Summary 4-Carbethoxymethyl-2-[(chloroacetyl / ?-chloropropionyl / ?-bromobutyryl / ?-chloro-(?-phenylacetyl)amino]thiazoles (I?IV) were synthesized by reacting 4-carbethoxymethyl-2-ami-nothiazole with chloroacetyl chloride, ?-chloropropionyl chloride, ?-bromobutyryl bromide and ?-chloro-a-phenylacetyl chloride, respectively. Furthermore, I-IV were refluxed with ammonium thiocyanate to give 2-[(4-carbethoxymethylthiazol-2-yl)imino]-4-thiazolidinones (V- VIII). V was refluxed with various aromatic aldehydes to give 5-arylidene-2-[(4-carbethoxyme-thylthiazol-2-yl)imino]-4-thiazolidinones (IX-XIV). The structures of synthesized compounds were confirmed by elemental analyses, hydrolysis, UV, IR, 1H-NMR and EI mass spectral data. The antimicrobial activities of the compounds were assessed by microbroth dilution technique using Mueller-Hinton broth and Mueller-Hinton Agar. In this study, Staphylococcus aureus ATCC 6538, Staphylococcus epidermidis ATCC 12228, Escherichia coli ATCC 8739, Klebsiella pneumoniae ATCC 4352, Pseudomonas aeruginosa ATCC 1539, Salmonella typhi, Shigella flexneri, Proteus mirabilis and Candida albicans ATCC 10231 were used as test microorganisms. Among the tested compounds, XI and XIV showed activity against S. aureus (MIC: 78 ?g/ml, 1.6 ?g/ml), whereas compound V had an activity against S. flexneri (MIC: 39 ?g/ml) and compound I against C. albicans (MIC: 125 (|?g/ml). Compounds I, IV- XIV were also evaluated for antituberculosis activity against Mycobacterium tuberculosis H37Rv using the BACTEC 460 radiometric system and BACTEC 12B medium. Only compounds I and XIV showed 86% and 67% inhibition in the primary screen.

imino--4-thiazolidinon-5-ylidene]-5-substituted/nonsubstituted 1H-Indole-2-ones and Investigation of Their Structure-Activity Relationships. -Several novel promising compounds such as (III) for the title pharmacological activities are synthesized. The activity of (IIIc) is close to that of cefuroxime sodium against Staphylococcus epidermidis ATCC 12228. The preparation of the starting materials (I) is also given. -(ALTINTAS*, H.; ATES, O.; UYDES-DOGAN, B. S.; ALP, F. I.; KALELI, D.; OEZDEMIR, O.; BIRTEKSOEZ, S.; OETUEK, G.; SATANA, D.; UZUN, M.; Arzneim.-Forsch. 56 (2006) 3, 239-248; Dep. Pharm. Chem., Fac. Pharm., Univ. Istanbul, Beyazit, TR-34452 Istanbul, Turk.; Eng.) -K. Schneider 30-137

imino]-4-thiazolidinones. -Some of the title Mannich bases (VI) (13 examples), e.g. (VIc), (VId) and (VIe), are found to exhibit significant activity against S.aureus ATCC 6538. -(ALTINTAS*, H.; ATES, O.; KOCABALKANLI, A.; BIRTEKSOEZ, S.; OETUEK, G.; Indian J. Chem., Sect. B: Org. Chem. Incl. Med. Chem. 44 (2005) 3, 585-590; Dep. Pharm. Chem., Fac. Pharm., Univ. Istanbul, Beyazit, TR-34452 Istanbul, Turk.; Eng.) -A. Forchert 28-137

[2-[2-(N, N-Disubstituted thiocarbamoyl-sulfanyl)acylamino ]thiazol-4-yl]acetic acid ethyl esters (3a-x) were synthesized by the reaction of potassium salts of N, N-disubstituted dithiocarbamoic acids with [2-(2-chloroalkanoyl)amino-thiazol-4-yl]acetic acid ethyl esters. The structures of the synthesized compounds were confirmed by elemental analyses, UV, IR, (1)H-NMR, and EI mass spectral data. The antimicrobial activities of all the compounds were investigated by microbroth dilution technique using Mueller-Hinton broth and Mueller-Hinton agar. In this study, Staphylococcus aureus ATCC 6538, Staphylococcus epidermidis ATCC 12228, Escherichia coli ATCC 8739, Klebsiella pneumoniae ATCC 4352, Pseudomonas aeruginosa AT CC 1539, Salmonella typhi, Shigella flexneri, Proteus mirabilis ATCC 14153 and Candida albicans ATCC10231 were used as test microorganisms. Among the tested compounds 3a, d, e, f, h, k, w activity against S. epidermidis ATCC 12228 (MIC: 156 mg/L, 78 mg/L, 62.5 mg/L, 78 mg/L, 62.5 mg/L, 312 mg/L, 250 mg/L, respectively), compound 3d had some activity against S. aureus ATCC 6538 (MIC: 156 mg/L) and C. albicans ATCC 10231(MIC: 156 mg/L). Compounds 3l, 3x also evaluated for antituberculosis activity against Mycobacterium tuberculosis H37Rv using the BACTEC 460 radiometric system and BACTEC 12B medium. The preliminary results indicated that all of the tested compounds were inactive against the test organism.

Summary In the present study, 20 new compounds having 3-[2-(5-aryl-1,3,4-oxadiazol-2-yl) imino-4-thiazolidinon-5-ylidene]-5-substituted/nonsubstituted 1H-indole-2-one (I?XII) and 3-[2-(4-carbethoxymethylthiazol-2-yl)imino-4-thiazolidinon-5-ylidene]-5-substituted/nonsubstituted 1H-indole-2-one (XIII-XX) systems were synthesized. The structures were confirmed by spectral methods (UV, IR, 1H-NMR, 13C-NMR, 13C-DEPT (135), electron impact mass spectrometry) and elemental analysis. All compounds were tested for in vitro antimicrobial activity against Staphylococcus aureus ATCC 6538, Staphylococcus epidermidis ATCC 12228, Escherichia coli ATCC 8739, Klebsiella pneumoniae ATCC 4352, Pseudomonas aeruginosa ATCC 1539, Salmonella typhi, Shigella flexneri, Proteus mirabilis ATCC 14153, Candida albicans ATCC 10231, Microsporum gypseum (NCPF-580), Microsporum canis, Trichophyton mentagrophytes and Trichophyton rubrum and some of them were found to be active. Especially, compound I was more active than cefuroxime sodium (CAS 56238-63-2) which was used as a standard, and the activity of compound XII was close to that of cefuroxime sodium against Staphylococcus epidermidis ATCC 12228. Primary screening for antituberculous activity was conducted at 6.25 ?g/ml against Mycobacterium tuberculosis H37Rv in BACTEC 12B medium using the BACTEC 460 radiometric system. The anticonvulsant activities of selected prototoype compounds (I, IV-VI, VIII, XI, XIII, XVI-XVIII) administered at doses of 50-200 mg/kg (i.p.) were evaluated using the pentetrazol test (PTZ) in mice.