6296-54-4Relevant articles and documents
Synthesis of pyrazine-2,3-dicarbonitriles via the one-pot three-component reaction of 4-benzoyl-5-phenylamino-2,3-dihydrothiophene-2,3-dione, diaminomaleonitrile, and functionalized alcohols in acetonitrile
Shahnaei, Roya,Kabirifard, Hassan,Fathololoomi, Parinaz
, p. 550 - 555 (2020)
An efficient one-pot three-component reaction of 4-benzoyl-5-phenylamino-2,3-dihydrothiophene-2,3-dione, diaminomaleonitrile, and alcohols with hetero-atom substituents or several hydroxyl groups in acetonitrile solvent under reflux led to the formation o
Reactions of 4-benzoyl-5-phenylamino-2,3-dihydrothiophene-2,3-dione and diaminomaleonitrile in the presence of alcohols as reactant and solvent
Moloudi, Maryam,Kabirifard, Hassan,Kabirifard, Raihaneh,Mahdikhani, Mona
, p. 347 - 356 (2017)
The one-pot synthesis of a novel class of 5-(2-alkoxy-2-phenyl-1-N-phenylthiocarbamoylethenyl)-6-oxo-1,6-dihydropyrazine-2,3-dicarbonitriles (2a–o) is achieved in moderate to good yields by the sequential reaction between 4-benzoyl-5-phenylamino-2,3-dihyd
Small-molecule vasopressin-2 receptor antagonist identified by a G-protein coupled receptor "pathway" screen
Yangthara, Buranee,Mills, Aaron,Chatsudthipong, Varanuj,Tradtrantip, Lukmanee,Verkman, Alan S.
, p. 86 - 94 (2007)
G-protein-coupled receptors (GPCRs) such as the vasopressin-2 receptor (V2R) are an important class of drug targets. We developed an efficient screen for GPCR-induced cAMP elevation using as read-out cAMP activation of cystic fibrosis transmemb
Design, synthesis, and biological activity evaluation of 2-(benzo[b]thiophen-2-yl)-4-phenyl-4,5-dihydrooxazole derivatives as broad-spectrum antifungal agents
Zhao, Liyu,Sun, Yin,Yin, Wenbo,Tian, Linfeng,Sun, Nannan,Zheng, Yang,Zhang, Chu,Zhao, Shizhen,Su, Xin,Zhao, Dongmei,Cheng, Maosheng
, (2021/11/22)
To discover antifungal compounds with broad-spectrum and stable metabolism, a series of 2-(benzo[b]thiophen-2-yl)-4-phenyl-4,5-dihydrooxazole derivatives was designed and synthesized. Compounds A30-A34 exhibited excellent broad-spectrum antifungal activity against Candida albicans with MIC values in the range of 0.03–0.5 μg/mL, and against Cryptococcus neoformans and Aspergillus fumigatus with MIC values in the range of 0.25–2 μg/mL. In addition, compounds A31 and A33 showed high metabolic stability in human liver microsomes in vitro, with the half-life of 80.5 min and 69.4 min, respectively. Moreover, compounds A31 and A33 showed weak or almost no inhibitory effect on the CYP3A4 and CYP2D6. The pharmacokinetic evaluation in SD rats showed that compound A31 had suitable pharmacokinetic properties and was worthy of further study.
RETRACTED ARTICLE: IspH inhibitors kill Gram-negative bacteria and mobilize immune clearance
Singh, Kumar Sachin,Sharma, Rishabh,Reddy, Poli Adi Narayana,Vonteddu, Prashanthi,Good, Madeline,Sundarrajan, Anjana,Choi, Hyeree,Muthumani, Kar,Kossenkov, Andrew,Goldman, Aaron R.,Tang, Hsin-Yao,Totrov, Maxim,Cassel, Joel,Murphy, Maureen E.,Somasundaram, Rajasekharan,Herlyn, Meenhard,Salvino, Joseph M.,Dotiwala, Farokh
, p. 597 - 602 (2020/12/25)
Isoprenoids are vital for all organisms, in which they maintain membrane stability and support core functions such as respiration1. IspH, an enzyme in the methyl erythritol phosphate pathway of isoprenoid synthesis, is essential for Gram-negati