BACKGROUND Pyrazole and pyrazolone motifs are well known for their wide range of biological activities such as antimicrobial, anti-inflammatory, and antitumor activities. The incorporation of more than one pharmacophore in a single scaffold is a well known approach for the development of more potent drugs. In the present investigation, a series of differently substituted 4-arylidene pyrazole de...

Medical Progress in the Last Hundred Years: DR. Anesthetic Effects of Some N-aryl Barbituric Acids M. G. SEELIG .................... .................... 275 Containing Dye-forming Groups: DRS. AXEL M. ScientificEvents: IHJORT, DR. DAVID W. FASSETT and EDWIN J. Scientific Events: DEBEER. Diffraction of X-rays by Built-up Films The Institute of Neuropsychiatry of the University of Proteins: PROF...

A stereoselective synthesis of arylidene N-alkoxydiketopiperazines via oxime-ether formation and intramolecular acylation is described, followed by an acid-catalysed rearrangement-fragmentation to give novel diketopiperazine hemiaminal derivatives with useful bioactivity against certain tumour cell lines.

An organocatalytic asymmetric synthesis of spironitrocyclopropanes has been demonstrated starting from 2-arylidene-1,3-indandiones and bromonitroalkanes catalyzed by a cinchona-derived bifunctional organocatalyst. The products were obtained with excellent enantioselectivities, diastereoselectivities and with good yields.

Background/aims: Pyrimidines have a long and distinguished history extending from the days of their discovery as important constituents of nucleic acids to their current use in medicinal chemistry. As a part of project devoted to the development of pyrimidine analogs as antimicrobial agents we have focused our attention on synthesis of C5/C6 substituted pyrimidine derivatives, specifically C6 s...

Novel near-infrared pyrimidine-fused pH fluorescent probes were prepared by an unusual barbiturate-mediated debenzoindolation and subsequent heteroannulation. A plausible mechanistic pathway is proposed, and the final structures were further elucidated by 2D-NMR. All new compounds are highly fluorescent in the near-infrared region and possess excellent spectral sensitivities to environmental pH...

Model tetrahydropyrido[3',2':4,5]thieno[2,3-b][1,4]thiazines 9a-c were synthesized via reductive lactamization, using sodium dithionite, of the respective 2-[(carboxyalkyl)thio]-3-nitro-4,7-dihydrothieno[2,3-b]pyridine-5-carboxylic acids 7a-c. The latter derivatives were made via interaction of 2-chloro-7-cyclopropyl-3-nitro-4,7-dihydrothieno[2,3-b]pyridine-5-carboxylic acid (6) with each of al...

1-[4-(2-Alkylaminoethoxy) phenylcarbonyl]-3,5-bis(arylidene)-4-piperidones are a novel class of potent cytotoxic agents. These compounds demonstrate low micromolar to submicromolar IC50 values against human Molt 4/C8 and CEM T-lymphocytes and murine leukemia L1210 cells. In this study, a comparative QSAR investigation was performed on a series of 3,5-bis (arylidene)-4-piperidones using differen...

Synthesis of random copolyester bearing 4-arylidene curcumin M 1 in the polymer backbone was prepared by solution polycondensation method. The influence of copolyester bearing 4-arylidene curcumin M 1 unit on the properties of copolyester such as inherent viscosity, solubility, and thermal stability was investigated and studied in detail. The inherent viscosity and polydispersity index of the c...

Dengue is a severe mosquito-borne viral infection causing half a million deaths annually. Dengue virus NS2B/NS3 protease is a validated target for anti-dengue drug design. A series of hitherto unreported 3,5-bis(arylidene)-4-piperidones analogues 4a-4j were synthesized and screened in silico against DENV2 NS2B/NS3 protease to elucidate their binding mechanism and orientation around the active s...