{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,1]],"date-time":"2026-10-01T08:44:04Z","timestamp":1790844244356,"version":"4.1.0"},"reference-count":28,"publisher":"MDPI AG","issue":"11","license":[{"start":{"date-parts":[[2011,11,9]],"date-time":"2011-11-09T00:00:00Z","timestamp":1320796800000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/3.0\/"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>A new series of 1,3-thiazole and benzo[d]thiazole derivatives 10\u201315 has been developed, characterized, and evaluated for in vitro antimicrobial activity at concentrations of 25\u2013200 \u03bcg\/mL against Gram+ve organisms such as methicillin-resistant Staphylococcus aureus (MRSA), Gram\u2013ve organisms such as Escherichia coli (E. coli), and the fungal strain Aspergillus niger (A. niger) by the cup plate method. Ofloxacin and ketoconazole (10 \u03bcg\/mL) were used as reference standards for antibacterial and antifungal activity, respectively. Compounds 11 and 12 showed notable antibacterial and antifungal activities at higher concentrations (125\u2013200 \u03bcg\/mL), whereas benzo[d]thiazole derivatives 13 and 14 were found to display significant antibacterial or antifungal activity (50\u201375 \u03bcg\/mL) against the Gram+ve, Gram\u2013ve bacteria, or fungal cells used in the present study. In addition, a correlation between calculated and determined partition coefficient (log P) was established which allows future development of compounds within this series to be carried out based on calculated log P values. Moreover, compounds 13 and 14 show that the optimum logarithm of partition coefficient (log P) should be around 4.<\/jats:p>","DOI":"10.3390\/molecules16119386","type":"journal-article","created":{"date-parts":[[2011,11,10]],"date-time":"2011-11-10T03:14:58Z","timestamp":1320894898000},"page":"9386-9396","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":42,"title":["Antimicrobial Prospect of Newly Synthesized 1,3-Thiazole Derivatives"],"prefix":"10.3390","volume":"16","author":[{"given":"Bassem","family":"Sadek","sequence":"first","affiliation":[{"name":"Department of Pharmacology and Therapeutics, College of Medicine and Health Sciences, UAE University, Al-Ain, P.O. Box 17666, United Arab Emirates"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Moawia Mohammad","family":"Al-Tabakha","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Sciences, College of Pharmacy, Al-Ain University of Science and Technology, P.O. Box 64141, Al-Ain, United Arab Emirates"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Khairi Mustafa Salem","family":"Fahelelbom","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Sciences, College of Pharmacy, Al-Ain University of Science and Technology, P.O. Box 64141, Al-Ain, United Arab Emirates"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2011,11,9]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"274","DOI":"10.1016\/S0966-842X(00)01762-5","article-title":"The bactericidal action of penicillin: New clues to an unsolved mystery","volume":"8","author":"Bayles","year":"2000","journal-title":"Trends Microbiol."},{"key":"ref_2","doi-asserted-by":"crossref","first-page":"1169","DOI":"10.1093\/clinids\/20.5.1169","article-title":"Bacteremia due to viridans streptococci that are highly resistant to penicillin: Increase among neutropenic patients with cancer","volume":"20","author":"Carratala","year":"1995","journal-title":"Clin. Infect. Dis."},{"key":"ref_3","doi-asserted-by":"crossref","first-page":"1025","DOI":"10.1001\/archinte.1992.00400170105020","article-title":"Results of the National Institute of Allergy and Infectious Diseases Collaborative Clinical Trial to test the predictive value of skin testing with major and minor penicillin derivatives in hospitalized adults","volume":"152","author":"Sogn","year":"1992","journal-title":"Arch. Intern. Med."