Prophylactic activity

Though dental afflictions constitute a very significant disease entity, these have received relatively little attention from medicinal chemists. (The fluoride toothpastes may form an important exception.) This therapeutic target Is, however, sufficiently Important to be the focus of at least some research. A highly functionalized piperazine derivative that has come out of such work shows prophylactic activity against dental caries. Condensation of the enol ether 1 of thiourea with ji-pentylisocyanate gives the addition product 1J. Reaction of this with diamine 78, derived from piperazine, leads to substitution of the methylthio moiety by the primary amine, in all likelihood by an addition-elimination sequence. There is thus obtained ipexidine (79). ... 

Bosshardt, S.C., McCall, J.W., Coleman, S.H., Jones, KL., Petit, T.A. and Klei, T.L. (1993) Prophylactic activity of tetracycline against Brugia pahangi infection in Jirds (Meriones unguiculatus). Journal of Parasitology 79, 775-777. 

I he discovery that some retinoids posess prophylactic activity against carcinogenesis in epithelial tissueshas reawakened... 

The antiepileptic agent carbamazepine (Tegretol1 1) has been discussed for many years as an alternative to lithium because it also has an antimanic effect and prophylactic activity against depression, with possibly better tolerability. However, carbamazepine has not yet been proven to be superior to lithium,... 

A milk product is described having prophylactic activity due to cultured-milk strains of microorganisms. It includes several lactic acid bacteria (e.g., Lactobacillus acidophilus strain 317/402), and inulin from Jerusalem artichoke. 

Shapiro TA, Ranasinha CD, Kumar N, Barditch-Crovo P. Prophylactic activity of atovaquone against Plasmodium falciparum in humans. Am J Trop Med Hyg 1999 60(5) 831-6. 

Curd, F. H. S., Davey, D. G., Rose, F. L. Studies on synthetic antima-larial drugs-X. Some biguanide derivatives as new types of antimalar-ial substances with both therapeutic and causal prophylactic activity. Ann. Trap. Med. 1945, 39, 208-214. 

Following the observation made by Chinese scientists that nitrofurazone (1) possesses prophylactic activity against S. japonicum in albino rats [10,11], a large number of nitrofurans were synthesized as potential schistosomicidal agents, of... 

Although a number of these sulphones (15-24) exhibit curative and/or prophylactic activities against experimental malaria and experimental mycobacterial infections, none offered any distinct advantage over DDS. Even after over 50 years of its use in clinical practice DDS or its repository forms, DFDDS (15) and DADDS (16) are the main sulphones in clinical use. The therapeutic effects of DFDDS and DADDS have been attributed to their metabolic conversion in to DDS [34,35]. 

The fact that naphthoquinones are potent inhibitors of respiration in parasitized RBCs, characterised by an abnormal content of coenzyme Q (ubiquinone, 18) [16], a variety of heterocyclic quinones have been tested for their antimalarial activity [19-26]. Of these compounds 19-21 exhibited promising prophylactic activity. At a dose of 10 mg/kg given subcutaneously, 20 gave complete protection to ducks against sporozoite-induced P. gallinaceum infection [27], while 21 suppressed para-sitaemia in monkeys infected with P. cynomolgi at an intravenous dose of 3.16 mg/kg [8]. 

Direct electrophilic, Lewis acid-catalyzed C-ribosylation of pyrrolo [2,3-d]pyrimidin-4-ones with 317 gave pyrrolo[2,3-d]pyrimidin-7-yl C-nucleosides 318. The latter were halogenated at C6 and de-O-benzoylated to 319, which showed good prophylactic activity against the lethal Semliki Forest virus infection in mice (90JMC2750) (Scheme 97). 

Its effectiveness, however, seems to be less than that of the tetracyclines. Kimura proved di-(hydroxymethyl) panfuran to be effective in vivo against Strep, pyogenes infections as the following Table 6.26 shows. The three tested compounds exhibit the same prophylactic activity. 

Prophylactically active agaiust a wide range of viruses, including those causing canine distemper, lymphomatosis in fowl, shipping fever in cattle, transmissible gastroenteritis iu swine, and coryza and other upper respiratory illnesses, as well as against ECHO viruses, enteroviruses in monkeys, MM neurotropic virus, Semliki Forest virus, and NEF 1 poliomyelitis virus. Antitumor activity demonstrated in experimental leukemia and sarcoma. 

Boraadamantane (5) is used as a starting compound in the most effective synthesis of 1-azaadamantane (Section 8.34.5.5.3). Several complexes of 1-boraadamantane (5) reveal significant therapeutic and prophylactic activity against influenza <79Mi 834-01 >. 

Once-weekly administration of this antibiotic has prophylactic activity against bacteremia due to M avium complex in AIDS patients. 

A large number of diphenylsulfone analogues have been developed for the treatment of leprosy. Incidentlly one such member chemically known as 4,4 -diaminodiphenyl sulfone (dapsone) exhibited prophylactic activity against resistant/ falciparum. Dapsone in conjimction with pyrimethamine has been effectively used in the treatment of malaria due to chloroquine resistant P. falciparum. 

Picumast dihydrochloride (PDH), (3,4-dimethyl-7-[4-chlorobenzyl) piperazine-l-yl]propoxycoumarin dihydrochloride) is a prophylactically active anti-allergic compound, which combines inhibition of mediator... 

Another cytosine derivative with antiviral activity is the 5-(4-aminophenyl) cytosine (LVII). This substance, according to results of clinical trials, possesses good prophylactic activity against influenza A2 [343]. The LD50... 

Tests in man are, of course, the pinnacle of antimalarial evaluation procedures, and the factors governing such tests are similar to any organised clinical trial [23]. However, the search continues for a perfect animal model of hiunan malarias, and the similarity between human and simian malarias has prompted a number of investigations of their interrelationships. P. cynomolgi has long been used as a secondary screen for prophylactic activity to test drugs which showed activity in the primary screens [23], since the course and therapeutic response of this infection are directly parallel to those of human vivax malaria. Moreover, human infections with the simian... 

Wine, phenoHc constHuents of. Besides the volatile constituents of wine flavor, alcohols, tartaric acid and tartrates, especially red wines contain phenolic constituents stilbenes, e.g. resveratrol, the vitisins, tannins and other polyphenols like ellagic acid and the viniferins, and other oligomeric stilbenes, e.g. e-viniferin. Mainly to these phenolic compounds, the anti-atherosclerotic and infarction-prophylactic activity is attributed, explaining the so-called French Para-... 

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