Broad-spectrum antibacterials

Aminomethyl- cyclines Amino- methyl- cycline MK-2764 (PTK-0796 BAY 73-7388) (153) Antibacterial (broad spectrum antibiotic against MRS A, MDR Streptococcus pneumoniae and vancomycin-resistant enterococci) Inhibits bacterial protein synthesis Phase III (treatment of hospital infections in both oral and i.v. injectable formulations) Paratek/Novartis 810... 

Norfloxacin (1, R = C2H5, R = H), a typical example, exhibits broad-spectrum activity and is useful in the treatment of upper respiratory tract and urinary infections [7] Lomefloxacin (2), a very recent introduction, is a third-generation product that, given once daily, is especially useful against pathogens resistant to cephalosponns, penicillins, and aminoglycosides [4] Floxacillin (J) is a stable, orally active antibacterial with improved activity over thenonfluonnated product (cloxacillin) [5]... 

There are several methods of preparation of antibacterial quinolones, drugs widely used in the therapy of various bacterial diseases. The most general method is based on the nucleophilic cyclization of 2-halobenzoyl derivatives 402, leading to the key intermediates 403. The methodology is exemplified in Scheme 63 by the synthesis of a broad-spectrum drug ciprofloxacin... 

Triclosan is a broad-spectrum antibacterial and antifungal agent. It is an ingredient in toothpastes and mouthwashes, detergents, laundry soaps, and cosmetics. It kills germs by interfering with the enzyme necessary for fatty-acid synthesis. 

Hexachlorophene is a broad-spectrum antibacterial agent. It is used in hospital scrubs, shampoos, and deodorants. 

The magaiitins are a class of hnear, cationic, faciaUy amphipathic and hehcal antibacterial peptides derived from frog skin [51]. The magaiitins exhibit highly selective and potent antimicrobial activity against a broad spectrum of organisms [52, 53]. As these peptides are faciaUy amphipathic, the magainins have a cationic heli-... 

A 43-year-old male in the surgical ICU after exploratory laparotomy following a motor vehicle accident develops fever that is unresponsive to broad-spectrum antibacterial therapy (piperacillin-tazobactam 3.75 g every 6 hours, gentamicin 120 mg every 8 hours, and vancomycin 1 g every 12 hours). The patient has a central venous catheter and a Foley catheter. Blood cultures are negative at the time, but the patient has yeast growing in the sputum and urine. Laboratory studies reveal a white blood cell count of 11,300 cells/mm3 (11.3 x 109/L). 

O A risk assessment should be performed at presentation of febrile neutropenia to identify low-risk patients for potential outpatient treatment. Patients who do not meet low-risk criteria should be hospitalized for immediate parenteral administration of broad-spectrum antibacterials before culture results are obtained. 

Triclosan is a broad spectrum antibacterial agent with antifungal and antiviral properties, widely employed in personal care products such as soaps, shampoos, toothpastes, and cosmetics [40]. Fungal-mediated degradation studies have been mainly performed by means of enzymatic processes, although a couple of whole cell transformation reports are available. 

A virtual screening on pharmacophores derived from available structures of FabH delivered YKAs3003 (10). This Schiff base displays a KV) of 20 nM against E. coli FabH but has no significant antibacterial activity [19]. Other derivatives based on similar templates have been subsequently reported, such as 11 [20] and 12 [21]. They show low micromolar IC50 s against E. coli FabH with broad-spectrum antibacterial activity... 

In order to overcome the limitations of the above drugs, a series of rifamycin derivatives with improved pharmacokinetic (i.e. virtually absence of GI absorption) and pharmacodynamic (i.e. with broad spectrum of antibacterial activity) properties have been synthesized at Alfa Wassermann laboratories [33]. Amongst the different molecules, the compound marked L-105 and later... 

Due to the frequent difficulty of doing cultures before giving an antibacterial drug, topical treatment often requires the use of broad-spectrum antibiotics. However, the selection of resistant strains, especially via the use of broad-spectrum antimicrobials with marked systemic dif-... 

Since the introduction of nalidixic acid in 1963, structural modifications on the quinolones have been performed to improve either the antibacterial efficacy or pharmacokinetic/toxicologic profiles of these compounds. The newest quinolones possess broad-spectrum activity, favorable pharmacokinetic/toxicologic profiles, and potency against bacterial strains that are resistant to older generations of quinolones. This section describes the synthetic procedures for the new generation of quinolones that were studied during the 1995-2005 period. 

In search of novel and more effective antibacterial agents, numerous /1-lactam antibiotics bearing a pyridazine core have been synthesized mainly in Japan. Thus, the penicillin derivative (125) characterized by a 3-hydroxypyridazine-4-carboxamido subunit has been patented as a broad-spectrum bactericide [342-345] likewise, the corresponding cephalosporin analogue has been claimed in a patent [346]. 

Treatment relies on the use of broad spectrum antibacterial and antifungal drugs bone marrow transplant or gene therapy are possible options. The prognosis for a child with CGD is not good and many will not live beyond their mid-teens. 

Cyclo(Pro-Trp) and cyclo(Phe-Pro) showed broad-spectrum antibacterial properties, whereas cyclo(Trp-Pro) and cyclo(Trp-Trp) exhibited broad-spectrum antifungal properties. The maturation of the gastrointestinal cells was enhanced by cyclo(Trp-Trp), cyclo(Trp-Pro), cyclo(Phe-Pro), and cyclo(Tyr-Pro). ... 

A patient who is taking phenytoin and is hypersensitive to penicillin requires a broad-spectrum antibacterial agent for a respiratory tract infection. 

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