},{"key":"ref_4","doi-asserted-by":"crossref","first-page":"671","DOI":"10.1093\/clinids\/20.3.671","article-title":"Diminished Activity of Ceftizoxime in Comparison to Cefotaxime and Ceftriaxone Against Streptococcus pneumoniae","volume":"20","author":"Haas","year":"1995","journal-title":"Clin. Infect. Dis."},{"key":"ref_5","doi-asserted-by":"crossref","first-page":"188","DOI":"10.1093\/clinids\/18.2.188","article-title":"Treatment Failure with Use of a Third-Generation Cephalosporin for Penicillin-Resistant Pneumococcal Meningitis: Case Report and Review","volume":"18","author":"John","year":"1994","journal-title":"Clin. Infect. Dis."},{"key":"ref_6","doi-asserted-by":"crossref","first-page":"141","DOI":"10.1056\/NEJM199001183220301","article-title":"A comparison of ceftriaxone and cefuroxime for the treatment of bacterial meningitis in children","volume":"322","author":"Schaad","year":"1990","journal-title":"N. Engl. J. Med."},{"key":"ref_7","doi-asserted-by":"crossref","first-page":"1009","DOI":"10.2174\/0929867043455530","article-title":"The development of the antitumour benzothiazole prodrug, Phortress, as a clinical candidate","volume":"11","author":"Bradshaw","year":"2004","journal-title":"Curr. Med. Chem."},{"key":"ref_8","doi-asserted-by":"crossref","first-page":"744","DOI":"10.1021\/jm011025r","article-title":"Antitumor benzothiazoles. 16. Synthesis and pharmaceutical properties of antitumor 2-(4-aminophenyl)benzothiazole amino acid prodrugs","volume":"45","author":"Hutchinson","year":"2002","journal-title":"J. Med. Chem."},{"key":"ref_9","doi-asserted-by":"crossref","first-page":"1446","DOI":"10.1021\/jm001104n","article-title":"Antitumor benzothiazoles. 14. Synthesis and in vitro biological properties of fluorinated 2- (4-aminophenyl)benzothiazoles","volume":"44","author":"Hutchinson","year":"2001","journal-title":"J. Med. Chem."},{"key":"ref_10","doi-asserted-by":"crossref","first-page":"4172","DOI":"10.1021\/jm990104o","article-title":"Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles","volume":"42","author":"Kashiyama","year":"1999","journal-title":"J. Med. Chem."},{"key":"ref_11","doi-asserted-by":"crossref","first-page":"1455","DOI":"10.1016\/j.bmcl.2004.01.023","article-title":"Synthesis and SAR of 2-arylbenzoxazoles, benzothiazoles and benzimidazoles as inhibitors of lysophosphatidic acid acyltransferase-beta","volume":"14","author":"Gong","year":"2004","journal-title":"Bioorg. Med. Chem. Lett."},{"key":"ref_12","doi-asserted-by":"crossref","first-page":"471","DOI":"10.1016\/S0960-894X(02)00930-7","article-title":"Antitumour benzothiazoles. Part 20: 3'-cyano and 3'-alkynyl-substituted 2-(4'-aminophenyl)benzothiazoles as new potent and selective analogues","volume":"13","author":"Hutchinson","year":"2003","journal-title":"Bioorg. Med. Chem. Lett."},{"key":"ref_13","first-page":"266","article-title":"Synthesis and HIV-1 Reverse Transcriptase Inhibitor Activity of Some 2,5,6-Substituted Benzoxazole, Benzimidazole, Benzothiazole and Oxazolo(4,5-b)pyridine Derivatives","volume":"53","author":"Akbay","year":"2003","journal-title":"Arzneimittel-Forsch."},{"key":"ref_14","doi-asserted-by":"crossref","first-page":"2587","DOI":"10.1016\/S0960-894X(03)00511-0","article-title":"Discovery of 2-amino-heteroarylbenzothiazole-6-anilides as potent p56(lck) inhibitors","volume":"13","author":"Das","year":"2003","journal-title":"Bioorg. Med. Chem. Lett."},{"key":"ref_15","doi-asserted-by":"crossref","first-page":"1425","DOI":"10.1002\/jps.2600831013","article-title":"Substituted 2-Benzothiazolamine as Sodium Flux Inhibitors\u2014Quantitative Structure-Activity-Relationships and Anticonvulsant Activity","volume":"83","author":"Hays","year":"1994","journal-title":"J. Pharm. Sci."},{"key":"ref_16","first-page":"295","article-title":"Synthesis and pharmacodynamic study of new derivatives of benzothiazole","volume":"35","author":"Foscolos","year":"1977","journal-title":"Ann. Pharm. Fr."