There into clinical practice. Telithromycin was developed
There is an increasing number ofantibiotic resistance bacterial strains in the worldwide. As a result of thiscondition, lots of researcher focused on discovering new antimicrobial agentsfor treating patogenic diseases and a number of new agents were discovered.Theseagents show considerable improved activity against bacteria that haveresistance or show lower sensitivity to previous antimicrobialagents. Changing the chemical structure of molecules and introduction ofmolecules with new chemical structure have provided agents able to overcome thepresent resistance mechanism. These searces are especially at penicillins,quinolones and macrolides.Eritromycin is the well-known macrolideand it was discovered in early 1950s.
After this, macrolide antibiotics used fortreating Streptococcus pneumoniae infections.At the same time, macrolides have wide spectrum antimicrobial activity againstpatogens.The one of the advantages of macrolides is that it is an alternatetreatment of b-lactam intolerant patients.
But, in the last two decades, there isan increasing resistance to macrolides such as erythromycin, azithromycin andclathromycin. To overcome this problem, ketolides were developed. Ketolides arederivated from eritromycin and they are semisynthetic derivatives oferitromycin. They have higher ribosomal binding affinity because of secondaryinteraction.The main chemical characteristics of a ketolide is the displacementof cladinose with a ketone moiety.Telithromycin is the first availableoral ketolide. It is confirmed by the US Food and Drug Administration (FDA) in2001 and it is introduced into clinical practice.
Telithromycin was developedat Aventis and reached the market as Ketek. Telithromycin is used for treatment of respiratorytract infections such as mild-to-moderately-severe CAP, chronic bronchitis andacute bacterial sinusitis. Also it is quite effective against macrolideresistant Streptecoccus pneumoniae 2. CHEMICAL and PHYSICAL PROPERTIES of TELITHROMYCIN· Molecular formula of telithromycin is C43H65N5O10· Molecularweight of telithromycin is 812.018 g/mol.· Telithromycin has 1 hydrogen bond donor· Telithromycin has 13 hydrogen bond acceptor· Telithromycin has 11 rotatable bond· Formal charge of telithromycin is 0· Telithromycin has 13 defined atom stereocenter· Telithromycin has 1 covalently bonded unit· Telithromycin is canonicalized compound· Log P value of telithromycin is 3· Water solubility of telithromycin is 300 mg/L· Melting point of telithromycin is between 176 °C and 188 °C
