68114-93-2

Upstream product

• 103-29-7 1,1'-(1,2-ethanediyl)bisbenzene 
• 79-04-9 chloroacetyl chloride 

Downstream Products

• 103096-77-1 4,4'-bis-iodoacetyl-bibenzyl 
• 397872-17-2 1,2-bis(4-(2-chloroethyl)phenyl)ethane 
• 793-06-6 4,4'-diacetylbibenzyl 
• 89302-45-4 2,2'-(1,2-ethanediyldi-1,4-phenylene)bis<2-hydroxy-4,4-dimethylmorpholinium> dichloride 
• 855940-60-2 4,4'-bis-acetoxyacetyl-bibenzyl 

Relevant academic research and scientific papers

Design, synthesis, and biological evaluation of a new series of biphenyl/bibenzyl derivatives functioning as dual inhibitors of acetylcholinesterase and butyrylcholinesterase

Alzheimer's disease (AD), the most common form of dementia in adults, is a progressive neurodegenerative disorder of the brain characterized by loss of memory and steady deterioration of cognition. Here, a series of symmetrical molecules containing biphenyl/bibenzyl scaffolds (12-36) were designed, synthesized, and evaluated for their ability to inhibit both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). A biological evaluation showed that most of these biphenyl derivatives were potent AChE and BuChE inhibitors. Among them, compound 15 displayed the greatest ability to inhibit BuChE (IC50 = 0.74 μM) and was also a good AChE inhibitor (IC50 = 1.18 μM). Compound 19 was not only a potent AChE inhibitor (IC50 = 0.096 μM), but also a mild BuChE inhibitor (IC50 =1.25 μM). Overall, these results suggested that compound 19 may be a promising agent in the treatment of AD.

The b, butyrylcholinesterase with double-inhibiting active compound

The invention provides an inhibitor of acetylcholine esterase and cholinesterase shown in the general formula (I), wherein R1, R2 and N form an aliphatic heterocyclic ring with 3-7 carbons containing 1-2 hetero atoms, and X is selected from a covalent bon

HEPATITIS C VIRUS INHIBITORS

This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds

Synthesis and structure-activity analysis of new phosphonium salts with potent activity against African trypanosomes

A series of 73 bisphosphonium salts and 10 monophosphonium salt derivatives were synthesized and tested in vitro against several wild type and resistant lines of Trypanosoma brucei (T. b. rhodesiense STIB900, T. b. brucei strain 427, TbAT1-KO, and TbB48). More than half of the compounds tested showed a submicromolar EC50 against these parasites. The compounds did not display any cross-resistance to existing diamidine therapies, such as pentamidine. In most cases, the compounds displayed a good selectivity index versus human cell lines. None of the known T. b. brucei drug transporters were required for trypanocidal activity, although some of the bisphosphonium compounds inhibited the low affinity pentamidine transporter. It was found that phosphonium drugs act slowly to clear a trypanosome population but that only a short exposure time is needed for irreversible damage to the cells. A comparative molecular field analysis model (CoMFA) was generated to gain insights into the SAR of this class of compounds, identifying key features for trypanocidal activity.

HEPATITIS C VIRUS INHIBITORS

This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.

Synthesis and Conformational Properties of Paracyclo(2,5)thiophenoparacyclophanes

Cyclic diketo sulfides 4 (n=3-8, 10) were condensed with glyoxal to give thiophenophanediones 6.The NMR, IR and UV spectral data of 6 are consistent with the following picture.The thiophene-2,5-dicarbonyl moiety in 6 (n=10) is in the mean molecular plane