177559-01-2

Upstream product

• 1121-25-1 2-methyl-3-pyridinol 
• 100-39-0 benzyl bromide 

Downstream Products

• 177557-27-6 2-(8-Benzyloxy-3-cyclopentylmethyl-2-ethylindolizin-1-yl)glyoxylamide 
• 182115-78-2 2-(8-benzyloxy-3-cyclopentylmethyl-2-cyclopropyl-8-hydroxylndolizin-1-yl)glyoxylamide 
• 1026304-81-3 (8-Benzyloxy-3-cyclopentylmethyl-2-cyclopropyl-indolizin-1-yl)-oxo-acetyl chloride 
• 1027484-82-7 (8-Benzyloxy-3-cyclopentylmethyl-2-ethyl-indolizin-1-yl)-oxo-acetyl chloride 
• 177557-48-1 2-(8-(Carbomethoxymethyloxy)-3-cyclohexylmethyl-2-ethylindolizin-1-yl)glyoxylamide 
• 177557-35-6 2-(8-benzyloxy-2-ethyl-3-(thiophen-2-yl methyl)indolizin-1-yl)glyoxylamide 
• 1028285-67-7 (8-Benzyloxy-2-ethyl-3-pentyl-indolizin-1-yl)-oxo-acetyl chloride 
• 177557-29-8 2-(8-Benzyloxy-2-ethyl-3-pentyl-indolizin-1-yl)-2-oxo-acetamide 
• 177557-33-4 2-(8-Benzyloxy-2-ethyl-3-(2-phenylethyl)indolizin-1-yl)glyoxylamide 
• 1026458-32-1 (8-Benzyloxy-2-ethyl-3-phenethyl-indolizin-1-yl)-oxo-acetyl chloride 
• 177557-42-5 2-(3-Benzyl-8-benzyloxy-2-cyclopropylindolizin-1-yl)-glyoxylamide 
• 1026198-63-9 (3-Benzyl-8-benzyloxy-2-cyclopropyl-indolizin-1-yl)-oxo-acetyl chloride 
• 1027538-62-0 (8-Benzyloxy-3-cyclopentylmethyl-2-methyl-indolizin-1-yl)-oxo-acetyl chloride 
• 177557-46-9 2-(8-Benzyloxy-3-cyclopentylmethyl-2-methyl-indolizin-1-yl)-2-oxo-acetamide 

Relevant academic research and scientific papers

Manganese-Based Contrast Agents for Magnetic Resonance Imaging of Liver Tumors: Structure-Activity Relationships and Lead Candidate Evaluation

Gd-based MRI contrast agents (GBCAs) have come under intense regulatory scrutiny due to concerns of Gd retention and delayed toxicity. Three GBCAs comprising acyclic Gd chelates, the class of GBCA most prone to Gd release, are no longer marketed in Europe

Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2

We report a series of inhibitors of secreted phospholipases A2 (sPLA2s) based on substituted indoles, 6,7-benzoindoles, and indolizines derived from LY315920, a well-known indole-based sPLA2 inhibitor. Using the human group X sPLA2 crystal structure, we prepared a highly potent and selective indole-based inhibitor of this enzyme. Also, we report human and mouse group IIA and IIE specific inhibitors and a substituted 6,7-benzoindole that inhibits nearly all human and mouse sPLA 2s in the low nanomolar range.

Acid-catalyzed rearrangement of 1-benzyl-2-methyl-3-piperidone to 1-benzyl-2-acetylpyrrolidine

We report that 1-benzyl-2-methyl-3-piperidone, conveniently prepared from 3-hydroxy-2-methylpyridine, undergoes rearrangement to 1-benzyl-2-acetylpyrrolidine in aqueous 6 N HCl at reflux. Studies showing that the 2,2-dimethyl analog is inert under the same conditions support a mechanism of reversible tautomeric equilibria via ring-opened intermediates, one of which was independently synthesized and shown to be a kinetically competent intermediate to product.

A platform for designing HIV integrase inhibitors. Part 1: 2-Hydroxy-3-heteroaryl acrylic acid derivatives as novel HIV integrase inhibitor and modeling of hydrophilic and hydrophobic pharmacophores

We present a novel series of HIV integrase inhibitors, showing IC50s ranging from 0.01 to over 370 μM in an enzymatic assay. Furthermore, pharmacophore modeling study for the inhibitors was carried out to elucidate the structure-activity relationships. Finally, we found a 3D-pharmacophore model, which is composed of a hydrophilic and a hydrophobic domain, providing valuable information for designing other novel types of integrase inhibitors.

Indolizine SPLA2inhibitors

A class of novel indolizine-1-functional compounds and indolizine-3-functional compounds is disclosed together with the use of such indolizine compounds for inhibiting sPLA2mediated release of fatty acids for treatment of conditions such as septic shock. The compounds are indolizine-1-acetamides, indolizine-1-acetic acid hydrazides, indolizine-1-glyoxylamides, indolizine-3-acetamides, indolizine-3-acetic acid hydraxides, and indolizine-3-glyoxylasides.

Potent inhibitors of secretory phospholipase A2: Synthesis and inhibitory activities of indolizine and indene derivatives

Phospholipase A2 is an enzyme which hydrolyzes the sn-2 position of certain cellular phospholipids. The liberated lysophospholipid and arachidonic acid are precursors in the biosynthesis of various biologically active products. As human nonpancreatic sPLA2 is present in high levels in the blood of patients in several pathological conditions, the potent sPLA2 inhibitors have been suggested to be useful drugs. Here we describe the synthesis, structure-activity relationship, and inhibitory activities of indolizine and indene derivatives. 1-(Carbamoylmethyl)indolizine derivatives and 1-oxamoylindolizine derivatives exhibited very potent inhibitory activity. The former was unstable to air oxidation, but the latter exhibited an improvement both in stability and in potency. Some compounds approached the stoichiometric limit of the chromogenic assay.