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Topic: Ketolides

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	Telithromycin: a brief review of a new ketolide antibiotic.(ARTICLES) - Encyclopedia.com (Site not responding. Last check: 2007-10-24)
		The defining differentiating characteristic of the ketolides as opposed to other macrolides is the removal of the neutral sugar, L-cladinose from the 3 position of the macrolide ring and the subsequent oxidation of the 3-hydroxyl to a 3-keto functional group.
		The defining characteristic of the ketolides is the removal of the neutral sugar, L-cladinose from the 3 position of the macrolide ring and the subsequent oxidation of the 3-hydroxyl to a 3-keto functional group (2).
		The structure of ketolides with their ketone group at position 3 of the macrolide ring facilitates intrinsic activity against respiratory tract pathogens and prevents induction of macrolide, lincosamide and streptogramin B resistance.
	www.encyclopedia.com /doc/1G1-130058403.html (1638 words)

	ACP Online - Session Topics - New Antibiotics: When to Use and When Not to Use
		The ketolides telithromycin and ABT773 are semisynthetic macrolides.
		The ketolides are semisynthetic derivatives of the macrolides.
		In the ketolides, the cladinose sugar is removed and replaced by a ketone group, and carbon atoms C11 and C12 are modified.
	www.acponline.org /ear/vas2002/new_antibiotics.htm (2600 words)

	MEDLINE Search on Medscape.com
		levofloxacin, ciprofloxacin, moxifloxacin and grepafloxacin), ketolides (ABT-773 and telithromycin) and macrolides (clarithromycin,...
		Ketolides are a new class of antibacterials that have been specifically developed for the treatment of community-acquired respiratory tract infections in...
		Pneumococcal resistance to macrolides, lincosamides, ketolides, and streptogramin B agents: molecular mechanisms and resistance phenotypes.
	search.medscape.com /medline-search?queryText=Ketolides (394 words)

	Journal of Drugs in Dermatology: Telithromycin: a brief review of a new ketolide antibiotic
		The defining differentiating characteristic of the ketolides as opposed to other macrolides is the removal of the neutral sugar, L-cladinose from the 3 position of the macrolide ring and the subsequent oxidation of the 3-hydroxyl to a 3-keto functional group.
		The defining characteristic of the ketolides is the removal of the neutral sugar, L-cladinose from the 3 position of the macrolide ring and the subsequent oxidation of the 3-hydroxyl to a 3-keto functional group (2).
		The structure of ketolides with their ketone group at position 3 of the macrolide ring facilitates intrinsic activity against respiratory tract pathogens and prevents induction of macrolide, lincosamide and streptogramin B resistance.
	www.findarticles.com /p/articles/mi_m0PDG/is_4_3/ai_n12417033 (1290 words)

	New antibiotic next year (Site not responding. Last check: 2007-10-24)
		To create ketolides, scientists altered the structure of the so-called macrolides, a class of antibiotics that includes the popular agent erythromycin, said Bruno Leroy of Aventis.
		Ketolides are better at stopping the pumping process that allows bugs to evade destruction.
		The fact that ketolides appear to eradicate infections after only five days of treatment is important, Craig said.
	www2.lymenet.org /domino/flash.nsf/8178b1c14b1e9b6b8525624f0062fe9f/b5245205a08f823a8525696000714d61?OpenDocument (929 words)

	Ketolides -- Facts, Info, and Encyclopedia article (Site not responding. Last check: 2007-10-24)
		Ketolides are (A chemical substance derivable from a mold or bacterium that kills microorganisms and cures infections) antibiotics belonging to the (additional info and facts about macrolide) macrolide group.
		These modifications give ketolides much broader spectrum than other macrolides.
		The only ketolide on the market at this moment is (additional info and facts about telithromycin) telithromycin, which is sold under the brand name of Ketek.
	www.absoluteastronomy.com /encyclopedia/k/ke/ketolides.htm (65 words)