},{"key":"ref_17","doi-asserted-by":"crossref","first-page":"1016","DOI":"10.1021\/jm00306a011","article-title":"Heterocyclic substituted ureas. II. Immunosuppressive and antiviral activity of benzothiazolyl- and benzoxazolylureas","volume":"12","author":"Paget","year":"1969","journal-title":"J. Med. Chem."},{"key":"ref_18","doi-asserted-by":"crossref","first-page":"4339","DOI":"10.3390\/molecules16064339","article-title":"Synthesis, Characterization, and Antimicrobial Evaluation of Oxadiazole Congener","volume":"16","author":"Sadek","year":"2011","journal-title":"Molecules"},{"key":"ref_19","doi-asserted-by":"crossref","first-page":"2895","DOI":"10.1016\/j.ejmech.2011.04.012","article-title":"Synthesis and antimicrobial activities of hexahydroimidazo[1,5-a]pyridinium bromides with varying benzyl substituents","volume":"46","author":"Ceyhan","year":"2011","journal-title":"Eur. J. Med. Chem."},{"key":"ref_20","doi-asserted-by":"crossref","first-page":"5032","DOI":"10.1039\/c1dt10250h","article-title":"The antimicrobial activity of inert oligonuclear polypyridylruthenium(ii) complexes against pathogenic bacteria, including MRSA","volume":"40","author":"Li","year":"2011","journal-title":"Dalton Trans."},{"key":"ref_21","first-page":"47","article-title":"Quantitative structure activity relationship studies for new antimicrobial N2- substituted phenazines","volume":"3","author":"Fahelelbom","year":"2009","journal-title":"Afr. J. Pharm. Pharmacol."},{"key":"ref_22","doi-asserted-by":"crossref","unstructured":"Podunavac-Kuzmanovi\u01071, S.O., Cvetkovi\u01071, D.D., and Barn, D.J. (2008). The effect of lipophilicity on the antibacterial activity of some 1-benzylbenzimidazole derivatives. J. Serb. Chem. Soc., 73, 967\u2013978.","DOI":"10.2298\/JSC0810967P"},{"key":"ref_23","unstructured":"Metzger, J.V. (1979). General Synthesis Methods for Thiazole and Thiazolium Salts, Interscience."},{"key":"ref_24","doi-asserted-by":"crossref","first-page":"3328","DOI":"10.1016\/j.bmcl.2005.05.077","article-title":"Synthesis and biological evaluation of benzothiazole derivatives as potent antitumor agents","volume":"15","author":"Yoshida","year":"2005","journal-title":"Bioorg. Med. Chem. Lett."},{"key":"ref_25","doi-asserted-by":"crossref","first-page":"2289","DOI":"10.1016\/0040-4020(68)88130-X","article-title":"Demethylation of aryl methyl ethers by boron tribromide","volume":"24","author":"Mcomie","year":"1969","journal-title":"Tetrahedron"},{"key":"ref_26","doi-asserted-by":"crossref","first-page":"139","DOI":"10.3390\/12020139","article-title":"Antibacterial activity of long-chain fatty alcohols against Staphylococcus aureus","volume":"12","author":"Togashi","year":"2007","journal-title":"Molecules"},{"key":"ref_27","doi-asserted-by":"crossref","first-page":"11151","DOI":"10.1021\/jf8020859","article-title":"Naturally occurring phenolic antibacterial compounds show effectiveness against oral bacteria by a quantitative structure-activity relationship study","volume":"56","author":"Greenberg","year":"2008","journal-title":"J. Agric. Food Chem."},{"key":"ref_28","unstructured":"Barry, A.L. (1976). The Antimicrobial Susceptibility Test: Principle and Practices, Lea and Febiger. [Biol. Abstr., 64, 25183]."}],"container-title":["Molecules"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/www.mdpi.com\/1420-3049\/16\/11\/9386\/pdf","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2025,10,11]],"date-time":"2025-10-11T21:57:58Z","timestamp":1760219878000},"score":1,"resource":{"primary":{"URL":"https:\/\/www.mdpi.com\/1420-3049\/16\/11\/9386"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2011,11,9]]},"references-count":28,"journal-issue":{"issue":"11","published-online":{"date-parts":[[2011,11]]}},"alternative-id":["molecules16119386"],"URL":"https:\/\/doi.org\/10.3390\/molecules16119386","relation":{},"ISSN":["1420-3049"],"issn-type":[{"value":"1420-3049","type":"electronic"}],"subject":[],"published":{"date-parts":[[2011,11,9]]}}}