Antibiotic derivatives

Oligosaccharides also occur widely as components (via glycosidic bonds) of antibiotics derived from various sources. Figure 7.20 shows the structures of a few representative carbohydrate-containing antibiotics. Some of these antibiotics also show antitumor activity. One of the most important of this type is bleomycin A2, which is used clinically against certain tumors. 

Use antibacterial, semisynthetic p-lactam antibiotic, derivative of ampicillin (prodrug for ora application)... 

A microwave assisted Comforth rearrangement of oxazole-4-carboxamides 106 efficiently afforded 5-aminooxazole-4-carboxylates 107. This procedure was applied to the formal synthesis of a natural antibiotic derived from pseudomonic acid <06TL4698>. 

Tetracyclines are a group of antibiotics derived from bacteria. Chlortet-racycline was isolated from Streptomyces aureofaciens and oxytetracycline from Streptomyces rimosus. Tetracychnes act by binding to receptors on the bacterial ribosome and inhibit bacterial protein synthesis. 

Nicas, T.I. et al. Semisynthetic glycopeptide antibiotics derived from LY264826 active against vancomycin-resistant enterococci, Antimicrob. Agents Chemother., 40, 2194, 1996. 

During the development of a sterile formulation of pirlimycin, a semisynthetic, veterinary lincosaminide antibiotic derived from lincomycin 4, three lots of material were subjected to thermal stress at 40°C for a period of 4 months, which led to the observation of a previously unreported degradant present at 0.2% [69]. 

Pharmacology Rifabutin, an antimycobacterial agent, is a semisynthetic ansamycin antibiotic derived from rifamycin S. It is not known whether rifabutin inhibits DNA-dependent RNA polymerase in Mycobacterium avium or in Mycobacterium... 

Nephrogenic diabetes insipidus is due to resistance to action of vasopressin, and therefore DDAVP is not indicated, but some benefit may be gained by using thiazide diuretics or chlorpropamide. The syndrome of inappropriate antidiuretic hormone (SIADH) can be treated by using the antibiotic derivative demeclocycline to induce a state of vasopressin resistance and partial nephrogenic diabetes insipidus. 

The cephalosporins are semisynthetic antibiotics derived from products of various microorganisms, including Cephalosporium and Streptomyces. All cephalosporins... 

Although it is not chemically related to cyclosporine, tacrolimus (6.7) has a similar mechanism of action. Tacrolimus is an immunosuppressant macrolide antibiotic derived from Streptomyces tsukubaenis. Like cyclosporine, tacrolimus inhibits the same cytoplasmic phosphatase, calcineurin, which catalyzes the activation of a T-cell-specific transcription factor (NF-AT) involved in the biosyntheses of interleukins such as IL-2. Sirolimus (6.8) is a natural product produced by Streptomyces hydroscopicus, it blocks the ability of T cells to respond to cytokines. 

JK Epp, BE Schoner. Carbomycin biosynthetic gene, carG—used for increasing yields of carbomycin and for producing new antibiotics and antibiotic derivatives. US Patent 4952502, Dec. 15, 1988. 

THE CHEMISTRY AND BIOLOGY OE VANCOMYCIN AND OTHER GLYCOPEPTIDE ANTIBIOTIC DERIVATIVES... 

Vattcomycin and other glycopeptide antibiotic derivates > Antitumor and other related activities of Taxol and its aitalogs... 

Rifamycin SV is a semi-synthetic antibiotic derived from rifamycin B, a substance produced during growth of certain strains of Streptomyces mediterranei. 

New /3-lactam antibiotics derived from natural and synthetic sources 89PHA177. 

Niphimycin, an antimycotic antibiotic derived from Actinomyces hygroscopicus, is effective against both der-matomycosis and onychomycosis, with a 16-26% success rate in the latter. Tolerance is reportedly good, but there is a notable lack of recent data (SEDA-12, 236). 

Kirrstetter R, Durckheimer W. Development of new betalactam antibiotics derived from natural and synthetic sources. Pharmazie 1989 44(3) 177-85. 

Rifamycin SV (rINN), a semisynthetic macrocyclic antibiotic derived from natural rifamycin B, has been used in the therapy of tuberculosis and in some European countries as a topical antibiotic. Anaphylaxis has been reported after systemic administration, and rarely after topical application. 

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