One-pot three-component synthesis of peptidomimics for investigation of antibacterial and antineoplastic properties

AbstractThe α-hydroxyphosphonate generated from dialkyl phosphites and 1-phenyl-1H-pyrazole-4-carbaldehyde derivative was, in situ, trapped by isothiocyanates, isocyanates or acetic anhydride to produce dialkyl phosphorylmethyl-carbamothioates, -carbamates and/or -methyl acetates in good yields. The reactions were carried out in tetrahydrofuran (THF) in one step at room temperature, using K2CO3 catalyst. Antimicrobial and antineoplastic activities of the synthesized compounds were estimated. The results showed that all new compounds cause moderate to good antibiotic activities. However, phosphorylmethylcarbamothioates exhibited the highest growth inhibition. Furthermore, selected nine new synthesized compounds were evaluated for anticancer activity against eight human tumor cell lines (MCF7, MDA-MB-435, BT-549, IGROVI, SK-OV-3, PX-3, PU-145, and HEPG2). The majority of these compounds revealed moderate to potent activity against MCF7, PU-145, and HEPG2. Among them, two of the phosphorylmethylcarbamothioates showed excellent broad spectrum of anticancer activity with IC50 values ranging from 16.6 to 26.9 and 17.2 to 36.9μmolL−1, respectively (for 5-fluorouracil IC50: 17.7 to 38.8μmolL−1). Phosphorylmethyl methylcarbamothioate, in particular was more potent than 5-fluorouracil against all tested human carcinoma cell lines

BIOCHEMICAL STUDIES ON THE ISOLATED FRACTIONS OF DIFFERENT VARIETIES OF RICE

Rice is the staple food of the people of the world food grain. Besides bean the main source of calories and proteins, rice is an important cereal because it has the highest digestibility, biological value and protein efficiency ratio among all the cereals (KAUL et al. 1973). Although rice is an important food in mid and upper Egypt, the isolated fractions of grain rice cultivated in Egypt need to be fully investigated. The objective of the present work was to study the proximate analysis, mineral content, lipids and the amino acid content of some varieties of rice and its isolated fractions

Correlation Between the Total Small Bowel Length and Anthropometric Measures in Living Humans : Cross-Sectional Study

Open Access via Springer Compact AgreementPeer reviewedPublisher PD

Intermolecular interactions of 3,5-bis(4-Methoxyphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide in a cocrystal with 1,3-bis(4-Methoxyphenyl)prop-2-en-1-one and dimethylformamide solvate

Two new multicomponent crystals consisting of 3,5-bis(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide (1) with 1,3-bis(4-methoxyphenyl)prop-2-en-1-one (2) and with dimethylformamide (DMF), both in 1:1 ratio, prepared and structurally characterized. The occurrence of 1 in different crystal structures enabled a comparison of hydrogen bonding contacts between the two structures as well as with the known structure of pure 1. The backbone of molecule 1 was similar in the structures but the orientation of the methoxy groups varied. Molecule 1 was involved in various combinations of the possible hydrogen bonding contacts, including N–H…O=C, N–H…OMe, and N–H…S. Both N–H hydrogens in the cocrystal (1–2) and the solvate (1-DMF) participated in hydrogen bonding but only one hydrogen atom took part in the structure of pure 1. The S atom accepted contacts in both the structures of pure 1 and cocrystal 1–2 but not in that of the 1-DMF solvate. The oxygen atoms of both methoxy groups acted as acceptors in the structure of pure 1, whereas one oxygen was involved in the 1-DMF solvate and none in cocrystal 1–2

(Z)-2-(1-(5-Methyl-1-(4-nitrophenyl)-1H-1,2,3-triazol-4-yl)ethylidene)-N-phenylhydrazine-1-carbothioamide

Reaction of equimolar equivalents of 1-(5-methyl-1-(4-nitrophenyl)-1H-1,2,3-triazol-4-yl)ethan-1-one (1) and N-phenylhydrazinecarbothioamide (2) in boiling ethanol containing a catalytic amount of concentrated hydrochloric acid for 4 h gave (Z)-2-(1-(5-methyl-1-(4-nitrophenyl)-1H-1,2,3-triazol-4-yl)ethylidene)-N-phenylhydrazine-1-carbothioamide (3) with 88% yield. The structure of 3 was established using single-crystal X-ray diffraction and magnetic resonance spectroscopy

