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At least 451 records · Page 25Linked to original sources
PubMed2005

In vitro activity of 2-cyclohexylidenhydrazo-4-phenyl-thiazole compared with those of amphotericin B and fluconazole against clinical isolates of Candida spp. and fluconazole-resistant Candida albicans.

OBJECTIVES: The aim of this study was to investigate the in vitro antifungal activity of an isothiosemicarbazone cyclic analogue against isolates of Candida spp. including fluconazole-resistant Candida albicans. METHODS: We investigated the activity of 2-cyclohexylidenhydrazo-4-phenyl-thiazole (EM-01D2) against 114 clinical isolates of Candida spp., representing five different species, by microdilution, according to the NCCLS method 27-A. The activity against C. albicans biofilms was also investigated. Toxicity in vitro was evaluated by MTT reduction assay. RESULTS: EM-01D2 demonstrated low toxicity, broad spectrum, fungicidal activity and was active against C. albicans and Candida krusei at concentrations lower than those shown by amphotericin B and fluconazole (P < 0.05). It maintained potent in vitro activity against fluconazole-resistant C. albicans isolates. Fungicidal activity occurred at concentrations 1-2 doubling dilutions greater than the corresponding MICs, and time-kill analysis indicated that a 99.9% loss of C. albicans viability occurred after 6 h of incubation in the presence of EM-01D2 at concentrations equal to four times the MIC. EM-01D2 was also active in inhibiting the growth of C. albicans ATCC 10231 biofilms, even though such inhibition occurred at concentrations higher than the MICs determined under planktonic growth conditions. However, when C. albicans biofilms were pre-exposed to subinhibitory concentrations of EM-01D2, a reduction of MIC50 of amphotericin B was observed. CONCLUSIONS: Based on these results, EM-01D2 could represent a template for the development of novel fungicidal agents.

Amphotericin B↗
PubMed2002

4-Methyl-2-[N-(3,4-methylenedioxybenzylidene)hydrazino]thiazole and its reduction product, 4-methyl-2-[N-(3,4-methylenedioxybenzylidene)hydrazono]-4,5-dihydrothiazole.

The crystal structures of 4-methyl-2-[N-(3,4-methylenedioxybenzylidene)hydrazino]thiazole, C(12)H(11)N(3)O(2)S, and its reduction product 4-methyl-2-[N-(3,4-methylenedioxybenzylidene)hydrazono]-4,5-dihydrothiazole, C(12)H(13)N(3)O(2)S, have been determined and compared. In the reduction product, the tautomer observed bears an H atom on the exocyclic N atom. Both compounds form hydrogen-bonded dimers over centers of inversion.

Journal Article↗
PubMed2003

2,5-di-2-thienylthiazolo[4,5-d]thiazole.

The molecules of the title compound, C(12)H(6)N(2)S(4), lie on centres of symmetry. The thiophene and thiazole rings are almost planar and their planes make a dihedral angle of 1.68 (8) degrees. In the crystal structure, there is a relatively short intermolecular S...S contact distance of 3.5786 (9) A.

Journal Article↗
PubMed2003

4-(4-bromophenyl)-2-methyl-1,3-thiazole.

In the structure of the title compound, C(10)H(8)BrNS, the dihedral angles between the planes of the thiazole and aryl rings, viz. 4.2 (6) and 7.5 (6) degrees for the two independent molecules, are consistent with insignificant molecular perturbation by the weak intermolecular contacts. The molecules are close to being related by a non-crystallographic inversion centre, with C-H.pi and pi-pi intermolecular interactions observed.

Journal Article↗
PubMed2003

(2,2'-Diamino-4,4'-bi-1,3-thiazole-kappa2N3,N3')(oxydiacetato-kappa3O,O',O")copper(II) monohydrate.

The title compound, [Cu(C(4)H(4)O(5))(C(6)H(6)N(4)S(2))].H(2)O, displays a square-pyramidal coordination geometry. The tridentate oxydiacetate dianion chelates the Cu(II) atom in the facial mode. The large difference [0.487 (4) A] between the longest Cu-O distance in the basal plane and that in the apical direction correlates with the small displacement of the Cu(II) atom [0.0576 (13) A] from the basal plane towards the apex of the square pyramid. The intermolecular hydrogen-bonding network results in a closely overlapped arrangement of the coordination basal plane and the thiazole ring of a neighboring molecule.

Journal Article↗
PubMed2005

catena-Poly[[cyclo-tetra-mu-chlorotetracopper(I)]-bis{mu-3-[(2-morpholino-4-oxo-4,5-dihydro-1,3-thiazol-5-ylidene)methylphenoxy]propene}-2kappaN,1'eta2;1eta2,2'kappaN].

Crystals of a new copper(I) complex of composition [Cu4Cl4(C17H18N2O3S)2]n have been obtained by alternating-current electrochemical synthesis. In the crystal structure, the Cu and Cl atoms form a chair-like Cu4Cl4 cyclic fragment. The organic ligand acts as a bridge, being connected via the C=C bond of the allyl group to a Cu atom from one inorganic cycle and via the N atom of the thiazole ring to a Cu atom of another copper-chloride fragment. The geometry of the pi center indicates that the Cu-(C=C) interaction is moderately effective.

