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Synthesis, antimicrobial, antiquorum-sensing, antitumor and cytotoxic activities of new series of fused [1,3,4]thiadiazoles.
Eur J Med Chem. 2013 May; 63:185-95.EJ

Abstract

New series of [1,3,4]thiadiazolo[3,2-a]pyrimidines, benzo[h][1,3,4]thiadiazolo[2,3-b]quinazolines, benzothiadiazolotriazocine, and imidazo[2,1-b][1,3,4]thiadiazoles have been synthesized and characterized by analytical and spectrometrical methods (IR, MS, (1)H and (13)C NMR). Twenty of the synthesized compounds were screened for antibacterial activity against Escherichia coli, Staphylococcus aureus and Bacillus cereus. They were found to be either moderately active, slightly active or inactive against the tested microorganisms. The antifungal activity of these compounds were also tested against Candida albicans, Aspergillus fumigatus 293 and Aspergillus flavus 3375. Compounds 3g, h showed potent antifungal activity against C. albicans. In addition, the same compounds were tested for antiquorum-sensing activity against Chromobacterium violacium ATCC 12472, where compounds 3b,c, 3f-h, 6b-d, 9, 10 and 12 demonstrated acceptable activity. Compounds 3d, 9 and 10 were screened for antitumor activity at National Cancer Institute, USA. The in vitro cytotoxic activity of eighteen of the synthesized compounds was studied by brine shrimp lethality bioassay, and results indicated that compounds 6c, 13, 3h, 6d and 3d have the highest cytotoxic activity.

Authors+Show Affiliations

Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt. dr.nadiaelgohary@yahoo.comNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

23474904

Citation

El-Gohary, Nadia S., and Mona I. Shaaban. "Synthesis, Antimicrobial, Antiquorum-sensing, Antitumor and Cytotoxic Activities of New Series of Fused [1,3,4]thiadiazoles." European Journal of Medicinal Chemistry, vol. 63, 2013, pp. 185-95.
El-Gohary NS, Shaaban MI. Synthesis, antimicrobial, antiquorum-sensing, antitumor and cytotoxic activities of new series of fused [1,3,4]thiadiazoles. Eur J Med Chem. 2013;63:185-95.
El-Gohary, N. S., & Shaaban, M. I. (2013). Synthesis, antimicrobial, antiquorum-sensing, antitumor and cytotoxic activities of new series of fused [1,3,4]thiadiazoles. European Journal of Medicinal Chemistry, 63, 185-95. https://doi.org/10.1016/j.ejmech.2013.02.010
El-Gohary NS, Shaaban MI. Synthesis, Antimicrobial, Antiquorum-sensing, Antitumor and Cytotoxic Activities of New Series of Fused [1,3,4]thiadiazoles. Eur J Med Chem. 2013;63:185-95. PubMed PMID: 23474904.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis, antimicrobial, antiquorum-sensing, antitumor and cytotoxic activities of new series of fused [1,3,4]thiadiazoles. AU - El-Gohary,Nadia S, AU - Shaaban,Mona I, Y1 - 2013/02/18/ PY - 2012/10/01/received PY - 2013/02/04/revised PY - 2013/02/09/accepted PY - 2013/3/12/entrez PY - 2013/3/12/pubmed PY - 2013/12/16/medline SP - 185 EP - 95 JF - European journal of medicinal chemistry JO - Eur J Med Chem VL - 63 N2 - New series of [1,3,4]thiadiazolo[3,2-a]pyrimidines, benzo[h][1,3,4]thiadiazolo[2,3-b]quinazolines, benzothiadiazolotriazocine, and imidazo[2,1-b][1,3,4]thiadiazoles have been synthesized and characterized by analytical and spectrometrical methods (IR, MS, (1)H and (13)C NMR). Twenty of the synthesized compounds were screened for antibacterial activity against Escherichia coli, Staphylococcus aureus and Bacillus cereus. They were found to be either moderately active, slightly active or inactive against the tested microorganisms. The antifungal activity of these compounds were also tested against Candida albicans, Aspergillus fumigatus 293 and Aspergillus flavus 3375. Compounds 3g, h showed potent antifungal activity against C. albicans. In addition, the same compounds were tested for antiquorum-sensing activity against Chromobacterium violacium ATCC 12472, where compounds 3b,c, 3f-h, 6b-d, 9, 10 and 12 demonstrated acceptable activity. Compounds 3d, 9 and 10 were screened for antitumor activity at National Cancer Institute, USA. The in vitro cytotoxic activity of eighteen of the synthesized compounds was studied by brine shrimp lethality bioassay, and results indicated that compounds 6c, 13, 3h, 6d and 3d have the highest cytotoxic activity. SN - 1768-3254 UR - https://www.unboundmedicine.com/medline/citation/23474904/Synthesis_antimicrobial_antiquorum_sensing_antitumor_and_cytotoxic_activities_of_new_series_of_fused_[134]thiadiazoles_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0223-5234(13)00096-2 DB - PRIME DP - Unbound Medicine ER -