Synthetic Antibacterial Agents

Kirk-Othmer Encyclopedia of Chemical Technology (4th Edition) 

---

Chemically synthesized antimicrobials used in animal and poultry feeds include arsenicals, eg, arsanilic acid [98-50-0] sodium arsanilate [127-85-5] and roxarsone [121-19-7]-, sulfa dmgs, eg, sulfadimethoxine [122-11-2], sulfamethazine [57-68-1], and sulfathiazole [72-14-0]-, carbadox [6804-07-5]-, and nitrofurans, eg, furazoHdone [67 5-8] and nitrofurazone [59-87-0] (see Antibacterial agents, synthetic Antiparasitic agents). 

A Acetylation, O-Phosphorylation, and O-Adenylylation. A/-Acetylation, O-phosphorjiation, and O-adenyljiation provide mechanisms by which therapeutically valuable aminocyclitol antibiotics, eg, kanamycia [8063-07-8] gentamicin [1403-66-3] sisomicin [32385-11-8], streptomycia [57-92-1], neomycin, or spectinomycin are rendered either partially or completely iaactive. Thus, eg, kanamycia B [4696-78-8] (50) can be iaactivated by modification at several sites, as shown. The elucidation of these mechanisms has allowed chemical modification of the sites at which the iaactivation occurs. Several such bioactive analogues, eg, dibekacia and amikacin have been prepared and are not subject to the iaactivation hence, they inhibit those organisms against which the parent antibiotics are iaeffective (96) (see Antibacterial agents, synthetic). 

Although the antibacterial spectmm is similar for many of the sulfas, chemical modifications of the parent molecule have produced compounds with a variety of absorption, metaboHsm, tissue distribution, and excretion characteristics. Administration is typically oral or by injection. When absorbed, they tend to distribute widely in the body, be metabolized by the Hver, and excreted in the urine. Toxic reactions or untoward side effects have been characterized as blood dyscrasias crystal deposition in the kidneys, especially with insufficient urinary output and allergic sensitization. Selection of organisms resistant to the sulfonamides has been observed, but has not been correlated with cross-resistance to other antibiotic families (see Antibacterial AGENTS, synthetic-sulfonamides). 

ANTIBACTERIAL AGENTS SYNTHETIC - SULFONAMIDES] (Vol 2) p-Ammobenzoic acid (PABA) [150-13-0]... 

---