22746-83-4

Upstream product

• 79-37-8 oxalyl dichloride 
• 620-86-0 4-Benzylbenzoic acid 
• 611-95-0 4-carboxybenzophenone 
• 134-84-9 4-Methylbenzophenone 

Downstream Products

• 95622-37-0 4'-benzyl-2,3,5,6-tetramethyl-benzophenone 
• 92199-30-9 4-benzyl-benzamide 
• 151807-09-9 4-tolyl p-benzylbenzoate 
• 83038-71-5 4-benzylbenzoic acid cholesteryl ester 
• 151807-07-7 4-chlorophenyl p-benzylbenzoate 
• 15866-31-6 phenyl(p-vinylphenyl)methane 
• 262425-95-6 1-[(1E)-3-chloro-1-propenyl]-4-(phenylmethyl)benzene 
• 262425-93-4 methyl (2E)-3-[4-(phenylmethyl)phenyl]-2-propenoate 
• 193819-67-9 3-(4-benzyl-phenyl)-propionic acid methyl ester 
• 1026893-20-8 3-(4-benzyl-phenyl)-2,2-dichloro-cyclobutanone 
• 262425-94-5 1-[1-oxo-3-[4-(phenylmethyl)phenyl]propyl]pyrrolidine 
• 89094-64-4 norethisterone 4-benzylbenzoate 

Relevant academic research and scientific papers

Synthesis and evaluation of effective inhibitors of plant δ1-pyrroline-5-carboxylate reductase

Analogues of previously studied phenyl-substituted aminomethylene- bisphosphonic acids were synthesized and evaluated as inhibitors of Arabidopsis thaliana δ1-pyrroline-5-carboxylate reductase. With the aim of improving their effectiveness, two main modifications were introduced into the inhibitory scaffold: the aminomethylenebisphosphonic moiety was replaced with a hydroxymethylenebisphosphonic group, and the length of the molecule was increased by replacing the methylene linker with an ethylidene chain. In addition, chlorine atoms in the phenyl ring were replaced with various other substituents. Most of the studied derivatives showed activity in the micromolar to millimolar range, with two of them being more effective than the lead compound, with concentrations inhibiting 50% of enzyme activity as low as 50 μM. Experimental evidence supporting the ability of these inhibitors to interfere with proline synthesis in vivo is also shown.

3-Mercapto-1,2,4-triazoles and N-acylated thiosemicarbazides as metallo-β-lactamase inhibitors

The production of β-lactamases is an effective strategy by which pathogenic bacteria can develop resistance against β-lactam antibiotics. While inhibitors of serine-β-lactamases are widely used in combination therapy with β-lactam antibiotics, there are no clinically available inhibitors of metallo-β-lactamases (MBLs), and so there is a need for the development of such inhibitors. This work describes the optimisation of a lead inhibitor previously identified by fragment screening of a compound library. We also report that thiosemicarbazide intermediates in the syntheses of these compounds are also moderately potent inhibitors of the IMP-1 MBL from Pseudomonas aeruginosa. The interactions of these inhibitors with the active site of IMP-1 were examined using in silico methods.

NEW COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES

This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. The compounds have the formula (A1) wherein R1, R2, R4, R6, E, n, Y1, Y2, Y3, Y4, Y5, L, B, R8, and m are as defined in the claims.

NOVEL MCHR1 ANTAGONISTS AND THEIR USE FOR THE TREATMENT OF MCHR1 MEDIATED CONDITIONS AND DISORDERS

Compounds of formula (I) wherein R1 , D, R2 , A and R3 are as described in the specification, pharmaceutically- acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.

Structure-activity relationship studies on 1-[2-(4- phenylphenoxy)ethyl]pyrrolidine (SC-22716), a potent inhibitor of leukotriene A4 (LTA4) hydrolase

Leukotriene B4 (LTB4) is a pro-inflammatory mediator that has been implicated in the pathogenesis of a number of diseases including inflammatory bowel disease (IBD) and psoriasis. Since the action of LTA4 hydrolase is the rate-limiting step for LTB4 production, this enzyme represents an attractive pharmacological target for the suppression of LTB4 production. From an in- house screening program, SC-22716 (1, 1-[2-(4- phenylphenoxy)ethyl]pyrrolidine) was identified as a potent inhibitor of LTA4 hydrolase. Structure-activity relationship (SAR) studies around this structural class resulted in the identification of a number of novel, potent inhibitors of LTA4 hydrolase, several of which demonstrated good oral activity in a mouse ex vivo whole blood assay.

Intramolecular nucleophilic participation : A comparative study of the nucleophilic participating capacity of several new ortho substituents in benzhydryl bromide solvolysis

Rate studies for the solvolysis of several new ortho- and para-substituted benzhydryl bromides in 80percent aq. acetone have been conduced at two different temperatures.The carbophenoxy, 4-nitrocarbophenoxy, 4-chlorocarbophenoxy and 4-methylcarbophenoxy groups present at the ortho-position in benzhydryl bromide solvolyse faster than those present at the para-position.The results are further supported by the activation parameters evaluated for these compounds.A discussion of the various solvolysis mechanisms is presented in which it is proposed that the observed rate effects of these similarly constituted but electronically different substituents result from the variation in the nucleophilic capacity of these groups.

LONG-ACTING CONTRACEPTIVE AGENTS: NORETHISTERONE ESTERS OF ARYLCARBOXYLIC ACIDS

The synthesis of esters of norethisterone (17α-ethynyl-17β-hydroxyestr-4-en-3-one) with acids containing a benzene ring is described, two methods of esterification being compared in terms of yield and convenience.The activities of these esters as long-acting contraceptive agents have been evaluated.

INFLUENCE OF THE ANGULAR LINKAGE ON THE MESOMORPHIC PROPERTIES OF CHOLESTERYL ARYLBENZOATES.

Some cholesteryl esters of arylbenzoic acids incorporating angular linkage such as -Co-, -O-, -S-, and -CH//2-, were prepared, and the transition temperatures and heats determined. The cholesteric-isotropic transition temperatures are likely to correlate with the angular correlation parameters of these carboxylic acid moieties. The mesomorphic phenomena are discussed in terms of the molecular structure and electronic effect of these linkages.