Biomedical subjects

N Yulug

Publications and source records attributed to N Yulug.

24 records · Page 2Linked to original sources

PubMed1991

Synthesis and antimicrobial activities of some new tetrahydro-2H-1,3,5-thiadiazine-2-thione derivatives of cefadroxil.

Eleven new 7-[2-(dihydro-5-substituted-6-thioxo-2H-1,3,5-thiadiazine-3( 4H)-yl)-2- (4-hydroxyphenyl)acetamido]-3-methyl-3-cephem-4-carboxylic acid derivatives were synthesized by the reaction of cefadroxil monohydrate, formaldehyde and substituted potassium dithiocarbamate. Their structures have been elucidated by spectral data and elementary analysis. The title compounds were tested for antimicrobial activity in vitro against gram-positive bacteria (Staphylococcus aureus, Streptococcus faecalis), gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa) and yeast-like fungi (Candida albicans, C. parapsilosis, C. stellatoidea, C. pseudotropicalis) in comparison with cefadroxil monohydrate. The activity of compounds 1 and 10 against S. aureus (MBC: 37.5 micrograms/ml) and compound 1 against E. coli (MBC: 75 micrograms/ml) were found to be the same as cefadroxil monohydrate. Compounds 1 and 10 were more effective than cefadroxil monohydrate against S. faecalis with 25 and 37.5 micrograms/ml MBC values, respectively. None of the compounds and cefadroxil monohydrate proved to be effective against P. aeruginosa (MBC: greater than 100 micrograms/ml). While cefadroxil monohydrate had no activity against yeast-like fungi, compounds 9 and 10 were significantly effective against yeast-like fungi (MFC: 37.5 micrograms/ml).

Anti-Bacterial Agents↗

PubMed1991

Synthesis and antifungal activities of some new tetrahydro-2H-1,3,5-thiadiazine-2-thiones.

A number of new 3-benzyl-5-[alpha-(substituted)carboxymethyl]- tetrahydro-2H-1,3,5-thiadiazine-2-thiones has been synthesized as prodrugs by incorporating the amine group of some amino acids into tetrahydro-2-H-1,3,5-thiadiazine-2-thione ring. The compounds have been prepared by the reactions of benzylamine with potassium hydroxide, carbon disulphide formaldehyde and various amino acids. The structures of the compounds have been elucidated by UV, IR, 1H-NMR, mass spectra and elementary analysis. The in vitro activity of these compounds against yeast-like fungi (Candida albicans, C. parapsilosis, C. pseudotropicalis, C. stellatoidea) was investigated by tube dilution method. Their minimal inhibitory concentration (MIC) and minimal fungicidal concentration (MFC) values were determined. All the compounds were found to be active between 3.12-12.5 micrograms/ml against the four fungi tested.

Antifungal Agents↗

PubMed1990

Synthesis and antimicrobial activities of some new tetrahydro-2H-1,3,5-thiadiazine-2-thione derivatives of ampicillin.

Compounds having alpha-[dihydro-5-substituted 6-thioxo-2H- 1,3,5-thiadiazine-3(4H)-yl]benzylpenicillin structure were synthesized by the reaction of ampicillin trihydrate, formaldehyde and dithiocarbamic acid salts. The structures were evident from chemical and spectral analysis. The antimicrobial activities of the compounds were investigated against some gram-positive (Staphylococcus aureus and Streptococcus faecalis) and gram-negative (Escherichia coli and Pseudomonas aeruginosa) bacteria and some yeast-like fungi (Candida albicans, C. parapsilosis, C. stellatoidea and C. pseudotropicalis) and molds such as Trichophyton rubrum, T. mentagrophytes, Microsporum canis, M. gypseum, Penicillium and Aspergillus by the tube dilution method. In addition to MIC (minimal inhibitory concentration), MBC (minimal bactericidal concentration) and MFC (minimal fungicidal concentration) values were determined using ampicillin trihydrate as standard. The compounds synthesized were usually found as effective as ampicillin trihydrate against S. aureus and S. faecalis and less effective than ampicillin trihydrate against E. coli. Both the compounds synthesized and ampicillin trihydrate are ineffective in the concentrations studied against P. aeruginosa. Compound 10 and 11 are more effective against all the yeast-like fungi than the other compounds and ampicillin trihydrate.

