619-86-3Relevant articles and documents
Synthesis, biological activity, molecular docking studies of a novel series of 3-Aryl-7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivatives as the acetylcholinesterase inhibitors
Jin, Zhe,Zhang, Chao,Liu, Miao,Jiao, Simeng,Zhao, Jing,Liu, Xiaoping,Lin, Huangquan,Chi-cheong Wan, David,Hu, Chun
, p. 2478 - 2489 (2020/04/27)
The acetylcholinesterase inhibitors play a critical role in the drug therapy for Alzheimer’s disease. In this study, twenty-nine novel 3-aryl-7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivatives were synthesized and assayed for their human acetylcholinesterase (hAChE) inhibitory activities. Inhibitory ratio values of seventeen compounds were above 55% with 4c having the highest value as 77.19%. The compounds with the halogen atoms in the aromatic ring, and N,N-diethylamino or N,N-dimethylamino groups in the side chains at C-3 positions exhibited good inhibitory activity. SAR study was carried out by means of molecular docking technique. According to molecular docking results, the common interacting site for all compounds were found to be peripheral anionic site whereas highly active compounds were interacting with the catalytic active site too. HIGHLIGHTS A novel series of 3-aryl-7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivatives were synthesized and assayed for their human acetylcholinesterase (hAChE) inhibitory activities. The SAR study of the target 3-aryl-7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivatives was summarized. The active sites in the acetylcholinesterase were analyzed by molecular docking technique. Communicated by Ramaswamy H. Sarma.
Synthesis, mesomorphic properties and biological evolution of calamitic-shaped chalcone-based LCs: effect of lateral and terminal group
Dwivedi, Durgesh J.,Thakor, Akshay,Desai, Vipul,Sharma, Vinay S.,Patel
, p. 16 - 32 (2021/05/26)
The mesomorphic properties of linear shaped homologous series based on two linkage group have been designed and synthesized with different side chain substituents (-OR) on the one end of terminal side with presence of lateral nitro group and second terminal iodo substituted group. Novel series consists thirteen members (C1 to C8, C10, C12, C14, C16, C18). Compounds (C1 to C6) showed nonliquid crystalline properties while compound (C7 to C18) displayed smectic and nematogenic mesophase properties. The textures of smectic C and nematic phase are fan, schlieren and droplets type. All these compounds were characterized by spectroscopic techniques such as [FTIR] and 1H Nuclear magnetic resonance [NMR] spectroscopy. The mesomorphic properties of these compounds were observed by POM and further confirmed by DSC and XRD. Chalconyl ester based compounds (C3 to C12) shows good antibacterial as well as antifungal activity compared with corresponding standard drugs.
λ-shaped to T-shaped azo diester mesogens having methyl (–CH3)/methoxy(–OCH3) terminal substituents with trisubstituted benzene
Duan, Yongtao,Koshti, Rohit R.,Kumar Ameta, Rakesh,Patel, H. N.,Sangani, Chetan B.,Tarpada, Umesh P.,Vyas, Akshay,Yao, Yongfang
, (2021/07/12)
A two new homologous series of λ-shape to T-shape mesogenic azo diesters were synthesized, and their thermotropic properties were studied by differential scanning calorimetry and a hot-stage polarizing optical microscope. The difference between these two series is in the structure of terminal substituents methyl (–CH3) for series I and methoxy (–OCH3) for series II at one terminus. Structure variation from λ-shape to T-shape as we go from lower members to higher members is discussed. In the series I, methoxy to n-pentyloxy derivatives are non-mesogenic. n-hexyloxy derivative exhibits only monotropic nematic mesophase. n-heptyloxy to n-dodecyloxy derivatives exhibit monotropic smectic C mesophase. n-tetradecyloxy derivative exhibits enantiotropic SmA mesophase, whereas n-hexadecyloxy derivatives exhibit monotropic Smectic A mesophase. In series II, methoxy to n-hexyloxy derivatives are non-mesogenic. n-heptyloxy and n-octyloxy derivatives exhibit monotropic smectic C mesophase. Smectic A mesophase commences from the n-decyloxy derivative as a monotropic and persists up to the last member synthesized. The mesomorphic properties of the present series were compared with each other and with the structurally related mesogenic homologous series to evaluate the effect of methyl (–CH3)/methoxy (–OCH3) substituents as well as variation in the shape of the molecule by varying the alkoxy chain length of the bulky lateral substituent on mesomorphism.
