39181-49-2

Upstream product

• 1878-65-5 3-chlorophenylacetic acid 
• 79-19-6 thiosemicarbazide 

Downstream Products

• 1392281-41-2 C₁₅H₁₁ClN₄O₄S₂ 
• 1239310-96-3 tert-butyl cis-4-{5-[5-(3-chlorobenzyl)[1.3.4]thiadiazol-2-ylcarbamoyl]-pyridin-2-yloxy}cyclohexanecarboxylate 

Relevant academic research and scientific papers

Gamma-glutamyl transpeptidase inhibitors and methods of use

Compositions that are effective in inhibiting gamma-glutamyl transpeptidase are disclosed. Methods of producing and using these compositions are also disclosed.

Divergent effects of compounds on the hydrolysis and transpeptidation reactions of γ-glutamyl transpeptidase

A novel class of inhibitors of the enzyme γ-glutamyl transpeptidase (GGT) were evaluated. The analog OU749 was shown previously to be an uncompetitive inhibitor of the GGT transpeptidation reaction. The data in this study show that it is an equally potent uncompetitive inhibitor of the hydrolysis reaction, the primary reaction catalyzed by GGT in vivo. A series of structural analogs of OU749 were evaluated. For many of the analogs, the potency of the inhibition differed between the hydrolysis and transpeptidation reactions, providing insight into the malleability of the active site of the enzyme. Analogs with electron withdrawing groups on the benzosulfonamide ring, accelerated the hydrolysis reaction, but inhibited the transpeptidation reaction by competing with a dipeptide acceptor. Several of the OU749 analogs inhibited the transpeptidation reaction by slow onset kinetics, similar to acivicin. Further development of inhibitors of the GGT hydrolysis reaction is necessary to provide new therapeutic compounds.

THIADIAZOLE DERIVATIVES, INHIBITORS OF STEAROYL-COA DESATURASE

The present invention relates to substituted thiadiazole compounds of the formula (I) and pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds for modulating SCD activity.

2-Amino-5-(substituted or unsubstituted phenylalkyl)-thiadiazoles

2-amino-5-(substituted or unsubstituted phenylalkyl)-thiadiazoles, e.g., 2-amino-5-(4-[phenylbutyl])-thiadiazole, prepared, e.g., by ring closure, of corresponding 1-(substituted or unsubstituted phenylalkanoyl)-thiosemicarbazide in a strong acid medium.