• Archives of Pharmacal Research
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• 제12권4호
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• pp.289-294
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• 1989

A computer program which can differentiate compounds whose absorbance spectra are very similar was developed. The program. [SPECMAN PLUS], written in Pascal provides automated spectral comparison techniques, utilizing the values of Root Mean of Squares (RMS) of differences. This comparison routine of the program can deal with spectra of compounds different concentrations and different spectral recording resolutions. In addition, the program was designed applicable to any spectral data of digital form. The program was applied to the UV spectra of 13 pencillins and 5 cephalosporins, whose absorbance spectra are so similar. As a result, all compounds examined could be differentiated from each other.

• Biomolecules & Therapeutics
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• 제1권1호
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• pp.103-108
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• 1993

The synthesis and physicochemical properties of a novel cephalosporin, DWC-751 are described. DWC -751, (6R , 7R)-7-[ (Z)-2-(2-aminothiazol-4-yl)-2- methoxyiminoacetamido]-3-[(1-methylbenzotriazol-3-ium) methyl]-ceph-3-em-4-carboxylate monosulfate($IV_{\alpha}$) was conveniently obtained by the conversion of compound (IV) into the crystalline monosulfate. Adjusting pH 4.8-5.2 in aqeous solution of the crude crystalline, compound(IV) in the form of a crystalline pentahydrate was prepared with a high degree of purity. The influence of the various organic and inorganic acids on the solubility of compoud(IV) and its salts, was examined. Particularly, the solubility of DWC-751 was 92 mg/mι at pH 1.7 and 233 mg/mι at pH 3.0. DWC-751 showed a broad antimicrobial spectrum against gram-positive and negative bacteria.

• Toxicological Research
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• 제19권4호
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• pp.321-324
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• 2003

Antigenic potential of a novel cephalosporin, IDC7181 was examined a active systemic anaphylaxis (ASA) and passive cutaneous anaphylaxis (PCA) test, in guinea pig and mouse-rat models, respectively. In ASA test, IDC7181 induced the signs of restlessness in a few animals immunized with a high dose (100 mg/kg) of IDC7181 alone or in combination with Freund's complete adjuvant (FCA). In PCA test, only one of ten sera from the animals immunized with a high dose (100 mg/kg) of IDC7181 in the absence or presence of FCA showed positive reaction. The positive reaction, induced by IDC7181, which may be due to $\beta$-lactam ring, in ASA and PCA tests were negligible in comparison with those of traditional cephalosporins. Taken together, it is suggested that IDC7181 do not cause immunological problems in clinical dosage.

• 대한수의학회지
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• 제46권4호
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• pp.405-408
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• 2006

A 4-year-old male Miniature Pinscher was referred because of head tilt, nystagmus, and ataxia. The hemogram revealed a moderate neutrophilic leukocytosis. On magnetic resonance imaging, cerebellar inflammation was detected. And cerebrospinal fluid analysis indicated marked neutrophilic pleocytosis. Based on these results, bacterial meningoencephalitis was suspected. The clinical signs were well controlled by a combination antibiotics therapy of the third generation cephalosporins (cefotaxime and cefixime) and metronidazole. We tentatively diagnosed this case as a bacterial meningoencephalitis because clinical signs were improved after only antibiotics therapy and relapsed when stopped antibiotics administrations, even though the result of bacterial culture on communication of cerebrospinal fluid (CSF) was negative.

• Archives of Pharmacal Research
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• 제13권4호
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• pp.385-387
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• 1990

3-[(1-Methyl-1H-tetrazol-5-y)thiomethyl] is one of the most important side chains in cephaloporins. This side chain which occures in numerous antibacterial agents, suc as cefamandole, latamoxef, cefoperazone, and cefmenoxime, contributes remarkable potency and broad spectrum. For the continuous work of study on the development of broad spectrum cephalosporins, we become interested in the effect of structural modification of the substituent at the N-1 position of mercaptoterazole toward biological activity because our recent work had demonstraated that the arylsubstituted mercaptotetrazoles (Fig. 1) had favorable effect on the activity against gram-positive bacteria. The main focus of this report was to investigate the relationship between activity and functional groups in the mercaptotetrazole.

