58599-05-6

Upstream product

• 175838-22-9 (Z)-N',3-dihydroxybenzimidamide 
• 108-24-7 acetic anhydride 
• 873-62-1 m-cyanophenol 
• 175838-22-9 N',3-dihydroxybenzimidamide 
• 75-36-5 acetyl chloride 
• 1072880-70-6 3-[3-(2-methoxyethoxymethoxy)-phenyl]-5-methyl-1,2,4-oxadiazole 
• 1363593-63-8 3-[N'-(acetyloxy)carbamimidoyl]phenyl acetate 
• 1072880-69-3 N-acetoxy-3-(2-methoxy-ethoxymethoxy)-benzamidine 
• 1072880-68-2 N-hydroxy-3-(2-methoxy-ethoxymethoxy)-benzamidine 
• 303223-96-3 3-(2-methoxyethoxymethoxy)-benzonitrile 

Downstream Products

• 873925-60-1 diisopropyl-{2,3,5-trifluoro-6-[3-(5-methyl-[1,2,4]oxadiazol-3-yl)-phenoxy]-pyridin-4-yl}-amine 
• 443999-27-7 ethyl 2-[3-(5-methyl-1,2,4-oxadiazol-3-yl)-phenoxy]pentanoate 
• 362045-30-5 methyl [3-(5-methyl-1,2,4-oxadiazol-3-yl)phenoxy]-2-phenylacetate 
• 444615-40-1 ethyl [2-methyl-4-({[4-{[3-(5-methyl-1,2,4-oxadiazol-3-yl)phenoxy]methyl}-2-(4-{trifluoromethyl}phenyl)-1,3-thiazol-5-yl]methyl}sulfanyl)phenoxy]acetate 
• 1072880-71-7 3-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl cyclohexylcarbamate 
• 1363593-66-1 8-[3-(5-methyl-1,2,4-oxadiazol-3-yl)phenoxy]-3,4-dihydro-2H-5,1,2-benzoxathiazepine 1,1-dioxide 
• 1363593-73-0 tert-butyl 8-[3-(5-methyl-1,2,4-oxadiazol-3-yl)phenoxy]-3,4-dihydro-2H-5,1,2-benzoxathiazepine-2-carboxylate 1,1-dioxide 

Relevant academic research and scientific papers

Dihydrobenzoxathiazepine compounds, a process for their preparation and pharmaceutical compositions containing them

Compounds of formula (I): wherein R1 represents a hydrogen atom or a heterocyclic, cyano, alkoxycarbonyl, alkylsulphonylaminoalkyl or N-hydroxycarboximidamide group. Medicinal products containing the same which are useful as modulators of the A

3-Heterocycle-phenyl N-alkylcarbamates as FAAH inhibitors: Design, synthesis and 3D-QSAR studies

Carbamates are a well-established class of fatty acid amide hydrolase (FAAH) inhibitors. Here we describe the synthesis of meta-substituted phenolic N-alkyl/aryl carbamates and their in vitro FAAH inhibitory activities. The most potent compound, 3-(oxazol-2yl)phenyl cyclohexylcarbamate (2a), inhibited FAAH with a sub-nanomolar IC50 value (IC50=0.74 nM). Additionally, we developed and validated three-dimensional quantitative structure-activity relationships (QSAR) models of FAAH inhibition combining the newly disclosed carbamates with our previously published inhibitors to give a total set of 99 compounds. Prior to 3D-QSAR modeling, the degree of correlation between FAAH inhibition and in silico reactivity was also established. Both 3D-QSAR methods used, CoMSIA and GRID/GOLPE, produced statistically significant models with coefficient of correlation for external prediction (R2 PRED) values of 0.732 and 0.760, respectively. These models could be of high value in further FAAH inhibitor design.

HETEROCYCLIC PHENYL CARBAMATES AS NOVEL FAAH-INHIBITORS

Fatty acid amide hydrolase inhibitors of the Formula (I) are provided, wherein R is a heterocyclic or heterocyclic carbonyl moiety and R' is a group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted

Compounds enhancing antitumor activity of other cytotoxic agents

This invention relates to certain heterocyclic compounds and their pharmaceutically acceptable salts, which are useful for sensitizing multidrug-resistant tumor cells to anticancer agents and multidrug resistant forms of malaria, tuberculosis, leishmania and amoebic dysentery to chemotherapeutants. The compounds and their pharmaceutically acceptable salts are also inhibitors of the active drug transport capability of P-glycoprotein which is encoded by the human MDR1 gene, as well as of certain other related ATP-binding-cassette transporters from eukaryotic and prokaryotic organisms (e.g., pfmdr from Plasmodium falciprum, and murine mdr1 and mdr3 gene products).