Newly synthesized compounds

The efficient synthesis of 12-substituted-3,4,4a,5,12,12a-hexahydrobenzo[b]acridine-1,6,11(2H)-triones starting from 2-amino-1,4-naphthoquinone, 1,3-cyclohexanedione, and different (hetero)aromatic aldehydes was developed. These reactions were carried out in acetic acid under microwave irradiation in the presence of p-toluenesulfonic acid as catalyst. The structure of the newly synthesized compounds were confirmed employing spectroscopic data as well as elemental analysis. The plausible mechanism of these three-component domino reactions was also described.

7p dianmotminh02 03-05-2024 4 1   Download

The newly synthesized compounds were screened for their antimicrobial activities; some of them were found to be active towards the test microorganisms as the results demonstrated that the synthesized compounds exhibited a broad spectrum of activity with minimum inhibitory concentration (MIC) values of 31.3–500 µg/mL against gram-positive and gram-negative bacteria, Candia albicans and Saccharomyces cerevisiae.

12p langthannam 29-12-2021 9 0   Download

A number of novel N-acyl/aroyl-2-(5-phenyl-2H-tetrazol-2-yl)acetohydrazides (4a–j) of biological interest were efficiently synthesized by treating 2-(5-phenyl-2H-tetrazole-2-yl)acetohydrazide (3) with a variety of aroyl/heterocyclyl or alkanoyl chlorides. FTIR, 1H NMR, 13C NMR, GC-MS, and elemental analyses data confirmed the structures assigned to the newly synthesized compounds.

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All the complexes showed nonelectrolytic behavior. Moreover, the newly synthesized mixed ligand complexes were evaluated for their in vitro antimicrobial efficiency against bacteria and yeast. The compound named Co(L1 L) had good antifungal activity against Candida species, but no profound antibacterial effect against bacterial strains.

13p langthannam 29-12-2021 11 1   Download

The newly synthesized compounds were characterized and confirmed by analytical and spectroscopic data (IR, MS, 1H NMR, and 13C NMR). Pyrazolo[1,5-a]pyrimidines 5a–c and 9a–c and Schiff bases 11b–f were investigated for their cytotoxicity against four human cancer cell lines (colon HCT116, lung A549, breast MCF-7, and liver HepG2) according to SRB assay and the structure–activity relationship was discussed.

12p langthannam 29-12-2021 14 0   Download

New furanoside-based NHC precursor salts (2) were synthesized using amino alcohols from the chloralose derivatives of glucose (a), galactose (b), and mannose (c). The novel compounds were fully characterized by 1H NMR, 13C NMR, and elemental analyses. The catalytic activities of these salts were tested in the arylation of aldehydes as catalysts that were generated in situ from [RhCl(COD)]2. In addition, 2a was converted to the rhodium complex 3a in order to compare the results obtained in situ.

9p langthannam 29-12-2021 4 0   Download

In the current study, cisplatin loaded (Poly(lactic-co-glycolicacid)) (PLGA) stabilized with 4-phenylphenacylbromide based surfactants nanoparticles were developed for drug delivery applications. For the course of this study four new 4-phenylphenacylbromide based compounds abbreviated as PA(C2 )3 , PA(C8 )3 , PAC16 and PAC18 have been synthesized by the reaction of 4-phenylphenacylbromide with various long chain amines. The new surfactants were characterized with 1 H and 13C NMR and FTIR spectroscopy.

10p langthannam 29-12-2021 10 0   Download

A group of N−4 piperazinyl derivatives of norfloxacin was synthesized and identified by different spectroscopic techniques. The N−4 piperazinyl substituent in target compounds 2a–2k, 3a–3c, and 4a and 4b was designed to have different electronic, steric, and physicochemical properties. The antibacterial activity of the newly synthesized compounds was evaluated against Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae, and Staphylococcus aureus strains using norfloxacin as a reference. Results showed that most of the tested compounds had higher activity against E. coli and K.

14p tudichquannguyet 29-11-2021 8 1   Download

One-pot synthesis of novel quinoline- and quinolone-substituted 1,2,3-triazoles has been performed from the key intermediates, quinoline- and quinolone-substituted propargyl derivatives 1–3 (48%–88% yields). The antioxidant properties of the newly synthesized compounds, 1a–1c, 2a–2c, and 3a–3c, were evaluated by monitoring DPPH (2,2- diphenyl-1-picrylhydrazyl) radical scavenging abilities, metal chelating effects, and reducing power. The scavenging effects of compounds on the free radical decreased in the order of 3b > 3a > 1b and were found to be 36.3%, 34.9%, and 27.

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2-Substituted 8-propargyloxyquinoline derivatives have been synthesized from 2-substituted-8-hydroxyquinolines by O-propargylation method (30%–98% yields). The newly synthesized compounds were tested for in vitro antioxidant activities such as DPPH radical scavenging, ferrous chelating, and reducing power activities. The maximum radical scavenging (46.5%) and reducing power activities were obtained from 1 and maximum ferrous chelating effect was obtained from 6 (72.1%) at the concentration of 500 µg/mL. To indicate DNA binding activity of the complexes calf thymus DNA was used.

12p tudichquannguyet 29-11-2021 14 1   Download

A new series of acetamide derivatives containing 1,2,4-triazole and azinane moieties has been synthesized and characterized using 1H NMR, 13C NMR, IR, and EI-MS spectroscopic analysis. The intermediate triazole was synthesized through a sequential synthesis of carboxylate and carbohydrazide. The bovine serum albumin (BSA) binding of the newly synthesized 1,2,4-triazole derivatives was evaluated along with thermodynamics, site-selective binding, and synchronous study.