	Infectious Disease News
		The ketolides are a new class of semisynthetic macrolide antibiotics.
		Ketolides are a novel class of 14-membered ring macrolides characterized by the substitution of the
		The ketolides have a spectrum of activity similar to the macrolides.
	www.infectiousdiseasenews.com /200109/pharm.asp (1064 words)

	Macrolide - Wikipedia, the free encyclopedia
		There is also a new class of antibiotics called ketolides that is structurally related to the macrolides.
		Ketolides such as telithromycin are used to fight respiratory tract infections caused by macrolide-resistant bacteria.
		The drug Tacrolimus, which is used as an immunosuppressant, is also a macrolide.
	en.wikipedia.org /wiki/Macrolides (218 words)

	The American Journal of Managed Care: The Evolution of Antimicrobial Agents Used for the Management of CARTIs: A Focus ...
		Ketolides that possess a carbamate extension at positions 11/12 allows for strong binding to domain II, whereas the macrolides form a weak bond to domain II.
		Bronchopulmonary disposition of the ketolide telithromycin (HMR 3647).
		Telithromycin (HMR 3647), a new ketolide antimicrobial, is metabolized and excreted mainly in faeces in man. Proceedings of the 5th International Conference on Macrolides, Azalides, Streptogramins, Ketolides, and Oxazolidinones; Selville, Spain; January 26-28, 2000.
	www.ajmc.com /Article.cfm?Menu=1&ID=2729 (5741 words)

	Johns Hopkins Division of Infectious Diseases Antibiotic Guide (Site not responding. Last check: 2007-10-24)
		For example, the ketolide drug, telithromycin, which is active against pneumococcal strains expressing the erythromycin ribosomal methylase which results in methylation of the A2058 site, would be predicted to fail based on 3-dimensional structure considerations.
		Ketolides are a new generation of macrolide-like antibiotics which act at a similar site on the 50S ribosome but are resistant to macrolide efflux pumps and to ribosomal methylation — two prominent mechanisms of resistance in gram-positive bacteria.
		This conferred an erythromycin MIC of 128 mcg/ml and a telithromycin MIC of 0.015 mcg/ml.
	hopkins-abxguide.org /show_pages.cfm?content=F28_022502_content.html (3911 words)

	New Antibiotic Class Offers Alternative In War Against Resistant Bacteria
		A new class of antibiotics, the ketolides, is on the horizon for pneumonia and other similar conditions.
		Ketolides are derived from the macrolides, but they are chemically different, so they will kill bacteria that are resistant to macrolides.
		Reports on two varieties of ketolides were presented in Toronto on Wednesday at an infectious diseases meeting sponsored by the American Society for Microbiology.
	www.vidyya.com /archives/0922_2.htm (322 words)

	Clinical efficacy of ketolides in the treatment of respiratory tract infections -- Reinert 53 (6): 918 -- Journal of ...
		In vitro activities of cethromycin (ABT-773), a new ketolide, against Streptococcus pneumoniae strains that are not susceptible to penicillin or macrolides.
		In vitro activities of the ketolides ABT-773 and telithromycin and of three macrolides against genetically characterized isolates of Streptococcus pneumoniae, Streptococcus pyogenes, Haemophilus influenzae and Moraxella catarrhalis.
		Community-acquired respiratory tract infections caused by resistant pneumococci: clinical and bacteriological efficacy of the ketolide telithromycin.
	jac.oxfordjournals.org /cgi/content/full/53/6/918 (5331 words)

	Structural Insight into the Antibiotic Action of Telithromycin against Resistant Mutants -- Berisio et al. 185 (14): ...
		Activity of the ketolide telithromycin is refractory to Erm monomethylation of bacterial rRNA.
		A ketolide resistance mutation in domain II of 23S rRNA reveals the proximity of hairpin 35 to the peptidyl transferase centre.
		Reinert, R. Clinical efficacy of ketolides in the treatment of respiratory tract infections.
	jb.asm.org /cgi/content/full/185/14/4276?view=full&pmid=12837804 (1814 words)