• Archives of Pharmacal Research
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• 제24권2호
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• pp.89-94
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• 2001

Several quaternary pyridinium cephalosporin analogues were prepared analogues were Prepared and evaluated in vitro for antibacterial activity against selected Gram-positive and Cram-negative organisms. Most of the synthesized analogues were either as effective or less effective against the tested bacterial organ isms than the reference com pounds, Cefpirome and Ceftazidime.

• 약학회지
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• 제43권3호
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• pp.306-315
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• 1999

To develop new cephalosporin antibiotics with improved antibacterial activities, a series of 7$\beta$-[2-(2-aminothiazol-4-y)-(Z)-2-(1-carboxy-1-methylethoxyimino)acetamido] -3-[5-(heterocycle)thiomethylpy-rrolidin-3-ylthio]methyl-3-cephem-4-carboxylic acid (14~18) having aminothiazol carboxymethylethoxy-imino group on the C-7 position and (heterocycle) thiomethyl pyrrolidinthiomethyl group on the C-3 position of the cephem ring were synthesized. These compounds were tested for antimicrobial activity in vitro against Gram(+) and Gram(-) bacteria. Compounds 15 and 16 showed remarkable antibacterial activity against Salmonella typhimurium TV119 and Alcalienes faecalis KCTC1004, but most of compounds showed lower activity than cefotaxime.

• Bulletin of the Korean Chemical Society
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• 제11권5호
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• pp.383-386
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• 1990

We have synthesized several bicyclic heteroaromatic compounds with bridgehead nitrogen from N-amine salts of heteroaromatic amines. 2-Amino and 2-unsubstituted thiazolo[3,2-b][l,2,4]triazole derivatives 2a-b were prepared by the cyclization reaction from N-amine salts of aminothiazole-5-yl(N-methoxyimino)acetate with cyanogen bromide and formamidine acetic acid salt, respectively. 2-Methylthiazolo[3,2-b][1,2,4]triazole 2c was obtained from N-acetylated N-amine salt of aminothiazole-5-yl(N-methoxyimino)acetate by the cyclization reaction in the presence of polyphosphoric acid (PPA). 2-Substituted and 2-unsubstituted thiazole[3,2-b][1,2,4]triazole derivatives 2a-c were coupled with 7-aminocephalosporanic acid (7-ACA). Coupled cephalosporin derivatives 1a-c did not have good antibacterial activities in vitro.

• Bulletin of the Korean Chemical Society
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• 제8권5호
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• pp.418-421
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• 1987

Syntheses of cefotaxime analogs with halosubstituted phenyltetrazolthiomethyl at the $C_{3^-}$position are described. Their in vitro potency was established. The compounds exhibited a broad antibacterial spectrum. Some of these compounds showed activity against Gram-positive bacteria superior to the parent cefotaxime. Against Gram-negative bacteria, these compounds are less effective than cefotaxime.

• Bulletin of the Korean Chemical Society
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• 제15권6호
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• pp.453-455
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• 1994

Semiempirical MO calculations are applied to estimate the substituent effects on acylations of the nonfused N-vinyl-2-amino $\beta-lactams$ having frameworks analogous to 3-cephems. The stabilization energy for the reaction intermediate of the nucleophilic attack by the hydroxide ion is selected as the reactivity index and calculated by AM1 and PM3 methods for the model $\beta-lactams$ with substituents at the C1 and N-vinyl terminal positions. The reactivities are larger for -SH connected to the C1 and strong $\pi-acceptors$ at the N-vinyl terminal implying the large reactivity for known active cephalosporins. Quantum chemical calculation of stabilization energy could be useful in correlating antibiotic activities of many compounds obtained as derivatives of a lead compound.