Antiinfective agents

L-Dopa and Trimethoprim are two other dmgs that can be made from vanillin. u-Dopa is used for the treatment of Parkinson s disease Trimethoprim is an antiinfective agent used mainly for urinary tract infections and certain venereal diseases. Also, Mebeverine, an antispasmodic agent, and Verazide, a generic antitubercular agent, are dmgs that can be made from vanillin or its derivatives. 

As demonstrated above, nitro derivatives of five-membered heterocycles have found extensive use as antiinfective agents. It is therefore of interest that the nitro derivative of a substituted thiazole was at one time used as an antitrichomonal agent. Bro-mination of 2-aminothiazole (136) (obtained from condensation of thiourea with chloroacetaldehyde) gives the 4-bromo derivative (138) this is then acetylated to 139. Treatment of 139 with nitric acid leads to an interesting displacement of bromine by a nitro group to afford aminitrazole (140)... 

The finding that 2,4-diaminopyrimidines inhibit the growth of microorganisms by interfering with their utilization of folic acid led to an intensive search for antiinfective agents in this class of heterocyclic compounds. This work led to the develop-... 

Bentley P.H. Ponsford R. (199 3) Recent Advances in the Chemistry of Antiinfective Agents. London Royal Society of Chemistry. 

Khalifa AE. Antiinfective agents affecting cognition a review. J Chemother 2007 19(6) 620-31. 

A U H It NO, lis salt with 7-(phenylacetylaniino)-ccphnlosporanic acid is an antiinfective agent 906... 

The presence of food in the GI tract reduces the absorption of many antiinfective agents. Although there are some exceptions (e.g., penicillin V, amoxicillin, and doxycycline), it is generally recommended that penicillin and tetracycline derivatives, as well as certain other antiinfective agents, be given at least 1 h before meals or 2 h after meals to achieve optimum absorption. 

Bicillin benzathin penicillin, bicozamycin [inn] is a diketopiperazine antibiotic. It can be used as an ANTIBACTERIAL antiinfective agent for gut infections, and commercially as a growth stimulant for chickens and swine. 

Boric acid, a topical antiinfective agent (fill ear canal with solution and plug with cotton repeat t.i.d. or q.i.d.), is used for the treatment of external ear canal infection. In addition, 5% ointment is used for the relief of abrasions, dry skin, minor bums, insect bites, and other skin irritations. 

Methenamine is an antiinfective agent. In acidic urine, methenamine is hydrolyzed to ammonia and formaldehyde, which is bactericidal to certain bacteria in urine. Acid salts (methenamine mandelate and hippurate) have some nonspecific bacteriostatic activity and help to maintain low nrine pH. It is indicated in suppression or elimination of bacterinria associated with pyelonephritis, cystitis, and other chronic UTls in treatment of infected residual urine, sometimes accompanying nenrologic disease or diabetes. 

Methenamine, a urinary tract antiinfective agent, is used in long-term prophylaxis or snppression of chronic urinary tract infections (methenamine hippnrate), and in the treatment of urinary tract infections associated with neurogenic bladder. 

Nitrofurantoin, a nitrofuran urinary tract antiinfective agent (50 to 100 mg p.o. q.i.d. with meals), is indicated in initial or recurrent urinary tract infections caused by susceptible organisms, or as a long-term suppression therapy. 

Because adrenocorticoids increase the susceptibility to mask symptoms of infection, paramethasone should not be used (except in life-threatening situations) in patients with viral or bacteria infections not controlled by antiinfective agents. 

Rifaximin is an antiinfective agent that inhibits bacterial RNA synthesis. It is indicated in the treatment of traveler s diarrhea by noninvasive strains of Escherichia coli. 

The Microbial Strain Collection and the Microbial Product Library are currently used in our internal process for the discovery of novel antiinfective agents and for the structural manipulation of proprietary lead compounds through our technologies in biotransformation. Our asset in strain isolation, natural product chemistry and manipulation of lead structures together with our capacity in HTS can also be provided to interested partners in joined research programs for the screening/improvements of biocatalysts. 

Vila, J., Sanchez-Cespedes, J., and Giralt, E. (2005) Old and new strategies for the discovery of antibacterial agents. Curr. Med. Chem. Antiinfect. Agents 4, 337-353. 

Clements, J. M., Ayscough, A. P., Keavey, K., and East, S. P. (2002) Peptide deformylase inhibitors, potential for a new class of broad spectrum antibacterials. Curr. Med. Chem. Antiinfect. Agents 1, 239-249. 

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