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Antimicrobial Activity of New 2-Thioxo-benzo[g]quinazolin-4(3H)-one Derivatives.
Med Chem 2016; 13(1):85-92MC

Abstract

BACKGROUND

The antimicrobial activity of a synthesized series of 28 2-thioxobenzo[ g]quinazolin-4(3H)-one derivatives was evaluated in vitro against five Gram-positive bacteria, including Bacillus subtilis, Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis and Streptococcus pyogenes. The antibacterial activity was extended to include five Gramnegative bacteria: Pseudomonas aeruginosa, Escherichia coli, Proteus mirabilis, Klebsiella oxytoca and Enterobacter cloacae. Furthermore, the antifungal activity was evaluated against 10 fungal strains, including Aspergillus fumigatus, Syncephalastrum racemosum, Geotricum candidum, Candida albicans, Aspergillus niger, Cryptococcus neoformans, Candida tropicalis, Penicillium expansum, Microsporum canis and Trichophyton mentagrophytes.

METHODS

The agar well diffusion method was adopted against Gram-positive and Gram-negative bacteria and fungi, using ampicillin, gentamicin and amphotericin B as reference drugs, respectively.

RESULTS

The findings of the antibacterial studies revealed that most of the tested compounds possess strong activity against both bacterial species. Compounds 8 and 23 were the most active on Grampositive bacteria, while several compounds demonstrated significant antibacterial activity on Gramnegative bacteria, especially Escherichia coli. Furthermore, several compounds showed strong antifungal activity against many of the investigated fungi. The obtained results were reinforced by determination of the minimum inhibitory concentration for the active compounds against Grampositive and Gram-negative bacteria, as well as fungi, compared to the reference drugs.

CONCLUSION

Many of the investigated compounds showed potent activity against all tested microbial species. The discovery has provided a foundation for the synthesized compounds to serve as a platform for further design and development of more potent antimicrobial agents.

Authors+Show Affiliations

Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.. Saudi Arabia.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

27306606

Citation

Al-Salahi, Rashad, et al. "Antimicrobial Activity of New 2-Thioxo-benzo[g]quinazolin-4(3H)-one Derivatives." Medicinal Chemistry (Shariqah (United Arab Emirates)), vol. 13, no. 1, 2016, pp. 85-92.
Al-Salahi R, Abuelizz HA, Dib RE, et al. Antimicrobial Activity of New 2-Thioxo-benzo[g]quinazolin-4(3H)-one Derivatives. Med Chem. 2016;13(1):85-92.
Al-Salahi, R., Abuelizz, H. A., Dib, R. E., Marzouk, M., & Alshammari, M. B. (2016). Antimicrobial Activity of New 2-Thioxo-benzo[g]quinazolin-4(3H)-one Derivatives. Medicinal Chemistry (Shariqah (United Arab Emirates)), 13(1), pp. 85-92. doi:10.2174/1573406412666160610095706.
Al-Salahi R, et al. Antimicrobial Activity of New 2-Thioxo-benzo[g]quinazolin-4(3H)-one Derivatives. Med Chem. 2016;13(1):85-92. PubMed PMID: 27306606.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Antimicrobial Activity of New 2-Thioxo-benzo[g]quinazolin-4(3H)-one Derivatives. AU - Al-Salahi,Rashad, AU - Abuelizz,Hatem A, AU - Dib,Rabab El, AU - Marzouk,Mohamed, AU - Alshammari,Mohammed B, PY - 2015/11/16/received PY - 2016/06/03/revised PY - 2016/06/03/accepted PY - 2016/6/17/pubmed PY - 2017/8/30/medline PY - 2016/6/17/entrez KW - Antimicrobial KW - amphotericin B. KW - ampicillin KW - benzo[g]quinazoline KW - gentamicin SP - 85 EP - 92 JF - Medicinal chemistry (Shariqah (United Arab Emirates)) JO - Med Chem VL - 13 IS - 1 N2 - BACKGROUND: The antimicrobial activity of a synthesized series of 28 2-thioxobenzo[ g]quinazolin-4(3H)-one derivatives was evaluated in vitro against five Gram-positive bacteria, including Bacillus subtilis, Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis and Streptococcus pyogenes. The antibacterial activity was extended to include five Gramnegative bacteria: Pseudomonas aeruginosa, Escherichia coli, Proteus mirabilis, Klebsiella oxytoca and Enterobacter cloacae. Furthermore, the antifungal activity was evaluated against 10 fungal strains, including Aspergillus fumigatus, Syncephalastrum racemosum, Geotricum candidum, Candida albicans, Aspergillus niger, Cryptococcus neoformans, Candida tropicalis, Penicillium expansum, Microsporum canis and Trichophyton mentagrophytes. METHODS: The agar well diffusion method was adopted against Gram-positive and Gram-negative bacteria and fungi, using ampicillin, gentamicin and amphotericin B as reference drugs, respectively. RESULTS: The findings of the antibacterial studies revealed that most of the tested compounds possess strong activity against both bacterial species. Compounds 8 and 23 were the most active on Grampositive bacteria, while several compounds demonstrated significant antibacterial activity on Gramnegative bacteria, especially Escherichia coli. Furthermore, several compounds showed strong antifungal activity against many of the investigated fungi. The obtained results were reinforced by determination of the minimum inhibitory concentration for the active compounds against Grampositive and Gram-negative bacteria, as well as fungi, compared to the reference drugs. CONCLUSION: Many of the investigated compounds showed potent activity against all tested microbial species. The discovery has provided a foundation for the synthesized compounds to serve as a platform for further design and development of more potent antimicrobial agents. SN - 1875-6638 UR - https://www.unboundmedicine.com/medline/citation/27306606/Antimicrobial_Activity_of_New_2_Thioxo_benzo[g]quinazolin_4_3H__one_Derivatives_ L2 - http://www.eurekaselect.com/143199/article DB - PRIME DP - Unbound Medicine ER -