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Hydrazones of 2-aryl-quinoline-4-carboxylic acid hydrazides: synthesis and preliminary evaluation as antimicrobial agents.
Bioorg Med Chem. 2006 Dec 15; 14(24):8675-82.BM

Abstract

A new series of 2-arylquinoline-4-carboxylic acid hydrazide-hydrazones was synthesized using an appropriate synthetic route. All the target compounds were evaluated for their in vitro antimicrobial activity against Staphylococcus aureus as an example for Gram-positive bacteria, Escherichia coli as an example for Gram-negative bacteria, and Candida albicans as a representative of fungi. The minimum inhibitory concentration (MIC) was determined for test compounds as well as for reference standards. Among the compounds tested, compounds having nitro substituents at the arylidene moiety showed the most potent antifungal as well as antibacterial activities against E. coli. Compound 23 displayed an antifungal activity comparable to that of nystatin. However, none of the compounds demonstrated any antibacterial activity against S. aureus. Hydrophobicity of the target compounds correlated weakly with their antibacterial and antifungal activities. The most potent compounds namely, 7, 18, 19, 22, and 23 were assessed for hemolytic toxicity and found to be non-hemolytic up to a concentration of 100mug/mL. In addition, the most potent compound (23) was evaluated for in vitro cytotoxic activity against various cancer cell lines. This compound was found to display no cytotoxic activity but rather it induces the proliferation rate of Hep-G2 cells.

Authors+Show Affiliations

Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt. kametwally@hotmail.comNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

16949294

Citation

Metwally, Kamel A., et al. "Hydrazones of 2-aryl-quinoline-4-carboxylic Acid Hydrazides: Synthesis and Preliminary Evaluation as Antimicrobial Agents." Bioorganic & Medicinal Chemistry, vol. 14, no. 24, 2006, pp. 8675-82.
Metwally KA, Abdel-Aziz LM, Lashine el-SM, et al. Hydrazones of 2-aryl-quinoline-4-carboxylic acid hydrazides: synthesis and preliminary evaluation as antimicrobial agents. Bioorg Med Chem. 2006;14(24):8675-82.
Metwally, K. A., Abdel-Aziz, L. M., Lashine, e. l. -. S. M., Husseiny, M. I., & Badawy, R. H. (2006). Hydrazones of 2-aryl-quinoline-4-carboxylic acid hydrazides: synthesis and preliminary evaluation as antimicrobial agents. Bioorganic & Medicinal Chemistry, 14(24), 8675-82.
Metwally KA, et al. Hydrazones of 2-aryl-quinoline-4-carboxylic Acid Hydrazides: Synthesis and Preliminary Evaluation as Antimicrobial Agents. Bioorg Med Chem. 2006 Dec 15;14(24):8675-82. PubMed PMID: 16949294.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Hydrazones of 2-aryl-quinoline-4-carboxylic acid hydrazides: synthesis and preliminary evaluation as antimicrobial agents. AU - Metwally,Kamel A, AU - Abdel-Aziz,Lobna M, AU - Lashine,El-Sayed M, AU - Husseiny,Mohamed I, AU - Badawy,Rania H, Y1 - 2006/09/01/ PY - 2006/04/19/received PY - 2006/08/15/revised PY - 2006/08/15/accepted PY - 2006/9/5/pubmed PY - 2007/2/3/medline PY - 2006/9/5/entrez SP - 8675 EP - 82 JF - Bioorganic & medicinal chemistry JO - Bioorg. Med. Chem. VL - 14 IS - 24 N2 - A new series of 2-arylquinoline-4-carboxylic acid hydrazide-hydrazones was synthesized using an appropriate synthetic route. All the target compounds were evaluated for their in vitro antimicrobial activity against Staphylococcus aureus as an example for Gram-positive bacteria, Escherichia coli as an example for Gram-negative bacteria, and Candida albicans as a representative of fungi. The minimum inhibitory concentration (MIC) was determined for test compounds as well as for reference standards. Among the compounds tested, compounds having nitro substituents at the arylidene moiety showed the most potent antifungal as well as antibacterial activities against E. coli. Compound 23 displayed an antifungal activity comparable to that of nystatin. However, none of the compounds demonstrated any antibacterial activity against S. aureus. Hydrophobicity of the target compounds correlated weakly with their antibacterial and antifungal activities. The most potent compounds namely, 7, 18, 19, 22, and 23 were assessed for hemolytic toxicity and found to be non-hemolytic up to a concentration of 100mug/mL. In addition, the most potent compound (23) was evaluated for in vitro cytotoxic activity against various cancer cell lines. This compound was found to display no cytotoxic activity but rather it induces the proliferation rate of Hep-G2 cells. SN - 0968-0896 UR - https://www.unboundmedicine.com/medline/citation/16949294/Hydrazones_of_2_aryl_quinoline_4_carboxylic_acid_hydrazides:_synthesis_and_preliminary_evaluation_as_antimicrobial_agents_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0968-0896(06)00683-3 DB - PRIME DP - Unbound Medicine ER -