	The Ket-on-Line ICAAC Update Web Site: Daily News
		These results indicate that this novel ketolide can be taken with low-dose oral contraceptives without changing their pharmacokinetics in a way that would increase the risk of ovulation.
		The ketolides are a novel class of antibiotics derived from the structure of the macrolides.
		The ketolides are a new class of antimicrobials to treat respiratory tract infections.
	www.ket-on-line.com /icaac/news.htm (10362 words)

	TVM — News Release (Site not responding. Last check: 2007-10-24)
		Ly Tam Phan, Enanta’s Director of Medicinal Chemistry and Macrolide Project Leader presented for the first time data on a new class of antibacterial agents, discovered at Enanta, that are effective against antibiotic resistant Streptococcus pneumoniae and are being developed for the treatment of respiratory tract infections.
		Ketolides are emerging as particularly significant antibacterial agents, demonstrating potent activity against specific resistant organisms.
		The studies demonstrate that this new class of compounds is effective against macrolide and penicillin resistant strains of Streptococci and have potent efficacy in preclinical infection models.
	www.tvmvc.com /site/news/2003/ena0325.html (576 words)

	Antibiotic-Consult.com (Site not responding. Last check: 2007-10-24)
		Telithromycin is the first of the ketolides, a new class of antibacterial drugs that are derived from macrolide antibiotics.
		The only chemical modification necessary to classify a drug as a ketolide is replacement of the a-L-cladinose moiety at position 3 of the 14-membered erythronolide A ring of the macrolide with a keto function.
		The primary binding site of the macrolides and ketolides is with domain V of the 23S rRNA, where binding is a result of interactions between the erythronolide A ring of the macrolide/ketolide and several nucleotides within the central loop.
	www.antibiotic-consult.com /secure/consensusreports/drugcriteria1.htm (896 words)

	New drugs kill bacteria resistant to antibiotics (Site not responding. Last check: 2007-10-24)
		Reports on two varieties of ketolides were presented in Toronto yesterday at an infectious diseases meeting sponsored by the American Society for Microbiology.
		Because the ketolides are chemically different, the resistant bacteria do not spit them out.
		Dr. William Craig of the University of Wisconsin called the ketolides "a major step" because they give new life to the macrolides, which have long been used and have a good safety record.
	seattlepi.nwsource.com /national/medi213.shtml (346 words)

	EP-013420, Enanta
		Enanta is currently developing I.V. formulations for Enanta macrolides and ketolides to be used for the treatment of bacterial infections in the hospital.
		Macrolide and ketolide antibiotics have been used and studied in numerous specialty indications outside of community respiratory tract infections, including cystic fibrosis, acne, ocular infections, otic infections, dental infections, and nasal infections.
		These bridged macrolides and ketolides have been designed by Enanta to have optimal pharmacokinetics and to provide broad treatment against respiratory pathogens, including several multi-drug resistant strains for which traditional macrolides, penicillins, and fluoroquinolones are no longer effective, making these compounds ideal community respiratory tract infection drugs.
	www.enanta.com /ep-13420.html (822 words)

	CDC - Dead Bugs Don’t Mutate: Susceptibility Issues in the Emergence of Bacterial Resistance
		Telithromycin, the first of a new class of antibacterials, the ketolides, is approved for use in Europe and is currently being reviewed by the U. Food and Drug Administration (71).
		This similarity is not surprising, as the ketolides are novel semisynthetic erythromycin-A derivatives structurally similar to clarithromycin.
		Antipneumococcal activities of a ketolide (HMR 3647), a streptogramin (quinupristin-dalfopristin), a macrolide (erythromycin), and a lincosamide (clindamycin).
	www.cdc.gov /ncidod/EID/vol9no1/02-0172.htm (5131 words)

