Synthesis and Biological Activity of Some New Benzthiazoloazetidin-2-ones and Benzthiazolothizoiidin-4-ones, IV

Hassan, Kh. M.; Mahmoud, A. M.; Sherief, H. A. El

doi:10.1515/znb-1978-0912

Cited by 10 publications

(5 citation statements)

References 10 publications

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“…The mass spectrum164 of 4,4-dimethyl-2-thiono-5thiazolidinone (294) gave the molecular ion peaks at 161 (M+, 100), 133 (M+ -CO, 57) and 100 (M+ -CO -SH, Other workers have also reported the assignment of the various molecular ion peaks in the mass spectra of 4-thiazolidinone149 and the mesoionic derivatives270 of 4-thiazolidinone and 5-thiazolidinone. studied against pentylenetetrazol-induced sei-zures75,85-92,94 in albino mice of either sex at a dose of 100 mg/kg.…”

Section: Mass Spectroscopymentioning

confidence: 98%

Chemistry and biological activity of thiazolidinones

Singh¹,

Parmar²,

Raman³

et al. 1981

Chem. Rev.

398

183

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Section: Mass Spectroscopymentioning

confidence: 98%

Chemistry and biological activity of thiazolidinones

Singh¹,

Parmar²,

Raman³

et al. 1981

Chem. Rev.

398

183

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“…All the chemicals used for the synthesis were purchased from Aldrich, Dorset (UK). The compound, 2-aminobenzothiazole 1 was prepared by the reported method [14]. For COX catalysed prostaglandin…”

Section: Chemicals and Apparatusmentioning

confidence: 99%

“…Various substituted benzothiazoles are known to possess a wide range of pharmacological activities such as antitumour [12], antimicrobial [13,14], anthelmintic [15], analgesic [16], anti-inflammatory [17] and anticonvulsant [18] activities. Similarly, the ß-lactam nucleus is considered a general lead structure for the design and synthesis of not only new antibacterial products, but also for new inhibitors of enzymes like ß-lactamases [19], human leukocyte elastase [20], cholesterol absorption inhibitors [21] and human cytomegalovirus protease [22].…”

Section: Introductionmentioning

confidence: 99%

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Synthesis and Anti-inflammatory Activity of Alkyl/Arylidene-2-aminobenzothiazoles and 1-Benzothiazol-2-yl-3-chloro-4-substituted-azetidin-2-ones

Khedekar¹,

Bahekar

Chopade

et al. 2011

Arzneimittelforschung

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Ten new derivatives of 1-benzothiazol-2-yl-3-chloro-4-substituted-azetidin-2-ones (3a-j) were synthesized using various Schiff bases (alkyl/arylidene-2-aminobenzothiazoles; 2a-j), which in turn were prepared starting from 2-aminobenzothiazole (1). All the synthesised compounds were characterised by elemental analyses and spectral (IR, 1H-NMR, 13C-NMR and EI-MS) data. The title compounds 2a-j and 3a-j were screened in vivo using carrageenan-induced rat paw edema model. All the test compounds showed anti-inflammatory activity when tested in vivo. In general, compounds 3a-j were found to be more potent compared to compounds 2a-j. Among the compounds tested, compound 2g in the alkyl/arylidene-2-aminobenzothiazoles series and compound 3 g in the 1-benzothiazol-2-yl-3-chloro-4-substituted-azetidin-2-ones series were found to be the most potent. All the test compounds were also evaluated to check the gastric ulcer incidence. In gastric ulceration studies, all the test compounds were generally found to be safe at the 100 mg/kg dose level. Furthermore the most potent compounds 2 g and 3 g from each series were screened in vitro for inhibition of both COX-2 and COX-1 catalysed prostaglandin biosynthesis (radiochemical assay). Like most of the commercially available non-steroidal anti-inflammatory drugs (NSAIDs), in the in vitro study, compounds 2 g and 3 g showed anti-inflammatory activity by blocking the metabolism of arachidonic acid to prostaglandin via the cyclooxygenase pathways. In general, in the vitro assay, test compounds 2 g and 3 g were found to be more active after 15 min pre-incubation with the enzyme. Compound 3 g was found to be more COX-2 selective, while compound 2 g was found to be equally COX-2 and COX-1 selective.

