Antimicrobial Activity of Synthesized 2-Methylthiobenzo[g][1,2,4]- triazolo[1,5-a]quinazoline Derivatives

Al‐Salahi, Rashad; Abuelizz, Hatem A.; Wadi, Mahasin; Dib, Rabab A. El; Alotaibi, Mshari A.; Marzouk, Mohamed

doi:10.2174/1573406412666160502155106

Cited by 14 publications

(5 citation statements)

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“…On the other hand, the triazole moiety is found in many important biologically active compounds. Synthesized molecules with a triazole moiety possess anti-tubercular [ 17 ], antimicrobial [ 18 ], anti-cancer [ 19 ] and anti-inflammatory [ 20 ] activity. Triazole-based heterocyclic derivatives have enhanced biological activity or possess new biological activities [ 21 ].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, crystallographic characterization, molecular docking and biological activity of isoquinoline derivatives

Abuelizz

Al‐Salahi

Al-Asri

et al. 2017

Chemistry Central Journal

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The main objective of this work was to synthesize novel compounds with a benzo[de][1,2,4]triazolo[5,1-a]isoquinoline scaffold by employing (dioxo-benzo[de]isoquinolin-2-yl) thiourea as a building block. Molecular docking was conducted in the COX-2 active site to predict the plausible binding mode and rationalize the structure–activity relationship of the synthesized compounds. The structures of the synthesized compounds were confirmed by HREI-MS, and NMR spectra along with X-ray diffraction were collected for products 1 and 5. Thereafter, anti-inflammatory effect of molecules 1–20 was evaluated in vivo using carrageenan-induced paw edema method, revealing significant inhibition potency in albino rats with an activity comparable to that of the standard drugs indomethacin. Compounds 8, 9, 15 and 16 showed the highest anti-inflammatory activity. However, thermal sensitivity-hot plat test, a radiological examination and motor coordination assessment were performed to test the activity against rheumatoid arthritis. The obtained results indicate promising anti-arthritic activity for compounds 9 and 15 as significant reduction of the serum level of interleukin-1β [IL-1β], cyclooxygenase-2 [COX-2] and prostaglandin E2 [PGE2] was observed in CFA rats.Electronic supplementary materialThe online version of this article (doi:10.1186/s13065-017-0321-1) contains supplementary material, which is available to authorized users.

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Section: Introductionmentioning

confidence: 99%

Synthesis, crystallographic characterization, molecular docking and biological activity of isoquinoline derivatives

Abuelizz

Al‐Salahi

Al-Asri

et al. 2017

Chemistry Central Journal

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“…Firstly, the invitro analysis of HL and metal complexes were confimed through inhibition zone (IZ) with three fungi: Syncephalastrum racemosum (RCMB, 016001, Sr), Aspergillus fumigatus (RCMB 02568, Af), and G. candidum (RCMB 052006, Gc); two Gram-positive bacteria: S. pneumoniae (RCMB 010010, Sp) and Bacillus subtilis (RCMB 010069, Bs); and one Gram-negative bacteria: E. coli (RCMB 010052, Ec). [28][29][30][31][32] Various strains were supplied through immunizing refresh stock cultures in dispersed tubes with broth, each of which contained 7 ml of nutrient broth (peptone, 0.3%) and beef extract (0.3%). Vaccine tubes were raised at 37 C for 1 day.…”

Section: Antimicrobial Evaluationmentioning

confidence: 99%

Synthesis, characterization, thermal studies, electrochemical behavior, antimicrobial, docking studies, and computational simulation of triazole‐thiol metal complexes

