Substituted phenyl containing 1,3,4-oxadiazole-2-yl-but-2-enamides: synthesis and preliminary evaluation as promising anticonvulsants

In‐house chemical library repurposing: A case example for Pseudomonas aeruginosa antibiofilm activity and quorum sensing inhibition

“…The excess solvent was removed by simple filtration, and the crude product was subjected to column purification on 100–200 silica gel and Hex : EtOAc as eluent. All the synthesized hydrazine‐1‐carbothioamides were characterized using NMR, mass spectrometry and further confirmed by literature reports (Martins et al, ; Siddiqui et al, ).…”

“…High-resolution mass spectra (HRMS) recording was carried out by using 6,520 Agilent Q-Tof LC-MS/MS for the products. All the synthesized hydrazine-1-carbothioamides were characterized using NMR, mass spectrometry and further confirmed by literature reports (Martins et al, 2015;Siddiqui et al, 2014).…”

Facile synthesis, biological evaluation and molecular docking studies of novel substituted azole derivatives

“…The bond angles for the imine junction was slightly shortened from the trigonal geometry as the experimental values for C(7)-N(6)-N(1) was 114.93 (12). Meanwhile, very short bond angles was observed for the C(10)-S( 9)-C(8); 91.57 (9) due to presence of ring strain in the thiophene skeleton. Similarly, the shortening of the internal bond angles was observed for the thiophene nucleus i. e., C( 11 9); 122.53 (12).…”

“…The five-membered heteroaromatic rings are important building blocks of a wide range of biologically active molecules and have become a substantial construction motif in drug discovery [1,2]. The 1,3,4-oxadiazoles are influential heterocyclic systems in the field of synthetic, medicinal and materials chemistry due to their remarkable biological and pharmacological properties such as anti-bacterial [3,4], antimicrobials [5], antifungal [6], anti-oxidant [7], anticancer [8], anticonvulsants [9], antiproliferative [10], anti-inflammatory [11] and insecticidal activities [12], as well as conspicuous enzyme inhibitions against varieties of enzymes including superoxide dismutase [13], gluconeogenesis [14], telomerase [15], α-glucosidase [16], α-amylase [17], histone deacetylase [18] and thymidine phosphorylase [19]. The substituted 2 oxadiazole derivative also have attracted attention in photochemistry for the development of optical sensor, staining agent and storage material due to their consequential light harvesting potential [20,21].…”

Synthesis, spectral characteristics and electrochemistry of symmetrically substituted hybrids derived from 2,5-bis(4-bromophenyl)-1,3,4-oxadiazole under Suzuki cross-coupling reaction

“…[5][6][7][8] One of the most widely studied representatives of electron-injection/hole-blocking materials from this class is 2-(4-biphenylyl)-5-(4-tertbutylphenyl)-1,3,4-oxadiazole (PBD), exhibiting high photoluminescence quantum yield and good thermal and chemical stabilities. 9,10 A literature survey revealed some other examples of π-conjugated 1,3,4-oxadiazole hybrids connected directly or indirectly to other [19][20][21][22][23][24][25][26][27] The leading 1,3,4-oxadiazoles are usually prepared from acid hydrazides as cyclocondensation substrates with carboxylic acids, 28 aromatic aldehydes, 29 orthoesters 30 or by transformations involving other rings, such as 1,2,4-oxadiazole. 31 However, the most popular methodology involves reactions of diacylhydrazines with a range of cyclodehydrating agents, just to mention polyphosphoric acid, boron trifluoride-diethyl etherate, thionyl chloride, phosphorus oxychloride or the Burgess reagent.…”