	In Vitro Activities of Novel 2-Fluoro-Naphthyridine-Containing Ketolides -- Abbanat et al. 49 (1): 309 -- Antimicrobial ...
		isolates, the MIC of the ketolides was 0.25 µg/ml.
		Pharmacodynamic properties of HMR 3647, a novel ketolide, on respiratory pathogens, enterococci and Bacteroides fragilis demonstrated by studies of time-kill kinetics and postantibiotic effect.
		Clinical and bacteriological efficacy of the ketolide telithromycin against isolates of key respiratory pathogens: a pooled analysis of phase III studies.
	aac.asm.org /cgi/content/full/49/1/309 (2926 words)

	[No title]
		The comparison of ketolide activities with those of the other macrolides shows a much better activity in the majority of species, with macrolide MICs at which 90% of the isolates are inhibited between 8- and 10-fold higher.
		The ketolides HMR 3004 and HMR 3647 (telithromycin) are a new class of macrolides that have a potential clinical efficacy against intracellular pathogens.
		The activity of the ketolide telithromycin (HMR 3647) against intracellular Legionella pneumophila strain L-1033 was compared with the activities of erythromycin and levofloxacin.
	www.infectionkorea.org /infection/news/telithromycin.html (3758 words)

	UpToDate Resistance of Streptococcus pneumoniae to the macrolides, azalides, lincosamines, and ketolides
		Resistance of Streptococcus pneumoniae to the macrolides, azalides, lincosamines, and ketolides
		Macrolides, azalides, lincosamines and ketolides are related drugs that inhibit protein synthesis at the same site in the bacterial ribosome and are generally active against the same microorganisms.
		Macrolides, azalides, and ketolides are (or, at least, used to be) generally active against Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis, Legionella species, Chlamydia pneumoniae and Mycoplasma pneumoniae.
	patients.uptodate.com /topic.asp?file=pulm_inf/9089 (444 words)

	ICC: Telithromycin Effective For Treating Pneumococcal Pneumonia
		AMSTERDAM, THE NETHERLANDS -- July 3, 2001 -- Telithromycin (Ketek®), a new antibacterial agent belonging to the class of new agents termed ketolides, is highly effective for the treatment of patients with pneumococcal bacteremia associated with community acquired pneumonia (CAP).
		Ketolides are modified macrolides and differ from the macrolides in that they retain activity against a number of bacterial strains that are resistant to conventional macrolides like erythromycin and clarithromycin.
		Telithromycin is the first ketolide to reach the market and is available as an oral preparation.
	www.docguide.com /dg.nsf/PrintPrint/E72549A21C29F98285256A7E005F3C05 (520 words)

	Telithromycin (Ketek)
		The ketolides differ from the macrolides in that they are missing the L-cadinose at C3 and have an added substituted carbamate at C11/12.
		Binding of the ketolide occurs to domain V (Adenine 2058 and 2059) and domain II (Adenine 752).
		A ketolide resistance mutation in domain II of 23S rRNA reveals the proximity of hairpin 35 to the peptidyl transferase center.
	connection.lww.com /products/foye/documents/DrugUpdates/DrugUpdate34-04.asp (295 words)

	Introduction to Antimicrobial Testing and Empiric Therapy
		Ketolides and other members of the macrolide-lincosamide-streptogramin B class achieve their antimicrobial effect by blocking bacterial protein synthesis.
		The sequence of amino acids in the protein is specified by the nucleotide sequence of the mRNA, and is translated by the ribosome.
		The ketolides bind at two sites close to the ribosome active site, which results in inhibition of one of the steps (peptidyl transferase activity) required for adding new amino acids from the transfer RNA (tRNA) molecules to the growing peptide chain.
	spahp.creighton.edu /destache/PPTFall_2002/id_intro1_files/slide0187.htm (116 words)

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