Fahim

Magar

Ayoub

2022

Applied Organom Chemis

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In this study, we elucidate the structure and molecular properties of triazole‐thiol derivative (HL) which is confirmed via B3LYP/6‐31G(d) for DFT and HF basis set. Triazole‐thiol (HL) was conjugated with several metal ions to afford stable metal complexes. Consequently, confirmed via intensive physicochemical analysis including FT‐IR spectra, elemental analysis, electronic, 1H‐NMR, TGA, and DTA. The explanation of the thermal cracking of these metal complexes has been estimated. The FT‐IR of these complexes indicated the presence of triazole‐thiol ligand (HL) as chelated coordinated through the N atom of amino group and S atom of SH moiety. Furthermore, Fe(III) complex and Ni(II) adopt octahedral stereochemistry, while the Cu(II) complex is trigonal bipyramidal, and Cd(II) complex is square planar. Thermal investigation maintained the chemical formulation of these metal complexes and exhibited that they decompose in many stages dependent on the kind of ligand and geometry of complexes. Moreover, the HL and metal complexes were exhibited antimicrobial evaluation against bacterial and fungal strains and showed higher activity comparable HL. Additionally, the theoretical docking stimulation of the ligand HL and metal complexes with different proteins showed different in energy affinity with shortage bond length with metal complexes and confirmed the experimental biological results. Eventually, the electrochemical features were explored utilizing cyclic voltammetry (CV) and electrochemical impedance spectroscopy (EIS).

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“…Benzoquinazolines, the basic components of numerous well-known heterocyclic systems, have played a significant role in the creation of various bioactive molecules. Extensive research conducted on benzoquinazolines in our lab has demonstrated their powerful pharmacological effects in a variety of contexts such as antioxidant, antimicrobial, anticancer and antidiabetic agents [ 20 , 21 , 22 , 23 , 24 , 25 , 26 , 27 , 28 , 29 ], and particularly against a number of different viral infections as HSV-1, HSV-2, HAV, HCV and coxsackievirus B4 [ 30 , 31 , 32 ]. Through the analysis of our data, we were able to gather insights into the characteristics that will define future trials, which paved the path for the development of benzo[g]quinazolines as anti-human rotavirus Wa strain drugs.…”

Section: Introductionmentioning

confidence: 99%

Evaluation of Some Benzo[g]Quinazoline Derivatives as Antiviral Agents against Human Rotavirus Wa Strain: Biological Screening and Docking Study

Abuelizz

Bakheit

Marzouk

et al. 2023

CIMB

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Globally, rotavirus (RV) is the most common cause of acute gastroenteritis in infants and toddlers; however, there are currently no agents available that are tailored to treat rotavirus infection in particular. Improved and widespread immunization programs are being implemented worldwide to reduce rotavirus morbidity and mortality. Despite certain immunizations, there are no licensed antivirals that can attack rotavirus in hosts. Benzoquinazolines, chemical components synthesized in our laboratory, were developed as antiviral agents, and showed good activity against herpes simplex, coxsackievirus B4 and hepatitis A and C. In this research project, an in vitro investigation of the effectiveness of benzoquinazoline derivatives 1–16 against human rotavirus Wa strains was carried out. All compounds exhibited antiviral activity, however compounds 1–3, 9 and 16 showed the greatest activity (reduction percentages ranged from 50 to 66%). In-silico molecular docking of highly active compounds, which were selected after studying the biological activity of all investigated of benzo[g]quinazolines compounds, was implemented into the protein’s putative binding site to establish an optimal orientation for binding. As a result, compounds 1, 3, 9, and 16 are promising anti-rotavirus Wa strains that lead with Outer Capsid protein VP4 inhibition.

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Antimicrobial Activity of Synthesized 2-Methylthiobenzo[g][1,2,4]- triazolo[1,5-a]quinazoline Derivatives

Abstract: The promising compounds could be employed as useful scaffolds for building of new derivatives with more potent antimicrobial effects.

Cited by 14 publications

References 0 publications

Synthesis, crystallographic characterization, molecular docking and biological activity of isoquinoline derivatives

Synthesis, crystallographic characterization, molecular docking and biological activity of isoquinoline derivatives

Synthesis, characterization, thermal studies, electrochemical behavior, antimicrobial, docking studies, and computational simulation of triazole‐thiol metal complexes

Evaluation of Some Benzo[g]Quinazoline Derivatives as Antiviral Agents against Human Rotavirus Wa Strain: Biological Screening and Docking Study

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