Synthesis and Characterization of Some Complexes of Cr(iii), Co(ii), Ni(ii), and Cu(ii) With (1-Benzoyl-3-Methyl-1hpyrazol-5(4h)-One

Al-Sabti, Matheel D.; Al-Amiery, Ahmed A.; Al-Majedy, Yasmien K.; Hameed, Anaheed H.

doi:10.22401/jnus.12.4.05

Cited by 4 publications

(2 citation statements)

References 14 publications

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“…Benzohydrazide (2a) and 2‐phenylacetohydrazide (2b) were synthesized according to previously reported procedures (Al‐Sabti, Al‐Amiery, Al‐Majedy, & Hameed, ).…”

Section: Methodsmentioning

confidence: 99%

Synthesis, in vivo and in silico evaluation of novel 2,3‐dihydroquinazolin‐4(1H)‐one derivatives as potential anticonvulsant agents

Kothayer

Ibrahim

Soltan

et al. 2018

Drug Development Research

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In light of the pharmacophoric structural requirements for achieving anticonvulsant activity, a series of N‐(1‐methyl‐4‐oxo‐2‐un/substituted‐1,2‐dihydroquinazolin‐3[4H]‐yl)benzamide (4a‐g) and N‐(1‐methyl‐4‐oxo‐2‐un/substituted‐1,2‐dihydroquinazolin‐3[4H]‐yl)‐2‐phenylacetamide (4h‐n) derivatives were synthesized in two steps starting from the reaction of N‐methyl isatoic anhydride with the appropriate hydrazide and followed by condensation with the appropriate aldehyde. The anticonvulsant activities of the synthesized compounds were evaluated according to the anticonvulsant drug development (ADD) programme protocol. Among the synthesized compounds, 4n showed promising activity in both the maximal electroshock (MES) and pentylenetetrazole (PTZ) tests with median effective dose (ED50) values of 40.7 and 6 mg/kg, respectively. The six most promising derivatives, 4b, 4a, 4c, 4f, 4j, and 4i, showed very low ED50 values in the PTZ test (3.1, 4.96, 8.68, 9.89, 12, and 13.53 mg/kg, respectively). All the tested compounds showed no to low neurotoxicity in the rotarod test with a wide therapeutic index. Docking studies of compound 4n suggested that GABAA binding could be the mechanism of action of these derivatives. The in silico drug likeliness parameters indicated that none of the designed compounds violate Lipinski's rule of five and that they are able to cross the blood–brain barrier. Hit, Lead & Candidate Discovery

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“…Benzohydrazide (2a) and 2‐phenylacetohydrazide (2b) were synthesized according to previously reported procedures (Al‐Sabti, Al‐Amiery, Al‐Majedy, & Hameed, ).…”

Section: Methodsmentioning

confidence: 99%

Synthesis, in vivo and in silico evaluation of novel 2,3‐dihydroquinazolin‐4(1H)‐one derivatives as potential anticonvulsant agents

Kothayer

Ibrahim

Soltan

et al. 2018

Drug Development Research

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show abstract

“…The water molecule is also confirmed the band present at 1012 to 1133 cm -1 due to ν (H 2 O) rocking vibration. Band present in ligand at 1618 cm -1 due to ν (CH=N) vibration shifted to frequency at 1508 to 1643 cm -1 indicating the involvement of azomethine group in coordination [45,46]. Band present in ligand at 1570 cm -1 due to ν (CH=N) vibration of pyridine shifted to frequency at 1400 to 1537 cm -1 indicating the involvement of this group in coordination.…”

Section: Infrared Spectra Of Metal Complexmentioning

confidence: 95%

Synthesis and Spectral Characterization of Lanthanide Complexes Containing Bidentate Schiff Base Derived From Pyridine-2-Carbaldehyde and 2-Hydrazinylquinoline

Rajewar

Dharmale

Pingalkar³

2015

J. Pure App. Chem. Res.

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A series of new rare earth complexes of La(III) of the type [Ln(L) 2 (H 2 O) 2 ]Cl 3 where Ln= La(III), Pr(III), Nd(III), Sm(III) and Tb(III) and L=Schiff base ligand, 2-[2-(pyridin-2ylmethylidene)hydrazinyl]quinoline (PCQH). These complexes have been characterized on the basis of elemental analysis (Ln, C, H, N, and Cl), melting point, IR, 1 H-NMR and UV-Vis spectral data. X-ray powder diffraction study of two of the complex [Nd(L) 2 (H 2 O) 2 ]Cl 3 and Pr(L) 2 (H 2 O) 2 ]Cl 3 was found to be on powder diffraction with Cu-K α1 radiation (λ = 1.5406 Å) showing monoclinic crystal system. The complexes were found to be colored solid and were soluble only in DMF and DMSO.

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Design and synthesis of novel quinazolinones conjugated ibuprofen, indole acetamide, or thioacetohydrazide as selective COX-2 inhibitors: anti-inflammatory, analgesic and anticancer activities

Sakr

Rezq

Ibrahim

et al. 2021

Journal of Enzyme Inhibition and Medicinal Chemistry

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Novel quinazolinones conjugated with indole acetamide (4a–c) , ibuprofen ( 7a–e), or thioacetohydrazide ( 13a,b, and 14a-d ) were designed to increase COX-2 selectivity. The three synthesised series exhibited superior COX-2 selectivity compared with the previously reported quinazolinones and their NSAID analogue and had equipotent COX-2 selectivity as celecoxib. Compared with celecoxib, 4 b , 7c , and 13 b showed similar anti-inflammatory activity in vivo , while 13 b and 14a showed superior inhibition of the inflammatory mediator nitric oxide, and 7 showed greater antioxidant potential in macrophages cells. Moreover, all selected compounds showed improved analgesic activity and 13 b completely abolished the pain response. Additionally, compound 4a showed anticancer activity in tested cell lines HCT116, HT29, and HCA7. Docking results were consistent with COX-1/2 enzyme assay results. In silico studies suggest their high oral bioavailability. The overall findings for compounds ( 4a,b, 7c, 13 b, and 14c ) support their potential role as anti-inflammatory agents.

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Synthesis and Characterization of Some Complexes of Cr(iii), Co(ii), Ni(ii), and Cu(ii) With (1-Benzoyl-3-Methyl-1hpyrazol-5(4h)-One

Cited by 4 publications

References 14 publications

Synthesis, in vivo and in silico evaluation of novel 2,3‐dihydroquinazolin‐4(1H)‐one derivatives as potential anticonvulsant agents

Synthesis, in vivo and in silico evaluation of novel 2,3‐dihydroquinazolin‐4(1H)‐one derivatives as potential anticonvulsant agents

Synthesis and Spectral Characterization of Lanthanide Complexes Containing Bidentate Schiff Base Derived From Pyridine-2-Carbaldehyde and 2-Hydrazinylquinoline

Design and synthesis of novel quinazolinones conjugated ibuprofen, indole acetamide, or thioacetohydrazide as selective COX-2 inhibitors: anti-inflammatory, analgesic and anticancer activities

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