SjGST (Schistosoma japonicum Glutathione S-transferase), an attractive drug target against schistosomiasis, not only mediates detoxification in xenobiotic process but also implicates in the development of drug resistance. Knowledge of SjGST catalysis toward various substrates will reveal glutathione-dependent metabolism in parasite and disclose the development of new drugs. 5 out of 24 compounds (7、8、16、20 and 23) demonstrate exclusively SjGST-dependent catalysis of detoxification to afford glutathione conjugates (25、26、27、28、29、42 and 43). Metabolic products of glutathione conjugates were prepared through the strategy of enzymatic synthesis in preparative scale and characterized by 1H-, 13C-NMR, COSY, HMQC, HMBC and mass spectroscopy. Compounds 5、6、12、14、15、13 and 21 were able to produce glutathione conjugates (35、36、37、38、39、40 and 41) via chemical reactions. Interestingly，we discovered that the glutathione conjugates derived from chemical reactions displayed significant inhibitory properties toward SjGST. For example, compounds 36 and 39 have a value of IC50 ＜10μM.
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