Antileprotics

Also includes antiproto2oan agents and other urinary tract antiinfectives, but does not include the antileprotic sulfones. 

Most analytical work on sulphones has naturally been concerned with the compounds synthesized for special purposes, e.g. sulphonal, trional and tetronal as sedatives and hypnotics Sulphenone (4-chlorodiphenyl sulphone) and Tedion (2,4,4, 5 -tetrachlorodiphenyl sulphone) as acaricides 4,4 -diaminodiphenyl sulphone as an antileprotic. In choosing examples preference has been given to methods devoted to more than a single sulphone. 

Recent studies have been directed towards the synthesis of heterocyclic hydrazones which have lower toxicities than thiosemicarbazones [44], It has been proposed that the hydrazinic N-H group is essential for activity since it might be involved in a crucial radical formation step important in the mechanism of RDR. This is supported by the loss of antileprotic activity for this series of compounds when the hydrazinic hydrogen is replaced by a methyl group [44]. The heterocyclic hydrazones, like thiosemicarbazones, behave as tridentate ligands. 

Acedapsone (127), which is conveniently prepared by acetylation of dapsone, was intended to be a prodrug. Leprous patients being treated with dapsone were observed to have a lower incidence of malaria and acedapsone was made to capitalize on this observation. It, indeed, has both antileprotic and antimalarial activity. 

Dapsone (22 d -diaminodiphenyl sulfone) is an established antileprotic and antiinflammatory drug that is also effective in the therapy of Pneumocystis carinii pneumonia... 

Reverse micelles can also act as a convenient membrane mimetic medium for studying membrane interactions of bioactive peptides [329,330]. Fluorescence behavior of piroxicam in AOT-RMs and Triton X-100 microemulsions was investigated by Andrade and Costa [331].Dutta etal. [332] studied the interactions of an antileprotic drug dapson in dipalmitoyl phosphotidyl choline (DPPC)-RMs in chloroform. The DPPC was found to form RMs just beyond 6 mmol 1" concentration, which is relatively low compared to conventional AOT concentration. 

Other antileprotics include ethionamide and pro-thionamide. Thalidomide (see Index), despite its notorious past, still finds a use with corticosteroid in the control of allergic lepromatous reactions. 

It may also have ANTIPSYCHOTIC activity, dapiprazole hydrochloride dapiprazole. dapitant [inn] (RPR 100893) is a substituted isoindole, a TACHYKININ RECEPTOR ANTAGONIST, selective for the NK,-receptor subtype. It has potential as an ANTIMIGRAINE AGENT, dapsone [ban, inn, usan] is a sulphone with actions similar to SULPHONAMIDES and with ANTIBACTERIAL activity. It can be used as an antileprotic and for infective dermatitis herpetiformis. and is being investigated for the treatment and prevention of Pneumocystis carinii pneumonia (e.g. in AIDS), daptomycin [ban, inn, usan] is an (aminoglycoside) antibiotic. It has antibacterial properties. 

Spanish Fly cantharides. spantide I [DArg, oTrp -, Leu ] Pl-ll. sparfloxacin [ban. inn. usan] fluoroquinolone, is a broad-spectrum ANTIBACTERIAL which can be used as an ANTILEPROTIC and ANTITUBERCULAR AGENT. 

Sulfones are chemically related to sulphonamides, and are presumed to work by a similar mechanism. The only one still in clinical used is dapsone and this is used in combination with other drugs to treat leprosy. See antileprotic AGENTS. 

Mahato, S.B. Sahu, N.P. An improved process for the isolation of asiaticoside, useful as an antileprotic agent from Centella asiatica, Indian patent filed, 1993. 

Clofazimine is active against Mycobacterium leprae and is used clinically to treat leprosy (Hansen s disease). It was s)mthesised in 1957 by Barry et al.. Laboratories of the Medical Research Council of Ireland, Trinity College Dublin. The precise mechanism of the antileprotic action of clofazimine has not been established. The World Health Organisation classify clofazimine as an "essential drug" and recommend its use, in combination, with other agents to treat all cases of leprosy (WHO, 1982). 

Although the precise mechanism of the antileprotic activity of clofazimine has yet to be determined several explanations have been proposed (Hooper 1987). 

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