473403-22-4

Upstream product

• 1073-70-7 4-chlorophenylhydrazine hydrochloride 
• 504-02-9 1,3-cylohexanedione 

Downstream Products

• 329728-74-7 6-chloro-9-(4-fluorobenzyl)-1,2,3,9-tetrahydrocarbazol-4-one 
• 88368-11-0 6-Chloro-1,2,3,9-tetrahydro-4H-carbazol-4-one 

Relevant academic research and scientific papers

Conformationally restrained carbazolone-containing α,γ-diketo acids as inhibitors of HIV integrase

Since α,γ-diketo acid (DKA) compounds were identified as potent and selective inhibitors for HIV integrase, numerous structural modification studies have been carried out to search for a clinical candidate as a supplement for the highly active antiretroviral therapy regimen. Due to the lack of structural information on inhibitor-integrase interactions, a comprehensive structure-activity relationship study is necessary. Most of the reported modification studies on the key α,γ-diketo acid pharmacophore focused on substituting the carboxylate moiety with its bioisosteres or other electron-pair bearing heterocycles. We were interested in studying the conformation and geometry of the central diketo moiety. A series of carbazolone-containing α,γ-diketo acids were designed and synthesized by applying conformational restraint onto the open-chain form of the diketo acid. These compounds showed anti-integrase activity in the low micromolar range, and integrase assay results indicated that the geometry of the diketo acid moiety is crucial to potency. Carbazol-1-one containing DKA analogs (7-8) showed a 2- to 3-fold increase in activity compared with those of carbazol-4-one containing DKA analogs (5 and 6). Alkylation of carbazol-4-one DKA nitrogen (6a-c) led to a loss of activity, suggesting this nitrogen atom may directly interact with the active site of integrase. The halogens (7b-d) and para-fluorobenzyl substituents (8a-d) on carbazol-1-one ring had little effect on potency.

CARBAZOLE DERIVATIVES FOR TREATING POLYCYSTIC KIDNEY DISEASE

Compounds represented by Structural Formula (I): where X is -H, -OR, -SH, -OC(O)R, -OC(O)OR,-OC(O)NRR or -SC(O)OR have anti-cystogenic activity, particularly against polycystic kidney disease. Such compounds can be used in pharmaceutical compounds and in

(1-Substituted-indol-3-yl) alkylidenehydrazinecarboximidamide derivatives as 5-hydroxytryptamine-6 ligands

The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of a disorder relating to or affected by the 5-HT6 receptor.