20p tudichquannguyet 29-11-2021 15 1   Download

A total of 63 newly synthesized compounds were screened in terms of PARP inhibition by cellular PARylation assay in the HeLa cell line. It was found that 19 compounds significantly inhibited the H2O2 -induced cellular PARylation. The chemosensitizer effect of these compounds in cancer cells treated with doxorubicin (doxo) was investigated. It was found that the combination of potent PARP inhibitors with doxo potentiated a cytotoxic effect, similar to that of olaparib.

26p tudichquannguyet 29-11-2021 6 0   Download

The newly synthesized cyclotriphosphazene cored coumarin chemosensors 5, 6, and 7 were successfully characterized by 1 H NMR, 31P NMR, and MALDI-TOF mass spectrometry. Additionally, the photophysical and metal sensing properties of the targeted compounds were determined by fluorescence spectroscopy in the presence of various metals (Li+, Na+, K+, Cs+, Mg2+, Ca2+, Ba2+, Cr3+, Mn2+, Fe3+, Co2+, Al3+, Hg+, Cu2+, Zn2+, Ag+, and Cd2+). The fluorescence titration results showed that compounds 5, 6, and 7 could be employed as fluorescent chemosensors for Fe3+ ions with high sensitivity.

25p tudichquannguyet 29-11-2021 11 1   Download

Since benzo [b] thiophene scaffold is one of the privileged structures in drug discovery as this core exhibitsactivities for different biological problems, in this study bis (benzo[ b ]thiophene-2-yl) alkyl methanimine derivatives (1-9) were synthesized by reacting benzo[b]thiophene-2-carbaldehyde with diamines. All newly compounds were characterized by IR, 1H NMR and 13C NMR spectroscopic methods.

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Schiff base derivatives with anthracene- and pyrene-based units, A1-A6 and P1-P6 were synthesized (89%–99% yields). Schiff base derivatives were designed to possess an heterocyclic moiety on one side to enhance the coordination ability towards metals. To investigate the biological assay of the newly synthesized compounds, their DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging, metal chelating, reducing power, antibacterial and DNA binding activities were tested. A6 (63.1%) showed the maximum free radical scavenging activity among all.

16p tudichquannguyet 29-11-2021 7 2   Download

Phenyl-4,4-di(3,6-dibutoxyphthalonitrile) (3) was synthesized by the reaction of 1,4-phenylenebisboronic acid (1) and 4-bromo-3,6-dibutoxyphthalonitrile (2), using Suzuki cross-coupling reaction. The newly synthesized compound (3) was characterized by FT-IR, MALDI-MS, ESI-MS, 1 H-NMR, 13C-NMR, and 13C-DEPT-135-NMR.

11p tudichquannguyet 29-11-2021 6 1   Download

In the current research work, a facile synthesis of a series of novel thiophene-based derivatives of 5-bromothiophene-2- carboxylic acid (1) have been synthesized. All analogs (5a-5e, 10a-10f) were obtained from the coupling reaction of 5-bromothiophene2-carboxylic acid (1) and different arylboronic acids with moderate-to-good yields under controlled and optimal conditions. The structures of the newly synthesized compounds were characterized through spectral analysis and their spasmolytic activity, and most of the compounds exhibited potentially good spasmolytic effect.

13p tudichquannguyet 29-11-2021 10 2   Download

This study reports the 3 new phthalonitrile derivatives, namely 4, 5 Bis-[4-(4-bromophenoxy) phenoxy] phthalonitrile (1), 4,5 Bis-[4-(4-chlorophenoxy) phenoxy]phthalonitrile (2), and 4, 5 Bis[4-(4-fluorophenoxy) phenoxy] phthalonitrile (3). Their octasubstituted zinc phthalocyanines (4, 5, 6) are reported for the first time in this study. The resulting compounds were characterized by utilizing some spectroscopic methods, such as UV-Vis, 1 HNMR, FT-IR spectroscopy, as well as mass spectraand elemental analysis.

22p tudichquannguyet 29-11-2021 6 1   Download

In this study, a new series of Mannich bases, 3-(aminomethyl)-6-{3-[4-(trifluoromethyl)phenyl]acryloyl}-2(3H)- benzoxazolones (1a–g), were synthesized by the Mannich reaction. Inhibitory effects of the newly synthesized compounds towards carbonic anhydrases (CAs) and acetylcholinesterase (AChE) enzymes were evaluated to find out new potential drug candidate compounds. According to the inhibitory activity results, Ki values of the compounds 1 and 1a–g were in the range of 12.3 ± 1.2 to 154.0 ± 9.3 nM against hCA I, and they were in the range of 8.6 ± 1.9 to 41.0 ± 5.5 nM against hCA II.

14p tudichquannguyet 29-11-2021 6 1   Download

A series of 5-{[(6-substituted-2-hydroxyquinolin-3-yl)methylidene]/5-[(7-substitutedtetrazolo[1,5-a]quinoline-4-yl)methylidene]}-2-[(4-substitutedphenyl)amino]-1,3-thiazol-4(5H)-one was successfully synthesized under solvent free conditions by microwave irradiation in high yield. Structures of these newly synthesized compounds were established on the basis of spectral and analytical data. These novel compounds were also evaluated for their in vitro antioxidant, antibacterial and antifungal activity.

6p kethamoi1 17-11-2019 23 2   Download