A series of 4-amino-5-chloro-2-methoxy-N-(piperidin-4-ylmethyl)benzamides with a polar substituent group at the 1-position of the piperidine ring was synthesized and evaluated for its effect on gastrointestinal motility. The benzoyl, phenylsulfonyl, and benzylsulfonyl derivatives accelerated gas...

Novel 4-oxobenzo[d]1,2,3-triazin derivatives bearing pyridinium moiety 6a–q were synthesized and screened against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Most of the synthesized compounds showed good inhibitory activity against AChE. Among the synthesized compounds, the c...

Ullmann-type reactions are becoming a major tool in medicinal chemistry. In this article, we describe the use of these Copper-catalyzed reactions with various precursors, acyl-heteroarylamines or pyrazoles of interest for pharmacomodulation. To the medicinal chemist they offer new, usually untap...

In the search for new antifungal compounds and to explore structure activity relationships, a series of 24 chiral benzyl amine type antifungals was synthesised and characterised. In vitro testing against the human pathogen Cryptococcus neoformans revealed that several derivatives had MIC50 value...

We designed and synthesized a tri-(2-picolyl) amine (TPA) functionalized triarylborane, 1-(6-(4-(dimesitylboryl)phenyl)pyridin-2-yl)-N,N-bis(pyridin-2-ylmethyl)methanamine (PB2). The photophysical properties of PB2 were thoroughly explored. Moreover, PB2 can capture CN− and F− in aqueous solutio...

This work presents a three-step synthesis of a new series of 4-substituted 2-oxo-6-trihalomethyl-[1,3]oxazinane-3-carboxylic acid ethyl esters, from β-alkoxyvinyl trihalomethyl ketones of general formula X3C–C(O)–CHC(R)–OR1, where R = H, Me, Ph, and 4-Me-Ph; R1 = Me and Et; and X = F and Cl....

The multistep synthesis of 3,5-dimethyl-6-phenyl-8-(trifluoromethyl)-5,6-dihydropyrazolo[3,4-f][1,2,3,5]tetrazepin-4(3H)-one 15 has been carried out. The compound showed antiproliferative and apoptotic effects against K562, K562-R (imatinib mesilate resistant), HL60 and multidrug resistant (MDR)...

Cocrystallization experiments of the commonly available 4-aminobenzoic acid(L1)/2-aminobenzoic acid(L2), with a series of organic acids gave a total of five molecular salts with the compositions: (4-aminobenzoic acid): (dichloroacetic acid)2 (1) [(HL1)+ · (dca−) · (Hdca), dca− = dichloroacetat...

The acid hydrolysis l-N-(N’-vinyloxyethylthiocarbamoyl)ephedrine has been investigated and the X-ray diffraction analysis of the synthesised (4S,5R)-3,4-dimethyl-5-phenyl-2-(hydroxyethylimino)-1,3-thiazolidine has been carried out.

A green chemical route is reported for the synthesis of cobalt and cobalt carbide nanostructures using decomposition of cobalt acetate salt in a carbon matrix in situ during spark plasma sintering (SPS). The effect of SPS pressure on the phase formation was studied in detail and it revealed that...

Primarily, the vibrational analysis of 4-chloro-3-(trifluoromethyl)aniline, 4-bromo-3-(trifluoromethyl)aniline and 4-fluoro-3-(trifluoromethyl)aniline are studied through an experiment by means that of Fourier Transform-Infrared and Fourier Transform-Raman techniques. The electrons both of donat...

This study was navigated to examine the effects of fungicide-stress on the activities of plant-growth-promoting rhizobacterium Pseudomonas putida with inherent phosphate solubilizing activity. The fungicide-tolerant and phosphate solubilizing P. putida strain PS9 was isolated from the mustard rh...

Screening efforts identified (bis)sulfonic acid, (bis)benzamides (1–3) as compounds that interact with the follicle stimulating-hormone receptor (FSHR) and inhibit FSH-stimulated cAMP accumulation with IC50 values in the low micromolar range. Structure–activity relationship studies using novel...

In this paper, we describe the synthesis of 4′-C-aminoalkyl-2′-O-methylnucleosides and the properties of RNAs containing these analogs. Phosphoramidites of 4′-C-aminoethyl and 4′-C-aminopropyl-2′-O-methyluridines were prepared using glucose as starting material, and RNAs containing the anal...

2-Chloro-N-ethoxycarbonylmethylpyridinium bromide reacts with substituted acetonitriles in two steps; the initially formed pyridine anhydro baseses undergo further ring closure to 2-amino-3-ethoxycarbonylindolizines.

A one-pot efficient, green, practical, and environmentally friendly multicomponent synthesis of 5-oxo-4-aryl-5,6,7,8-tetrahydro-4H-chromenes, ethyl-6-amino-4-aryl-5-cyano-2-methyl-4H-pyran-3-carboxylates as well as 2-amino-4-aryl-7-hydroxy-4H-chromene-3-carbonitriles via tandem the Knoevenagel-c...

A facile and efficient one-pot synthesis of 1,4-disubstituted 3-amino-2-pyridone derivatives via three-component reactions of readily available alkynyl aldehydes, amines, and ethyl 2-((diphenylmethylene)amino)acetate has been developed. The alkynyl aldehyde substrates and the amine partners can ...

Design, microwave-assisted synthesis of novel 4-aryl (alkyl)amino-3-nitroquinoline (1a–1l) and 2,4-diaryl (dialkyl)amino-3-nitroquinolines (2a–2k and 3a) via regioselective and complete nucleophilic substitution of 2,4-dichloro-3-nitroquinoline, respectively in water are presented. The newly s...

Various thiazolidine-2,4-dione derivatives 3a-l possessing indole moiety were designed, synthesized using appropriate conventional heating as well as microwave irradiation methods. All the synthesized compounds were characterized physically and spectrally. The compounds were evaluated for in vit...

Cholesterol oxidation in food and model systems is usually monitored by evaluating cholesterol oxidation products, but the analysis is time-consuming and expensive. Therefore, the determination of volatile compounds deriving from cholesterol thermoxidation could be valuable to identify other pos...