Pharm Res. 1986 Apr;3(2):75-80. doi: 10.1023/A:1016385118265.
Pharmaceutical research
S Sharma
PMID: 24271464 DOI: 10.1023/A:1016385118265
Structural modifications of diethylcarbamazine (DEC), a drug of choice for treating different forms of human filariasis, are analyzed in order to delineate structure-activity relationships among various piperazine and nonpiperazine DEC analogues. The acyclic congeners of DEC do not possess any activity, probably because of their ability to exist in many conformations. On the other hand, many substituted piperazines display microfilaricidal activity, although they are less potent than DEC. A few rigid analogues of DEC have been found to possess promising antifilarial activity. This survey highlights the therapeutic potential of DEC against filariasis and trends in the design of better filaricidic drugs with DEC as a prototype molecule.