Synthesis, Antimicrobial Studies, and Docking Simulations of New Bis(4,5-dihydropyrazole) Derivatives
A novel series of bis(3-thienyl-4,5-dihydropyrazoles) has been synthesized by the cyclization reactions of bischalcones with phenyl hydrazine in basic medium. The O-alkylation reactions of chalcones with suitable 1,ω-dibromoalkanes in the presence of anhy
Thiophene and furan appended pyrazoline based fluorescent chemosensors for detection of Al3+ ion
Thiophene and furan appended pyrazoline receptors R1 and R2 were designed and synthesized for selective detection of Al3+ ion. Their photophysical properties were studied by UV–visible and fluorescence spectra. Surprisingly, both receptors R1 a
Rangasamy, Manjunath,Palaninathan, Kannan
p. 177 - 183
(2019/02/06)
Synthesis, characterization, and antioxidant activity of some new benzodiazepine derivatives
A series of novel 4-(substituted phenyl)-2-(2-thienyl)-2,3-dihydro-1H-benzo[b] [1,4] diazepines (MB1-MB8) has been synthesized from 3-(substituted phenyl)-1-(2-thienyl)prop-2-en-1ones (MC1-MC8). The latter compo
Bhat, K. Ishwar,Kumar, Abhishek
p. 397 - 400
(2018/09/29)
Syntheses and in Vitro Antiplasmodial Activity of Aminoalkylated Chalcones and Analogues
(Chemical Equqation Presented). A series of readily synthesized and inexpensive aminoalkylated chalcones and diarylpropane analogues (1-55) were synthesized and tested against chloroquinone-sensitive (D10 and NF54) and -resistant (Dd2 and K1) strains of Plasmodium falciparum. Hydrogenation of the enone to a diarylpropane moiety increased antiplasmodial bioactivity significantly. The influence of the structure of the amine moiety, A-ring substituents, propyl vs ethyl linker, and chloride salt formation on further enhancing antiplasmodial activity was investigated. Several compounds have IC50 values similar to or better than chloroquine (CQ). The most active compound (26) had an IC50 value of 0.01 μM. No signs of resistance were detected, as can be expected from compounds with structures unrelated to CQ and other currently used antimalarial drugs. Toxicity tests (in vitro CHO cell assay) gave high SI indices.
Wilhelm, Anke,Kendrekar, Pravin,Noreljaleel, Anwar E. M.,Abay, Efrem T.,Bonnet, Susan L.,Wiesner, Lubbe,De Kock, Carmen,Swart, Kenneth J.,Van Der Westhuizen, Jan Hendrik
p. 1848 - 1858
(2015/09/08)
Synthesis, pharmacological, and biological screening of novel derivatives of benzodiazepines
A series of novel 4-(substituted phenyl)-2-(thiophen-2-yl)-2,3-dihydro-1H- benzo[b][1,4]diazepine have been synthesized from 3-(substituted phenyl)-1-(thiophen-2-yl)prop-2-en-1-one. 3-(Substituted phenyl)-1-(thiophen-2- yl)prop-2-en-1-one was prepared by
Bhat, K. Ishwar,Chauhan, Manoj Kumar Singh,Kumar, Abhishek,Kumar, Pankaj
p. 1189 - 1192
(2014/08/05)
Thieny/furanyl-hydroxyphenylpropenones as inhibitors of LPS-induced ROS and NO production in RAW 264.7 macrophages, and their structure-activity relationship study
Twelve thienyl/furanyl-hydroxyphenylpropenones were systematically designed and synthesized, and evaluated for their inhibitory effect on LPS-induced ROS and NO production in RAW 264.7 macrophages. Compound 11 displayed the most significant inhibitory activity of LPS-induced ROS and NO production in RAW 264.7 macrophages. Structure-activity relationship study indicated that para-hydroxyphenyl moiety plays an important role for inhibitory activities on both LPS-induced ROS and NO production as well as 3- thienyl moiety on molecule.
Kadayat, Tara Man,Kim, Mi Jin,Nam, Tae-Gyu,Park, Pil-Hoon,Lee, Eung-Seok
p. 2481 - 2486
(2014/09/17)
Synthesis of thiophen-2-yl pyrimidines as antitumor, analgesic and antiinflammatory agents
A series of novel thiophen-2-yl pyrimidine derivatives IV, V(a-e) have beenf synthesized from the intermediate chalcones III(a-h). The structures of these compounds were confirmed by IR, NMR, Mass spectroscopy and elemental analysis. Biological studies of
James, Jainey P.,Bhat, Ishwar K.
p. 309 - 312
(2013/09/24)
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