Journal Article↗
PubMed1993

Functional differences of dyes in inducing respiratory immunogenicity by azo-, thiazole-, quinoline-, reactive-, and naphthol-dye-inactivated Sendai viruses.

The prophylactic effects by mouse nasal inoculation of 31 kinds of organic dye-inactivated Sendai viruses were investigated by contact exposure experiment that used mouse nasally infected with 10(5.8) EID50, immunofluorescent examination of the entire respiratory tract, and check of rise of serum HI titer postexposure. The relative merits of the dye-structures for inciting nasal immunogenicity were determined. Of 14 azo-dye-inactivated vaccines, only azo blue- and amido black 10B treated ones brought about nearly complete protection, while the other 5 dye-groups provided partial protection and the remaining 7 dye-groups the least protection. Of 6 thiazole dye-vaccines, primuline-, thioflavine S-, and thioflavine T-vaccines induced complete or almost complete protection, and the others moderate or the least protection. With 3 quinoline-vaccines, both pinacyanol- and quinaldine red-inactivated ones provided complete protection, but not with quinoline blue-vaccine. Of 4 reactive dye-vaccines, both cibacron brilliant yellow 3G-P- and reactive blue 4-treated ones brought about nearly complete protection, but the remaining 2 vaccines induced regional infection. Nevertheless, all 4 naphthol group (AS, AS-BS, AS-BI, and AS-MX)-treated vaccines yielded complete or almost complete protection. The thirteen most effective vaccine groups suppressed marked rise of high or low serum HI titers developed through nasal vaccination postexposure. In short, specified dyestuffs having a great affinity for cellulosic fibers, evidently incited mucosal immunogenicity, probably by major union of the dyes to viral core ribose.

Animals↗
PubMed1969

The pharmacology of fenclozic acid (2-(4-chlorophenyl)-thiazol-4-ylacetic acid; I.C.I. 54,450; 'Myalex'); a new compound with anti-inflammatory, analgesic and antipyretic activityl.

1. Fenclozic acid (2-(4-chlorophenyl)thiazol-4-ylacetic acid; I.C.I. 54,450; "Myalex") is one representative of a new class of compounds with antiinflammatory, analgesic and antipyretic properties as evidenced by its activity in a variety of tests in rats, mice and guinea-pigs.2. In tests of short duration the potency of fenclozic acid is similar to that of phenylbutazone.3. In tests of longer duration fenclozic acid is more potent than phenylbutazone.4. The activity of fenclozic acid is not mediated by stimulation of the adrenals and the compound is devoid of corticosteroid-like activity.

Adrenal Cortex Hormones↗
PubMed2003

In vitro and in vivo activities of novel 2-(thiazol-2-ylthio)-1beta-methylcarbapenems with potent activities against multiresistant gram-positive bacteria.

SM-197436, SM-232721, and SM-232724 are new 1beta-methylcarbapenems with a unique 4-substituted thiazol-2-ylthio moiety at the C-2 side chain. In agar dilution susceptibility testing these novel carbapenems were active against methicillin-resistant Staphylococcus aureus (MRSA) and Staphylococcus epidermidis (MRSE) with a MIC(90) of </=4 micro g/ml. Furthermore, SM-232724 showed strong bactericidal activity against MRSA, in contrast to linezolid, which was bacteriostatic up to four times the MIC. SM-232724 showed good therapeutic efficacy comparable to those of vancomycin and linezolid against systemic infections of MRSA in cyclophosphamide-treated mice. The MICs of SM-197436, SM-232721, and SM-232724 for streptococci, including penicillin-intermediate and penicillin-resistant Streptococcus pneumoniae strains, ranged from </=0.063 to 0.5 micro g/ml. These drugs were the most active beta-lactams tested against Enterococcus faecium, and the MIC(90) s for ampicillin-resistant E. faecium ranged between 8 and 16 micro g/ml, which were slightly higher than the value for linezolid. However, time-kill assays revealed the superior bactericidal activity of SM-232724 compared to those of quinupristin-dalfopristin and linezolid against an E. faecium strain with a 4-log reduction in CFU at four times the MIC after 24 h of exposure to antibiotics. In addition, SM-232724 significantly reduced the numbers of bacteria in a murine abscess model with the E. faecium strain: its efficacy was superior to that of linezolid, although the MICs (2 micro g/ml) of these two agents are the same. Among gram-negative bacteria, these three carbapenems were highly active against Haemophilus influenzae (including ampicillin-resistant strains), Moraxella catarrhalis, and Bacteroides fragilis, and showed antibacterial activity equivalent to that of imipenem for Escherichia coli, Klebsiella pneumoniae, and Proteus spp. Thus, these new carbapenems are promising candidates for agents to treat nosocomial bacterial infections by gram-positive and gram-negative bacteria, especially multiresistant gram-positive cocci, including MRSA and vancomycin-resistant enterococci.

