159017-85-3

Upstream product

• 100-83-4 meta-hydroxybenzaldehyde 
• 100-52-7 benzaldehyde 
• 27492-46-2 4,5-dimethyl-2-phenyl-oxazole 3-oxide 
• 103788-61-0 (5-methyl-2-phenyl-4-oxazolyl)methyl chloride 

Downstream Products

• 1026692-74-9 4-(3-ethynyl-phenoxymethyl)-5-methyl-2-phenyl-oxazole 
• 174258-08-3 3-(5-Methyl-2-phenyl-oxazol-4-ylmethoxy)-benzaldehyde oxime 
• 166253-56-1 ethyl (E)-3-(5-methyl-2-phenyl-4-oxazolylmethoxy)cinnamate 
• 174258-31-2 [3-[(5-methyl-2-phenyl-4-oxazolyl)methoxy]phenyl]methanol 
• 159017-97-7 4-(5-methyl-2-phenyl-4-oxazolylmethoxy)-acetophenone 
• 1027047-41-1 C₃₁H₃₆N₂O₇ 
• 1026197-45-4 N-{1-methyl-3-[3-(5-methyl-2-phenyl-oxazol-4-ylmethoxy)-phenyl]-prop-2-ynyl}-hydroxylamine 
• 1026651-91-1 4-[3-(5-methyl-2-phenyl-oxazol-4-ylmethoxy)-phenyl]-but-3-yn-2-ol 
• 174258-09-4 N-[3-(5-methyl-2-phenyl-oxazol-4-ylmethoxy)-benzyl]-hydroxylamine 
• 166254-15-5 5-[4-[3-(5-methyl-2-phenyl-4-oxazolylmethoxy)phenyl]-1,3-butadien-1-yl]tetrazole 
• 166253-59-4 (2E,4E)-5-[3-(5-Methyl-2-phenyl-oxazol-4-ylmethoxy)-phenyl]-penta-2,4-dienenitrile 
• 166253-57-2 (E)-3-[3-(5-Methyl-2-phenyl-oxazol-4-ylmethoxy)-phenyl]-prop-2-en-1-ol 
• 166253-58-3 (E)-3-(5-methyl-2-phenyl-4-oxazolylmethoxy)cinnamaldehyde 
• 250601-74-2 ethyl (E)-6-{3-[(5-methyl-2-phenyl-1,3-oxazol-4-yl)methoxy]benzyloxyimino}-6-phenylhexanoate 

Relevant academic research and scientific papers

A back-to-front fragment-based drug design search strategy targeting the DFG-out pocket of protein tyrosine kinases

We present a straightforward process for the discovery of novel back pocket-binding fragment molecules against protein tyrosine kinases. The approach begins by screening against the nonphosphorylated target kinase with subsequent counterscreening of hits against the phosphorylated enzyme. Back pocket-binding fragments are inactive against the phosphorylated kinase. Fragment molecules are of insufficient size to span both regions of the ATP binding pocket; thus, the outcome is binary (back pocket-binding or hinge-binding). Next, fragments with the appropriate binding profile are assayed in combination with a known hinge-binding fragment and subsequently with a known back pocket-binding fragment. Confirmation of back pocket-binding by Yonetani-Theorell plot analysis progresses candidate fragments to crystallization trials. The method is exemplified by a fragment screening campaign against vascular endothelial growth factor receptor 2, and a novel back pocket-binding fragment is presented.

Antihyperglycemic activity of new 1,2,4-oxadiazolidine-3,5-diones

A series of 1,2,4-oxadiazolidine-3,5-diones was synthesized and evaluated as oral antihyperglycemic agents in the obese insulin resistant db/db and ob/ob mouse - the two models for Type 2 diabetes mellitus. The majority of the prepared methoxy- and ethoxy-linked oxazole 1,2,4-oxadiazolidine-3,5-diones normalized plasma glucose levels at the 100 mg kg-1 oral dose in the db/db diabetic mouse model, and several amongst them reduced the glucose levels at the 20 mg kg-1 oral dose. The most potent compounds in the db/db mouse model were also active in the ob/ob mouse model normalizing the plasma glucose levels at the 20 mg kg-1 oral dose. The trifluoromethoxy analog 32 was the most active compound of the series, reducing significantly the plasma glucose levels at the 5 mg kg-1 oral dose. Oxadiazole-tailed 1,2,4-oxadiazolidine-3,5-diones were also active in both the db/db and ob/ob diabetic mouse models normalizing plasma glucose levels at the 100 mg kg-1 oral dose.

Oxazolidinedione derivatives and their use

Novel 2,4-oxazolidinedione compounds of the formula: STR1 wherein R is a hydrocarbon residue or a heterocyclic group each of which may be substituted; Y is --CO--, --CH(OH)-- or --NR3 -- (wherein R3 is an alkyl group which may be substituted); m is 0 or 1; n is 0, 1 or 2; X is CH or N; A is bivalent straight or branched hydrocarbon chain residue having 1 to 7 carbon atoms; R1 and R2 each are hydrogen or an alkyl group, or R1 and R2 are combined with each other to form a 5- to 6-membered heterocyclic group optionally containing nitrogen; L and M each are hydrogen, or L and M are combined with each other to form a bond, or pharmaceutically acceptable salts thereof, having excellent hypoglycemic and hypolipidemic activities and are useful as anti-diabetics or hypolipidemic agents.

Azole phenoxy hydroxyureas as selective and orally active inhibitors of 5- lipoxygenase

Azole phenoxy hydroxyureas are a new class of 5-lipoxygenase (5-LO) inhibitors. Structure-activity relationship studies have demonstrated that electronegative substituents on the 2-phenyl portion of the oxazole tail increased the ex vivo potency of these

Aralkyl-1,2,4-oxadiazolidine-3,5-diones as antihyperglycemic agents

This invention relates to novel compounds having antihyperglycemic properties of the formula: STR1 where A is STR2 wherein: n is 1 or 2; R1 and R3 are independently hydrogen, C1 -C8 alkyl, C1 -C8

ARALKYL-N-HYDROXYUREAS AS INHIBITORS OF 5-LIPOXYGENASE AND OXIDATION OF LOW DENSITY LIPOPROTEIN

This invention relates to compounds compounds useful in treating diseases mediated by one or more leukotrienes or oxidative modification of low density lipoprotein such as inflammation, bronchoconstriction or atherosclerosis. The compounds of this inventi