Ampicillin↗

PubMed1990

Synthesis and antimicrobial activities of some new tetrahydro-2H-1,3,5-thiadiazine-2-thione derivatives of amoxicillin.

A number of 6-[2-(dihydro-5-substituted-6-thioxo-2H-1,3,5-thiadiazine-3( 4H)-yl)-2-(4-hydroxyphenyl)acetamido]penicillanic acids has been synthesized as prodrugs by incorporating the amine group of amoxicillin trihydrate into tetrahydro-2H-1,3,5-thiadiazine-2-thione ring. The compounds have been prepared by the reaction of various alkyl or aralkyl amines with potassium hydroxide, carbon disulfide, formaldehyde and amoxicillin trihydrate. The structures of the compounds have been elucidated by UV, IR, 1H-NMR spectra and elementary analysis. The in vitro activity of these compounds against gram-positive bacteria (Staphylococcus aureus, Streptococcus faecalis), gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa) and yeast-like fungi (Candida albicans, C. parapsilosis, C. stellatoidea, C. pseudotropicalis) was investigated by the tube dilution method and compared with the activity of amoxicillin trihydrate. By this way their minimal inhibitory concentration (MIC), minimal bactericidal concentration (MBC) and minimal fungicidal concentration (MFC) values were determined. Compound I and Compound VII were significantly more effective than amoxicillin trihydrate against S. aureus (MBC: 6.25 micrograms/ml). Compound VI and Compound XI were effective against S. faecalis (MBC: 6.25 micrograms/ml) and Compound I and Compound VI were effective against E. coli (MBC: 12.5 micrograms/ml). All of the compounds and amoxicillin trihydrate were ineffective against P. aeruginosa (MIC: greater than 100 micrograms/ml). Compound IX and Compound X were the most active derivatives against yeast-like fungi; the MFC values for these compounds ranged between 6.25 and 37.5 micrograms/ml.

Amoxicillin↗

PubMed1989

Synthesis of some new Mannich bases derived from 6-acyl-3-(3,5-dimethylpiperidinomethyl)-2(3H)-benzoxazolones+ ++ and their biological activities.

A number of 6-acyl-3-(3,5-dimethylpiperidinomethyl)-2(3H)-benzoxazolones have been synthesized by Mannich reaction and their antibacterial and antifungal activities have been tested. Their chemical structures have been proved by means of their IR, NMR, mass spectroscopic data and by elementary analysis. Investigation of antimicrobial activity of compounds was done by tube dilution and paper disc techniques using bacteria (Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 25923, Pseudomonas aeruginosa ATCC 27853, Staphylococcus faecalis RSKK 10541) and yeast-like fungi (Candida parapsilosis, Candida albicans, Candida pseudotropicalis, Candida stellatoidea). Among the compounds tested 6-(2-chlorobenzoyl)-3-(3,5-dimethylpiperidinomethyl)-2(3H)-benz oxazolone (Compound 2) and 6-(3-chlorobenzoyl)-3-(3,5-dimethylpiperidinomethyl)-2(3H)-benz oxazolone (Compound 3) showed the most favorable activity.

Amines↗

PubMedDate not supplied

Synthesis and biological activity of 6-acyl-3-substituted-2(3H)-benzoxazolones.

The preparation of a series of 6-acyl-3-substituted-2-(3H)-benzoxazolones is described. Their structures have been elucidated by UV, IR, NMR, MS and elementary analysis. These compounds have been tested for their antimicrobial activities against to Escherichia coli ATCC 25922, Staphylococcus aureus, ATCC 25923, Pseudomonas aeruginosa ATCC 27853, Staphylococcus faecalis RSKK 10541, Candida parapsilosis, Candida albicans, Candida pseudotropicalis, Candida stellatoidea.

Anti-Bacterial Agents↗