Antibacterial antiprotozoal

Diaryl oxindoles are known to exhibit a wide range of biological activities such as antibacterial, antiprotozoal, and anti-inflammatory behavior [61-63]. Generally,... 

The antibacterial, antiprotozoal and anthelminthic members of this group are described in the appropriate sections. Antifungal azoles comprise the following ... 

Dlhydrofplate Reductase Inhibitors - This enzyme (DHFF) reduces dlhydrofollc acid (] ) to tetrahydrofollc acid - an essential cofactor with important roles In DNA synthesis and cell growth. DHFR can be widely different In structure in different cells, and Inhibitors which exploit these differences Include clinically useful antibacterial, antiprotozoal, Immunosuppressant and antlneoplastlc drugs. A vast amount of synthetic analog work in this field has been done, much of it by Baker.68 Hansch and co-workers used data from several groups and QSAR techniques to "map" receptor space for DHFR from rat liver, from... 

It has been known for many years that the onset of inflammatory diseases may follow or occur along with a variety of infections. As a result, it is of interest that copper complexes have antiviral, antibacterial, antiprotozoal, anthelmintic, antifungal, antialgal and antimycoplasmal activities. 

Nifuratel. Nihiratel, 5-[(methylthio)methyl]-3-[5-nitro-2-furanyl)-methyleneamino]-2-oxazohdinone, is prepared by treatment of the appropriate methyl-thiohydrazinopropanol with diethylcarbonated followed by condensation with 5-nitro-2-furancarboxaldehyde diacetate (44). The product has been used in antibacterial, antifungal, and antiprotozoal appHcations. 

Nystatin (100,000 lU) is also available in combination with neomycin sulfate [1405-10-3] (35,000 lU), polymyxin B sulfate [1405-20-5] (35,000 lU), acetarsol [97-44-9] (150 mg), and dimethicone [8050-81-5] (2,500 mg). One or two ovules per day are inserted vaginaHy for at least 6—12 days. This combination has an antibacterial, antimycotic, and antitrichomonas action (see also Antibiotics, oligosaccharides Antiparasitic agents, antiprotozoals). 

Keywords Antibacterial activity Antimycotic activity Antiprotozoal activity Antiviral activity Cathechins Proanthocyanidins... 

The occurrence in some plants of secondary metabolites characterized by an 0-heterocyclic structure and exhibiting antimicrobial properties is a well-known phenomenon [2,8-10]. Among them, catechins and proanthocyanidins are two classes of compounds exhibiting antimicrobial properties towards both prokaryotic and eukaryotic microorganisms. Yet, despite the large number of studies published so far, the real potentialities and limitations given by the use of this class of molecules as antiviral or antimicrobial (antibacterial, antimycotic, antiprotozoal) agents have not been critically evaluated. The present chapter represents an overview of the re-... 

While nitrofurans are often prepared as antibacterial agents, nitroimidazole forms the basis for an extensive class of agents used in the treatment of infections by the protozoans. Unlike bacterial infections, protozoal infections are seldom life-threatening. The physical discomfort occasioned by such infections is, however, of sufficient importance to provide a useful therapeutic place for antiprotozoal agents. A particularly common set of such conditions are parasitic infections of the genitalia caused by Trichomonas vaginalis. These disorders are called trichomoniasis. 

As noted above, nitrofurans and nitroimidazoles have proven useful moieties for the preparation of antibacterial and antiprotozoal agents. It is thus of note that nitrothiazoles have also been used successfully in the preparation of antiparasitic agents. Condensation of 6-nitro-2-aminothiazole (194, available from nitration of aminothiazole) with ethylisocyanate yields the antiprotozoal agent... 

Mecfianism of Action An anti-infective that interferes with nuclear metabolism and incorporation of nucleotides, inhibiting DNA, RNA, phospholipid, and protein synthesis, THerapeutic Effect Produces antibacterial and ID-antiprotozoal effects, Pfiarmacokinetics Well absorbed after IM administration minimally absorbed after inhalation. Widely distributed. Primarily excreted in urine. Minimally removed by hemodialysis, Half-life 6,5 hr (increased in impaired renal function). 