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“…anticonvulsant, 14,15 bronchodilator, 16,17 anti-inflammatory, [18][19][20] antimalarial, 21 antituberculous, 22 anti-HIV, 23 narcotic antagonist, 24 anti-tumor, 25 tyrosinekinase inhibitor, 26 adenosine antagonist, 27 antimicrobial, 28 etc. Similarly various substituted benzothiazoles are known to possess varied pharmacological activities like anti-tumor, 29 antimicrobials, 30,31 anthelmintic, 32 analgesic, 33 antiinflammatory, 34 anticonvulsant, 35,36 and CVS agents. 37 The simultaneous use of several drugs to treat inflammatory conditions, associated with some microbial infections may cause health problems especially in patients with impaired liver or kidney functions.…”

Section: Introductionmentioning

confidence: 99%

Studies on some biologically active substituted 4(3H)-quinazolinones. Part 1. Synthesis, characterization and anti-inflammatory-antimicrobial activity of 6,8-disubstituted 2-phenyl-3-[substituted-benzothiazol-2-yl]-4(3H)-quinazolinones

Laddha¹,

Wadodkar²,

Meghal³

2006

Arkivoc

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Two series of 6,8-disubstituted 2-phenyl-3-[substituted benzothiazol-2-yl]-4(3H)-quinazolinones [3a-m and 4a-m] have been synthesized and characterized by elemental analysis and spectral data. The anti-inflammatory activity of the title compounds (3a-m and 4a-m) was evaluated and the most active compounds were evaluated for COX-1 and COX-2 inhibitory activity and ulcerogenic activity. All the test compounds were administered orally/intraperitoneally at a dose 50 mg/Kg body weight and percentage inhibitions were determined. Further more all the compounds were also tested against Gram negative, Gram positive bacteria and fungi. Among the compounds tested in this study, compounds 2-phenyl-3-(4-methoxybenzothiazol-2-yl)-4(3H)-quinazolinone (3e), 2-phenyl-3-(5-methylbenzothiazol-2-yl)-4(3H)-quinazolinone (3f) and 2-phenyl-3-(4-6-dimethylbenzothiazol-2-yl)-4(3H)-quinazolinone (3l) showed most prominent anti-inflammatory activity with low gastric ulceration incidence compare to reference standard Indomethacin. Further compounds, 3e, 3f and 3l revealed superior inhibitory profile against COX-2 enzyme, when compared with reference standard Indomethacin. Among all the compounds, compounds 4g and 4j posses a broad spectrum of antibacterial activities against both Gram positive and Gram negative bacteria but insignificant antifungal and anti-inflammatory activity.Keywords: 2-Phenyl-3-[substituted-benzothiazol-2-yl]-4(3H)-quinazolinone, 6,8-dibromo, 2-phenyl-3-[substituted-benzothiazol-2-yl]-4(3H)-quinazolinone, anti-inflammatory, COX-1 and 2 inhibitory activity, antimicrobials

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Synthesis and Biological Activity of Some New Benzthiazoloazetidin-2-ones and Benzthiazolothizoiidin-4-ones, IV

Cited by 10 publications

References 10 publications

Chemistry and biological activity of thiazolidinones

Chemistry and biological activity of thiazolidinones

Synthesis and Anti-inflammatory Activity of Alkyl/Arylidene-2-aminobenzothiazoles and 1-Benzothiazol-2-yl-3-chloro-4-substituted-azetidin-2-ones

Studies on some biologically active substituted 4(3H)-quinazolinones. Part 1. Synthesis, characterization and anti-inflammatory-antimicrobial activity of 6,8-disubstituted 2-phenyl-3-[substituted-benzothiazol-2-yl]-4(3H)-quinazolinones

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