What are erythromycin derivatives?

What are erythromycin derivatives?

A second generation of erythronolide-modified derivatives: roxithromycin, clarithromycin, azithromycin, dirithromycin and flurithromycin, have been synthesized and have exhibited significant improvements in pharmacokinetic and/or microbiological features.

Is erythromycin a semisynthetic drug?

1 Introduction. Macrolide antibiotics, represented by erythromycin A (1), are large polyketide natural products and their semisynthetic derivatives.

What is the 6 methyl derivative of erythromycin?

The 6-O-methyl ether of erythromycin A, clarithromycin is a macrolide antibiotic used in the treatment of respiratory-tract, skin and soft-tissue infections. It is also used to eradicate Helicobacter pylori in the treatment of peptic ulcer disease.

What is a semisynthetic antibiotic?

Semi-synthetic antibiotics are derivatives of natural antibiotics with slightly different but advantageous characteristics. For example, they can act against bacteria which are resistant to the original compound, have a greater spectrum of activity or cause fewer side effects.

Is azithromycin a derivative of erythromycin?

Azithromycin and clarithromycin are derivatives of the older macrolide antibiotic erythromycin. They are used in the treatment of a variety of infections, including community-acquired respiratory tract infections and mycobacterial infections.

Which of the following is the general mechanism of action for erythromycin?

Erythromycin acts by inhibition of protein synthesis by binding to the 23S ribosomal RNA molecule in the 50S subunit of ribosomes in susceptible bacterial organisms.

What is the chemical name for erythromycin?

(3R,4S,5S,6R,7R,9R,11R,12R,13S,14R)-6- {[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy}- 14-ethyl-7,12,13-trihydroxy-4-{[(2R,4R,5S,6S)- 5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy}- 3,5,7,9,11,13-hexamethyl-1-oxacyclotetradecane-2,10-dioneErythromycin / IUPAC ID

What is the mechanism of action of erythromycin?

What is the specific molecular target of erythromycin?

Erythromycin is a broad-spectrum, macrolide antibiotic with antibacterial activity. Erythromycin diffuses through the bacterial cell membrane and reversibly binds to the 50S subunit of the bacterial ribosome. This prevents bacterial protein synthesis.

What is the difference between natural and semisynthetic penicillin?

Penicillin can be divided into two groups, namely natural and semisynthetic penicillins. Natural penicillins are produced from the fermentation of the fungus Penicillium chrysogenum. The semisynthetic penicillins, on the other hand, are prepared from (+)-6-aminopenicillanic acid.

What is semisynthetic penicillin?

Amoxycillin (α-amino-p-hydroxybenzylpenicillin) is a new semi-synthetic penicillin with a broad spectrum of antibacterial activity similar to that of ampicillin. Penicillin-sensitive strains of staphylococci, streptococci, and pneumococci were sensitive to concentrations of 0·1 μg or less of amoxycillin/ml.

Is erythromycin a semi-synthetic product?

All of the commercially available derivatives of erythromycin as well as those in various stages of development are semi-synthetic products. The rationale for synthesis of many of these derivatives has been largely influenced by the mechanism of decomposition of erythromycin.

What is the metabolism of erythromycin and its derivatives?

The metabolism of erythromycin and its semi-synthetic derivatives has been recently reviewed [276]. Among the most common metabolic pathways of 14-membered macrolides are N-demethylation of the aminosugar and hydrolysis of the neutral sugar. Oxidative N-demethylation involving cytochrome P-450 is a major route of erythromycin metabolism [277].

What is telithromycin (Ketek)?

Telithromycin (Ketek™), a semisynthetic derivative of erythromycin A with pyridylimidazole-alkyl side chain, belongs to the third generation of macrolide antibiotics, the so-called ketolides <01CMC1727, 04NRDD733>. The first generation of macrolide antibiotics includes 14-membered macrolides such as erythromycin, oleandomycin, and megalomicin.

Is there a second generation of erythronolidemodified derivatives of azithromycin?

A second generation of erythronolidemodified derivatives: roxithromycin, clarithromycin, azithromycin, dirithromycin and flurithromycin, have been synthesized and have exhibited significant improvements in pharmacokinetic and/or microbiological features.