Cefazaflur (INN) is a semisynthetic first-generation cephalosporin antibiotic patented by Smithkline Corp. For treatment of bacterial infections.

Cefcanel is a semisynthetic third-generation cephalosporin with antibacterial activity. Cefcanel is active against the species E. coli, K. aerogenes and Proteus mirabilis; H. influenzae and M. catarrhalis has reasonable susceptibility. Cefcanel inhibits 90% of S. aureus strains at 2 µg/ml, irrespective of the presence of a β-lactamase. Cefcanel binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.

Fumoxicillin was developed as an antibacterial agent that binds to penicillin-binding protein and inhibits the bacterial cell wall biosynthesis. Information about the current development of this compound is not available.

Levopropylcillin – is a penicillin derivative, L-enantiomer of antibiotic Propicillin. Levopropylcillin properties are similar to benzylpenicillin particularly used in streptococcal infections, not resistant to penicillinase. Levopropylcillin is acid resistant and can be used orally as the potassium salt.

Zabofloxacin (also known as DW-224a), a fluoroquinolone antibiotic agent, is a dual inhibitor of both DNA gyrase and topoisomerase IV of Streptococcus pneumonia. Zabofloxacin successfully has completed phase III clinical trial in patients with acute bacterial exacerbation of the chronic obstructive pulmonary disease. In addition, in May 2012, IASO terminated phase II trial of oral zabofloxacin capsules in patients with moderate-to-severe community-acquired pneumonia due to financial considerations.

Cetefloxacin is an oral fluoroquinolone derivative with potent antibacterial activity against a broad spectrum of microorganisms being particularly active against gram-positive bacteria. Cetefloxacin is highly toxic and mortality was recorded among rats receiving 2000 or 1000 mg/kg/d. Rats receiving dosages of 450 or 2000/1000 mg/kg/d showed less activated mandibular lymph nodes, cortical lymphocyte depletion of mandibular and/or mesenteric lymph nodes, atrophy of the white pulp of the spleen, cortical atrophy of thymus and thymic apoptosis. Enlarged caeca, increased water consumption and variations in plasma electrolyte levels were observed in animals receiving these dosages and in male rats receiving 100 mg/kg/d. Low neutrophil counts were observed in rats receiving dosages of 100 or 450 mg/kg/d, and increased alkaline phosphatase and alanine transaminase plasma levels and slightly decreased plasma protein levels in females receiving 450 or 2000/1000 mg/kg/d. Marmosets receiving dosages of 50 mg/kg/d and above displayed several clinical signs which included emesis, diarrhoea, ptosis, occasional episodes of under- and overactivity, and excessive scratching activity. Skin reddening was observed during the first week of treatment in marmosets receiving 300 mg/kg/d.

Droxacin is quinolone antibiotic. It is topoisomerase inhibitor.

Vebufloxacin (OPC-7241) is a nalidixic acid analog. It exhibited potent antibacterial activity against gram-positive and -negative bacteria, including Staphylococcus aureus and Pseudomonas aeruginosa.

Guamecycline, a tetracycline derivative was studied in patients with broncho-pulmonary diseases and for the treatment of acute pneumopathies. However, information about the current use of this compound is not available.

Brobactam is a synthetic inhibitor of beta-lactamases produced by both gram-positive and gram-negative bacteria. Brobactam potentiates the antibacterial activity of ampicillin against a wide range of clinically important bacterial strains which produce beta-lactamase. No resistant sub-population was observed amongst the strain s of staphylococci studied, and the development of resistance in vitro was not recorded in individual strains of Staphylococcus aureus and Escherichia coli exposed to subinhibitory concentrations of ampicillin/brobactam. Reduced sensitivity was observed in the case of one strain of M. morganii, which was known to produce an inducible chromosomal cephalosporinase.