Inspired by the common structural characteristics of numerous known antitumor compounds targeting DNA or topoisomerase I, 3-(benzazol-2-yl)-quinoxaline-based scaffold was designed via the combination of two important privileged structure units —quinoxaline and benzazole. Thirty novel 3-(benzazo...

Selective incorporation of a fluoroalkyl moiety to modulate the properties of an organic molecule has become a frequently used strategy in life science- and materials science-related applications. In this context, selective introduction of a (phenylsulfonyl)difluoromethyl group (PhSO2CF2) into o...

In this study, the reaction of pentafluoropyridine and 4-phenylsulfonyl tetrafluoropyridine with difunctional nitrogen and sulfur nucleophiles such as thiourea, thioamide derivatives, and unsymmetrical bidentate nitrogen nucleophiles such as diamino-triazole and amino-imidazole in the presence o...

2-Chloro-N-{2-fluoro-5-[N-(phenylsulfonyl) phenylsulfonamido]phenyl}benzamide was synthesized and its crystal structure was also determined by X-ray single-crystal diffraction. The title compound(C25H18CIFN2O5S2) belongs to monoclinic, space group P21/n with a=0.7377(3) nm, b=1.2036(5) nm, c=2.6...

A new strategy for nucleophilic addition to aldehydes with difluoromethyl organometallic reagents has been developed by functionalizing the difluoromethyl moiety with the phenylsulfonyl group (SO2Ph). This electron-withdrawing group influences both the thermodynamic stability and the nucleophili...

[2,3] Wittig ring contraction of the achiral 13-membered acetylenic ether 1 via treatment with lithio (R,R) or (S,S)-bis-(1-phenylethyl)amide afforded the (R)-(+) or (S)-(-)-propargylic alcohol (+)-2 or (-)-2, respectively, of > 60% ee in 75% yield.

The total synthesis of (±)-aristolactone (15) is described wherein the key cyclodecenynol precursor 10 is prepared in over 90% yield via a highly regio and stereoselective [2,3] Wittig rearrangement of the 13-membered propargylic ether 9.

The bioproduction of lactobionic acid and its salts can be performed by enzymatic complex glucose-fructose oxidoreductase (GFOR) and glucono-δ-lactonase (GL) of Zymomonas mobilis. Considering the applicability of these compounds in pharmaceutical area, the aim of this study was to assess the ac...

Trans-anethole (TA) is a phenolic phytocompound widely used in the food and health sector because of its diverse biological properties. However, its role in the promotion of bone formation is not known. With the enhanced bioavailability of TA, we aimed to determine its effect on osteogenesis; TA...

A series of 4-(1-substituted piperidin-4-yloxy) benzamides and 6-(1-substituted piperidin-4-yloxy)-3,4-dihydro-2H-isoquinolin-1-one derivatives have been synthesized and tested for their binding affinity towards H3 receptor. Most of these synthesized compounds have displayed potent binding affin...

Morpholine amides are cheap and safe alternative to Weinreb amides as acylating agents of organometallic species. Herein, the in-situ lithiation/borylation of 18 ortho- meta- and para-substituted morpholine benzamides has been investigated. 10 of the 18 substrates provided the desired boronic es...

A high-performance liquid chromatographic procedure is presented for the simultaneous determination of isoniazid and 1-isonicotinyl-2-lactosylhydrazine (I) in isoniazid tablet formulations. An aliquot of a diluted aqueous tablet extract is introduced onto a microparticulate cyanopropyl bonded-ph...

A variety of 2-amino-3-cyano-5-oxo-4-perfluoroalkyl-5,6,7,8-tetrahydro-4H-chromene derivatives were achieved via a one-pot, three-component reaction from easily available methyl 2-perfluoroalkynoate, malononitrile (or ethyl cyanoacetate), and diverse cyclic 1,3-diketones. Moderate to good yields...

An improved, forthright, and highly efficient one-pot synthesis of a wide range of pharmaceutically exciting diverse kind of functionalized 2-amino-3-cyano-4H-pyrans and especially bis-pyrans compounds is developed using piperazine as a low-cost and environmentally benign commercially available ...

Ligand-exchange chromatography data, polarimetric titration and electronic spectra show that in the mixture of (CuL2), (CuD2) and CuLD) complexes formed by Cu(II) ions with racemic N-benzyl-dl-valine in aqueous or methanolic solutions the equally-paired structures (CuD2) and (CuL2) are more stab...

α-Substituted amines are present in a myriad of biologically active natural and synthetic products. With the objective of developing atom-economical reactions, a panel of synthetic methods allowing the direct functionalization of C(sp3)‒H bonds adjacent to the nitrogen atom have been developed....

A novel computer model of the HIV reverse transcriptase (RT) non-nucleoside inhibitor (NNI) binding pocket, which was generated using high resolution crystal structure information from 9 individual RT/NNI complexes, revealed previously unrecognized ligand derivatization sites for phenethylthiazo...

Lantern-type dinuclear complexes, cis-[Ru2{3,5-(CF3)2-pf}2(O2CMe)2Cl] and [Ru2{3,5-(CF3)2-pf}3(O2CMe)Cl] (3,5-(CF3)2-pf− = N,N′-bis[3,5-bis(trifluoromethyl)phenyl]formamidinate anion), were prepared and characterized. The cis-(2:2) and (3:1) arrangements of the formamidinate and acetate bridgin...

Reaction of a trinuclear silver pyrazolate {[3,5-(CF3)2Pz]Ag}3 complex with tricyclohexylphosphine at different reagent ratios leads to the formation of heteroleptic dinuclear or tetranuclear complexes. According to the single crystal X-ray analysis of the dinuclear complex, hexane molecules are...

Pyrazoles represent important building blocks for the preparation of bioactive compounds and a large variety of materials, due to their rich coordination chemistry. Unusual and interesting properties may be imparted to molecules embodying highly fluorinated pyrazoles, but to date only few exampl...