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Synthesis and anti Methicillin resistant Staphylococcus aureus activity of substituted chalcones alone and in combination with non-beta-lactam antibiotics.
Bioorg Med Chem Lett. 2012 Jul 15; 22(14):4555-60.BM

Abstract

A total of 30 chalcone analogues was synthesized via a base catalyzed Claisen Schmidt condensation and screened for their in vitro antibacterial activity against Methicillin-sensitive Staphylococcus aureus (MSSA) and Methicillin-resistant Staphylococcus aureus (MRSA) alone or in combination with non beta-lactam antibiotics namely ciprofloxacin, chloramphenicol, erythromycin, vancomycin, doxycycline and gentamicin. In the checkerboard technique, fractional inhibitory concentration indices (FICI) show that the following combinations like ciprofloxacin with 25 (4'-bromo-2-hydroxychalcone); doxycycline with 21 (4-hydroxychalcone); doxycycline with 25; and doxycycline with 4 (2',2-dihydroxychalcone) were synergistic against MRSA. In term SAR study, the relationship between chalcone structure and their antibacterial activity against S. aureus and synergy with tested antibiotics were discussed. Possible mechanisms for antibacterial activity of chalcones alone as well as the synergistic effect in combinations were proposed by molecular modeling studies, respectively. Combinations of chalcones with conventional antibiotics could be an effective alternative in the treatment of infection caused by MRSA.

Authors+Show Affiliations

Department of Medicinal Chemistry, School of Pharmacy, University of Medicine and Pharmacy at Ho Chi Minh City, 41 Dinh Tien Hoang, Dist. 1, Ho Chi Minh City, Viet Nam. tranthanhdao@uphcm.edu.vnNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

22727643

Citation

Tran, Thanh-Dao, et al. "Synthesis and Anti Methicillin Resistant Staphylococcus Aureus Activity of Substituted Chalcones Alone and in Combination With Non-beta-lactam Antibiotics." Bioorganic & Medicinal Chemistry Letters, vol. 22, no. 14, 2012, pp. 4555-60.
Tran TD, Do TH, Tran NC, et al. Synthesis and anti Methicillin resistant Staphylococcus aureus activity of substituted chalcones alone and in combination with non-beta-lactam antibiotics. Bioorg Med Chem Lett. 2012;22(14):4555-60.
Tran, T. D., Do, T. H., Tran, N. C., Ngo, T. D., Huynh, T. N., Tran, C. D., & Thai, K. M. (2012). Synthesis and anti Methicillin resistant Staphylococcus aureus activity of substituted chalcones alone and in combination with non-beta-lactam antibiotics. Bioorganic & Medicinal Chemistry Letters, 22(14), 4555-60. https://doi.org/10.1016/j.bmcl.2012.05.112
Tran TD, et al. Synthesis and Anti Methicillin Resistant Staphylococcus Aureus Activity of Substituted Chalcones Alone and in Combination With Non-beta-lactam Antibiotics. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4555-60. PubMed PMID: 22727643.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis and anti Methicillin resistant Staphylococcus aureus activity of substituted chalcones alone and in combination with non-beta-lactam antibiotics. AU - Tran,Thanh-Dao, AU - Do,Tuong-Ha, AU - Tran,Ngoc-Chau, AU - Ngo,Trieu-Du, AU - Huynh,Thi-Ngoc-Phuong, AU - Tran,Cat-Dong, AU - Thai,Khac-Minh, Y1 - 2012/06/06/ PY - 2012/04/09/received PY - 2012/05/23/revised PY - 2012/05/30/accepted PY - 2012/6/26/entrez PY - 2012/6/26/pubmed PY - 2013/1/5/medline SP - 4555 EP - 60 JF - Bioorganic & medicinal chemistry letters JO - Bioorg. Med. Chem. Lett. VL - 22 IS - 14 N2 - A total of 30 chalcone analogues was synthesized via a base catalyzed Claisen Schmidt condensation and screened for their in vitro antibacterial activity against Methicillin-sensitive Staphylococcus aureus (MSSA) and Methicillin-resistant Staphylococcus aureus (MRSA) alone or in combination with non beta-lactam antibiotics namely ciprofloxacin, chloramphenicol, erythromycin, vancomycin, doxycycline and gentamicin. In the checkerboard technique, fractional inhibitory concentration indices (FICI) show that the following combinations like ciprofloxacin with 25 (4'-bromo-2-hydroxychalcone); doxycycline with 21 (4-hydroxychalcone); doxycycline with 25; and doxycycline with 4 (2',2-dihydroxychalcone) were synergistic against MRSA. In term SAR study, the relationship between chalcone structure and their antibacterial activity against S. aureus and synergy with tested antibiotics were discussed. Possible mechanisms for antibacterial activity of chalcones alone as well as the synergistic effect in combinations were proposed by molecular modeling studies, respectively. Combinations of chalcones with conventional antibiotics could be an effective alternative in the treatment of infection caused by MRSA. SN - 1464-3405 UR - https://www.unboundmedicine.com/medline/citation/22727643/Synthesis_and_anti_Methicillin_resistant_Staphylococcus_aureus_activity_of_substituted_chalcones_alone_and_in_combination_with_non_beta_lactam_antibiotics_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960-894X(12)00724-X DB - PRIME DP - Unbound Medicine ER -