Abscess↗
PubMedDate not supplied

Effect of UVC-induced damage to DNA on the intercalation of thiazole orange: a convenient reporter for DNA damage.

We report a novel method of identifying damage to DNA leading to the loss of intercalation sites. Thiazole orange (TO), an intercalating cyanine dye, fluoresces strongly when intercalated in DNA, but not free in solution. Upon UVC-induced damage to DNA, the change in TO fluorescence is greater than the change in any of the other spectral or biochemical indicators (absorbance, circular dichroism and agarose gel electrophoresis), thus providing a fast screening method to identify damage to DNA. The method is geared toward high levels of damage, such as those that may result during radiation treatment of food products.

Benzothiazoles↗
PubMed1993

Synthesis and biological properties of some 3-[(N-substituted-amino)pyridinium-4-thiomethyl]-7-[2-(2-amino-thiazol- 4-yl)-2-(Z)-(methoxyimino)acetamido]ceph-3-em-4-carboxylates.

The synthesis and antibacterial activity of a series of beta-lactamase stable, broad spectrum 7-[2-(2-amino-thiazol-4-yl)-2-(Z)-(methoxyimino)acetamido]-cephalo sporins, characterised by a C-3-[N-(substituted-amino)pyridinium-4-thiomethyl] group, is described. Gram-positive and Gram-negative bacteria including extended spectrum beta-lactamase-producing strains were most susceptible to the N-amino- and N-methylamino derivatives (3a) and (3b); with the exception of Pseudomonas aeruginosa, (3b) was more active in vitro and in vivo than cefpirome or ceftazidime.

Animals↗
PubMed2002

New anti-MRSA and anti-VRE carbapenems; synthesis and structure-activity relationships of 1beta-methyl-2-(thiazol-2-ylthio)carbapenems.

Discovery of novel antimicrobial agents effective against infections caused by drug-resistant pathogens is an important objective. In order to find a new parenteral carbapenem antibiotic, which has potent antibacterial activity especially against methicillin-resistant staphylococci, vancomycin-resistant enterococci and penicillin-resistant Streptococcus pneumoniae, a series of 1beta-methylcarbapenems with thiazol-2-ylthio groups at the C-2 position have been synthesized. Structure-activity relationships were investigated which led to SM-197436 (27), SM-232721 (44) and SM-232724 (41), being selected for further evaluation.

Anti-Bacterial Agents↗
PubMed1975

Prolongation of chemotherapeutically induced remission of a syneneic murine leukemia by L-2,3,5,6-tetrahydro-6-phenylimidazo[2.1-BETA]thiazole hydrochloride.

L-2,3,5,6-Tetrahydro-6-phenylimidazo[2,1-beta]thiazole hydrochloride (LMS), when used in concert with 1,3-bis(2-chloroethyl)-1-nitrosourea, resulted in a significantly higher percentage of long-term leukemic-free survivors. The additive effect provided by LMS treatment was evident during the immunosuppressed period induced by 1,3-bis(2-chloroethyl)-1-nitrosourea treatment and when tumor load was minimal. Treatment with LMS alone did not appear to possess any significant antitumor effect. The beneficial effect of LMS treatment may be attributable to the immunostimulatory activity reported for this drug. LMS appears to possess characteristics that make it an excellent candidate for use as an immunostimulant in cancer combined modality treatment.

Adjuvants, Immunologic↗
PubMed1985

[HR 810 (cefpirome). Experimental evaluation of the in vitro and in vivo antibiotic activity of a new amino-2-thiazole methoxy- imino cephalosporin].

HR 810 or cefpirome is a new amino thiazole cephalosporin whose specific characteristic is a cyclopentenopyridinium group in position 3 of the cephem nucleus. This structure is responsible for a broad spectrum of activity, covering Enterobacteriaceae, including cephalosporinase-producing Enterobacter spp. and Citrobacter spp., Staphylococcus aureus, Pseudomonas aeruginosa and group D Streptococci.

Animals↗
PubMed1997

Effect of 2,4-disubstituted thiazol-5yl-aminoketones on inflammation. In vitro and in vivo biological studies: a structure-activity approach.

Some modified novel thiazol-5yl-aminoketones were evaluated for their anti-inflammatory, analgesic and antiproteolytic activities. Their inhibitory activity on 12-lipoxygenase (12-LO) and beta-glucuronidase in vitro was estimated. Their interaction with the stable free radical 1,1-diphenyl-2-picrylhydrazyl (DPPH) and their RM values were also determined. For two of them, the effect on zoxazolamine-induced paralysis after a prolonged treatment was determined. The duration of paralysis for the same compounds, (only one administration, one before zoxazolamine injection) was recorded too. The 2-amino substituted derivatives seem to be more potent in comparison with the 2-phenyl. The tested compounds were found to influence proteolysis but not the activities at beta-glucuronidase and 12-LO. Their interaction with DPPH was mild. Compound 2 seems to modify the activity of the hepatic drug metabolizing enzymes. In conclusion, their activity is related to certain structural characteristics.

Analgesics↗