title: Synthesis, antimicrobial, antiquorum-sensing, antitumor and cytotoxic activities of new series of fused [1,3,4]thiadiazoles.
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.affiliation: Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt. dr.nadiaelgohary@yahoo.com
authors.forename: Nadia S
authors.initials: NS
authors.lastname: El-Gohary
authors.forename: Mona I
authors.initials: MI
authors.lastname: Shaaban
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001156:Artemia / Q000187:drug effects / Q000254:growth & development; D002176:Candida albicans / Q000187:drug effects; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D004926:Escherichia coli / Q000187:drug effects; D045325:HCT116 Cells; D018922:HL-60 Cells; D019073:HT29 Cells; D006801:Humans; D020014:K562 Cells; D007928:Lethal Dose 50; D061986:MCF-7 Cells; D008826:Microbial Sensitivity Tests; D008956:Models, Chemical; D015394:Molecular Structure; D053038:Quorum Sensing / Q000187:drug effects; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D000970:Antineoplastic Agents; D013830:Thiadiazoles