Iridoids have shown a broad range of biological activities, such as an antibacterial, antifungal, anti-inflammatory, antitumoral, hepatoprotective, cardioprotective, antioxidative, antiprotozoal and anti-insect properties [13,14,15,16,17,18,19]. In vitro activities inhibiting the hepatitis C virus, the differentiation of the adipocyte, and PPARa activation activities have been also described [20, 21]. 

Metronidazole is a nitroimidazole antiprotozoal drug (see Chapter 52) that also has potent antibacterial activity against anaerobes, including bacteroides and Clostridium species. It is well absorbed after oral administration, is widely distributed in tissues, and reaches serum levels of 4-6 mcg/mL after a 250-mg oral dose. Metronidazole can also be given intravenously or by rectal suppository. The drug penetrates well into the cerebrospinal fluid and brain, reaching levels similar to those in serum. Metronidazole is metabolized in the liver and may accumulate in hepatic insufficiency. 

Coptis chinensis Franch. C. japonica Makino C. teeta Wall. Huang Lian (Gold thread) (root) Berberine, coptisine, urbenine, worenine, palmatine, jatrorrhizine, columbamine, lumicaerulic acid33 60.248.510 This herb is toxic. Antiarrhythmic, antibacterial, antiviral, antiprotozoal, anticerebral ischemic. 

N.A. Acoric acid, asarone, linalool, palmitic acid, methylamine, saponin, mucilage, sesquiterpenes.99 100 103 105 Used as a panacea. It is antibacterial, antifungal, antiseptic, antiamebic, antiprotozoal, a vermifuge. Treat digestive upset, fevers. 

Mayer, A. M. S., Rodriguez, A. D., Berlinck, R. G. S., and Hamann, M. T. (2009). Marine pharmacology in 2005-6 Marine compounds with anthelmintic, antibacterial, anticoagulant, antifungal, antiinflammatory, antimalarial, antiprotozoal, antituberculosis, and antiviral activities affecting the cardiovascular, immune and nervous systems, and other miscellaneous mechanisms of action. Biochim. Biophys. Acta 5, 283-308. 

Tire major anticoccidial and other antiprotozoal drugs have no common chemical structure and therefore no group tests can be used to screen for residues in animal-derived foods. This is in complete contrast to the antibacterials previously discussed, which can be detected, although not identified, on the basis of their biological activity. 

Some drugs, including sulfaquinoxaline, sulfadimethoxine, sulfame-thoxypyridazine, sulfachlorpyrazine, sulfamethazine, sulfaguanidine, furazolidone, nitrofurazone, tetracycline, and chlortetracycline, in addition to their role as coccidiostats, are also used as antibacterials. These drugs will not be discussed in this chapter since they have been discussed previously. On the other hand, other compounds such as roxarsone, are classified as growth promoters and therefore will be described in the corresponding chapter. This chapter is limited to compounds whose primary function and use are as antiprotozoals. 

Infestations with parasitic worms and flukes are widespread both in humans and in animals, and their treatment requires drugs that act in a different manner from antibacterial and antiprotozoal agents. It is desirable for worms to be expelled from the body intact since the presence of dead worms in the tissues can provoke severe reactions. Such reactions are seen when filarial worms which circulate in the blood and lymph are killed by diethylcar-bamazine (264). Intestinal worms may be expelled when they are paralyzed by neuromuscular blockers such as piperazine citrate or pyrantel (265), or their metabolism may be disrupted by the anthelmintic drugs tetramisole and thiabendazole (266) which inhibit fumarate reductase, or mebendazole (267) which prevents glucose uptake by the worms. The anthelmintic activity of tetramisole is due to its laevo isomer levamisole (186). The dextro isomer has antidepressant activity. 

A variety of biological activities have been associated with labdane diterpenes including antibacterial, antifungal, antiprotozoal, enzyme induction, anti-inflammatory modulation of immune cell functions, as well as cytotoxic and cytostatic effects against human leukemic cell lines. 

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