Synthesis of new derivatives of the 1H-1,2,3-triazole ring using 1-aryl-5-phenyl-1H-1,2,3-triazole-4-carbohydrazides as precursors

Condensation of 1-(4-nitrophenyl)-5-phenyl-1H-1,2,3-triazole-4-carbohydrazide and phenyl isothiocyanate in ethanol in the presence of a catalytic quantity of triethylamine under reflux gave 5-(1-(4-nitrophenyl)-5-phenyl-1H-1,2,3-triazol-4-yl)-N-phenyl-1,3,4-oxadiazol-2-amine in 84% yield. 2-(2-(5-Phenyl-1H-1,2,3-triazole-4-carbonyl)hydrazineylidene)-N-propanehydrazonoyl chlorides were synthesized, in 87–90% yields, by the condensation of 1-(4-nitrophenyl)-5-phenyl-1H-1,2,3-triazole-4-carbohydrazide and hydrazonoyl chlorides. In a similar manner, condensation of 1H-1,2,3-triazole-4-carbohydrazides and carbonyl compounds in boiling ethanol under acidic conditions gave the corresponding hydrazones in 88–92% yield. The structures of the new heterocycles were confirmed by nuclear magnetic resonance spectral data and X-ray crystallography

Synthesis and characterization of novel 2-(1,2,3-triazol-4-yl)-4,5-dihydro-1 h -pyrazol-1-yl)thiazoles and 2-(4,5-dihydro-1 h -pyrazol-1-yl)-4-(1 h -1,2,3-triazol-4-yl)thiazoles

Reactions of 1-(5-methyl)-1H-1,2,3-triazol-4-yl)ethan-1-ones and benzaldehydes in ethanol under basic conditions gave the corresponding chalcones. Reactions of the chalcones combined with thiosemicarbazide in dry ethanol containing sodium hydroxide afforded the corresponding pyrazolin-N-thioamides. Reactions of the synthesized pyrazolin-N-thioamides and several ketones (namely, ethyl 2-chloro-3-oxobutanoate, 2-bromoacetylbenzofuran, and hydrazonoyl chloride) gave the corresponding novel 2-(1,2,3-triazol-4-yl)-4,5-dihydro-1H-pyrazol-1-yl)thiazoles in high yields (77–90%). Additionally, 2-(4,5-dihydro-1H-pyrazol-1-yl)-4-(1H-1,2,3-triazol-4-yl)thiazoles were obtained in high yields (84–87%) from reactions with N-pyrazoline-thioamides and 4-bromoacetyl-1,2,3-triazoles under basic conditions. The structures of six of the newly synthesized heterocycles were confirmed by X-ray crystallography

(E)-5-(4-Methoxyphenyl)-N?-(2-oxoindolin-3-ylidene)-1-phenyl-1H-pyrazole-3-carbohydrazide

The asymmetric unit of the title compound, C25H19N5O3, is composed of two independent molecules with slightly different conformations. The extended structure features N—H...O hydrogen bonds as well as π–π interactions

Tulžies latakų akmenligė: ligos įtarimas, diagnozė, gydymas

Bile duct stones are a quite common (10–18%) complication of gallstone disease or an autonomous condition. New noninvasive diagnostic methods established in the last decades allow to confirm suspected choledocholithiasis with minimal risk of iatrogenic complications.In this literature review we discuss various scores for choledocholithiasis risk degree, different diagnostic investigations and management approaches including timing for invasive procedures.Tulžies latakų akmenys – gana dažna (10–18 %) tulžies pūslės akmenligės komplikacija ar savarankiška patologija. Pastaraisiais dešimtmečiais atsiradę nauji neinvaziniai diagnostikos metodai leidžia patikslinti įtariamą tulžies latakų akmenligės diagnozę minimalizavus jatrogeninių komplikacijų riziką.Šioje literatūros apžvalgoje aptariamos rizikos vertinimo sistemos, leidžiančios apsispręsti dėl papildomų tyrimų tikslingumo, pristatomi įvairūs diagnostiniai metodai, skirtingos gydymo ir tyrimo taktikos, aptariamas gydymo laiko pasirinkimas