50547-51-8Relevant articles and documents
Design, synthesis, molecular docking, and some metabolic enzyme?inhibition properties of novel quinazolinone derivatives
Tokal?, Feyzi S.,Taslimi, Parham,Demircio?lu, ?brahim H.,Karaman, Muhammet,Gültekin, Mehmet S.,?endil, K?v?lc?m,Gül?in, ?lhami
, (2021/02/09)
3-Amino-2-ethylquinazolin-4(3H)-one (3) was synthesized in two steps from the reaction of amide (2), which was obtained from the treatment of methyl anthranilate (1) with propionyl chloride, with hydrazine. From the reaction of 3-amino-2-ethylquinazolin-4(3H)-one (3) with various aromatic aldehydes, novel benzylidenaminoquinazolin-4(3H)-one (3a–n) derivatives were synthesized. The structures of the novel molecules were characterized using infrared spectroscopy, nuclear magnetic resonance spectroscopy (1H-NMR and 13C-NMR), and high-resolution mass spectroscopy. The novel compounds were tested against some metabolic enzymes, including α-glucosidase (α-Glu), acetylcholinesterase (AChE), and human carbonic anhydrases I and II (hCA I and II). The novel compounds showed Ki values in the range of 244–988 nM for hCA I, 194–900 nM for hCA II, 30–156 nM for AChE, and 215–625 nM for α-Glu. The binding affinities of the most active compounds were calculated as ?7.636, ?6.972, ?10.080, and ?8.486 kcal/mol for hCA I, hCA II, AChE, and α-Glu enzymes, respectively. The aromatic ring of the quinazoline moiety plays a critical role in the inhibition of the enzymes.
Imidazolium chloride as an additive for synthesis of 4(3H)-quinazolinones using anthranilamides and DMF derivatives
Dai, Zeshu,Li, Dan,Li, Zhiyao,Liu, Heng,Luo, Wen,Shang, Suqin,Tian, Qingqiang,Wang, Shuqi,Wang, Xuetong,Wang, Yin,Wu, Huili,Xiao, Xin,Yuan, Jianyong,Zhou, Shangjun
, (2020/09/10)
Imidazolium chloride as an environmentally benign additive efficiently facilitates construction of 4(3H)-quinazolinones using anthranilamides and DMF derivatives. A series of 4(3H)-quinazolinones were prepared in moderate to excellent yields without conventional oxidants, metal catalysts and corrosive acids or other additives.
The stereodivergent aziridination of allylic carbamates, amides and sulfonamides
Davies, Stephen G.,Ling, Kenneth B.,Roberts, Paul M.,Russell, Angela J.,Thomson, James E.,Woods, Philip A.
experimental part, p. 6806 - 6813 (2010/09/17)
A stereodivergent protocol for the aziridination of a range of cyclic allylic amine derivatives has been developed. syn-Products can be obtained in >99:1 dr under H-bonded control and anti-products are obtained in >99:1 dr under steric control by judiciou
