21411-14-3

Upstream product

• 2916-09-8 2-ethyl-benzo[d][1,3]oxazin-4-one 
• 79-03-8 propionyl chloride 
• 28144-70-9 anthranilic acid amide 
• 123-38-6 propionaldehyde 
• 118-92-3 anthranilic acid 
• 19165-26-5 2-(propionylamino)benzoic acid 

Downstream Products

• 3137-64-2 2-ethyl-3H-quinazolin-4-one 
• 38154-40-4 4-chloro-2-ethylquinazoline 

Relevant academic research and scientific papers

Synthesis, in silico study and cholinesterases inhibition activity of 2-substituted 2, 3-dihydroquinazolin-4(1H)-one derivatives

We have synthesized and evaluated a number of 2, 3-dihydroquinazolin-4(1H)-one derivatives as inhibitors of cholinesterases. In vitro assay results revealed that all synthesized compounds are active against both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes and few compounds having longer alkyl chain at C-2 position showed better inhibition activity than standard drug galantamine. Moreover, bromo derivatives 6a-d were more active than nitro 5a-d and their un-substituted counterparts 4a-d. Amongst all, compound 6d, with IC50 values of 4.8±1.01 μM (AChE) and 11.1±1.15 μM (BChE) can be considered as good cholinesterase (AChE/BChE), inhibitor with greater selectivity towards BChE. In silico calculations revealed that all compounds have good pharmacokinetic profile along with having high probabilities for penetration across blood brain barrier (BBB), human intestinal absorption (HIA), non-AMES toxicity and non-carcinogenicity except nitro substituted derivatives which were predicted to show AMES toxicity. The synthesized compounds may lead toward development of new potent cholinesterase inhibitors.

Rapid synthesis of 2,3-disubstituted-quinazolin-4-ones enhanced by microwave-assisted decomposition of formamide

An efficient methodology for the preparation of a series of 2,3-disubstituted-quinazolin-4(3H)-ones is described via a three step reaction from anthranilic acid. The obtained results also reveal that microwave-assisted rapid decomposition of formamide under controlled conditions of power, temperature and time is a very convenient source of ammonia for the synthesis of 2-substituted-quinazolin-4(3H)-ones and other rings.

COMPOSITIONS AND METHODS FOR MODULATING GATED ION CHANNELS

Disclosed are quinoline and quinazoline compounds which modulate the activity of the gated ion channels. Compounds that modulate these gated ion channels are useful in the treatment of diseases and disorders related to pain, inflammation, the neurological system, the gastrointestinal system and genitourinary system. Preferred compounds include quinoline or quinazoline derivatives substituted at the 4- position via N(H), C(O) or O moieties.

Phosphodiesterase inhibitory properties of losartan. Design and synthesis of new lead compounds

A 4-centre PDE 4 pharmacophore search has been carried out in several 3D-databases containing compounds belonging to different therapeutic areas. Losartan, an angiotensin-II antagonist, has been identified as a new lead compound for developing PDE 4 inhibitors. New families of compounds derived from losartan has been synthesized and their PDE inhibition has been measured.