ 26,776) in healthy subjects [18].
• Monobactam antibiotics in subinhibitory concentrations enhance opsonophagocytosis and serum bacteriolysis in certain Escherichia coli strains [19].
• Aztreonam (Az), a minimally absorbable monobactam antibiotic, was compared to colistin plus neomycin (CN), for intestinal decontamination during Bone Marrow Transplantation (BMT) in a controlled study [20].

Anatomical context of Azactam

• A multicenter trial involving several urologic units in Italy provided pooled data on 1,427 patients with urinary tract infections to evaluate the efficacy and safety of aztreonam, a new monobactam antibiotic [21].
• The phagocytic killing activity of macrophages was enhanced by penicillins, cephems, and monobactam in the absence of antibodies specific to the capsule or complement [22].
• Fourteen cephalosporins, 11 penicillins and 1 monobactam were evaluated for their in vitro modulation of murine neutrophil cytokinesis [23].
• Moreover, addition of the monobactam to a growing culture inhibited cell wall synthesis [24].
• Possible clinical use of a recombinant human granulocyte colony stimulating factor (rG-CSF) and a newly developed monobactam antibiotics (Aztreonam) for the treatment of gram-negative sepsis was investigated [25].

Associations of Azactam with other chemical compounds

• In vitro evaluation of tigemonam, a novel oral monobactam [26].
• Pharmacokinetics and tissue penetration of carumonam, a new synthetic monobactam [27].
• Forecasting cephalosporin and monobactam antibiotic half-lives in humans from data collected in laboratory animals [28].
• Unchanged aztreonam accounted for 77 to 86% of the radioactivity excreted in the urine of rats, dogs, and monkeys; SQ 26,992, the metabolite resulting from hydrolysis of the monobactam ring, accounted for 10 to 15%; and minor, unidentified metabolites accounted for the remainder [29].
• Syn 2190, a 1,5 dihydroxy-4-pyridon monobactam inhibitor of AmpC enzymes, was tested against beta-lactamase-producing bacteria with piperacillin, piperacillin-tazobactam and ceftazidime as partner drugs [30].

Gene context of Azactam

• In vitro activity and beta-lactamase stability of a new monobactam, B0-1165 [31].
• Monobactam antibiotics selectively inhibit penicillin-binding protein 3 (PBP3), resulting in abnormally structured peptidoglycan, causing defective cell surface structures [19].
• BACKGROUND: Aztreonam lysinate for inhalation (AI) is a novel monobactam formulation being investigated for pulmonary Pseudomonas aeruginosa infections in patients with cystic fibrosis (CF) [32].
• Aztreonam is a new, totally synthetic beta-lactamase agent--the first monobactam [33].
• Synthesis and antibacterial activity of C-4 thio- and dithiocarbamate monobactam derivatives [34].

Analytical, diagnostic and therapeutic context of Azactam

• The monobactam can be cleared by hemodialysis but is only minimally cleared by peritoneal dialysis [35].
• The metabolism and pharmacokinetics of aztreonam (SQ 26,776) were studied in four healthy male volunteers, each of whom received single 500-mg intravenous and intramuscular doses of 14C-labeled drug according to a two-way crossover design [36].
• The pharmacokinetics of the monobactam carumonam (Ro 17-2301) as derived from serial measurement of the concentrations of this agent in serum, blister fluid, and urine were studied in six male volunteers subsequent to intravenous infusion of a single 2-g dose [27].
• The results of early clinical trials comparing aztreonam with aminoglycosides for treatment of Gram-negative bacterial pneumonias indicate that this monobactam antibiotic is a safe, effective alternative to aminoglycoside therapy [37].
• Serum bacteriolysis studies revealed that of the four K-encapsulated strains tested only one strain showed a significant enhancement of bacteriolysis after treatment with subinhibitory concentrations of monobactam antibiotics [19].

References