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PubMed2004

Molecular characterization of bifunctional hydroxymethyldihydropterin pyrophosphokinase-dihydropteroate synthase from Plasmodium falciparum.

A 2118-base pair gene encoding the bifunctional hydroxymethyldihydropterin pyrophosphokinase-dihydropteroate syntheses of Plasmodium falciparum (pfPPPK-DHPS) was expressed under the control of the T5 promoter in a DHPS-deficient Escherichia coli strain. The enzyme was purified to near homogeneity using nickel affinity chromatography followed by gel filtration and migrates as an intense band on sodium dodecyl sulfate-polyacrylamide gel electrophoresis with apparent mass of approximately 83 kDa. Gel filtration suggested that the native pfPPPK-DHPS might exist as a tetramer of identical subunits. The enzyme was found to be Mg2+ - and ATP-dependent and had optimal temperature ranging from 37 to 45 degrees C with peak activity at pH 10. Sodium chloride and potassium chloride at 0.2 and 0.4 M, respectively, activated the activity of the enzyme but higher salt concentrations were inhibitory. Guanidine-HCl and urea inhibited the enzyme activity by 50% at 0.25 and 0.9 M, respectively. Kinetic properties of the recombinant pfPPPK-DHPS were investigated. Sulfathiazole and dapsone were potent inhibitors of pfPPPK-DHPS, whilst sulfadoxine, sulfanilamide, sulfacetamide and p-aminosalicylic acid were less inhibitory. Our construct provides an abundant source of recombinant pfPPPK-DHPS for crystallization and drug screening.

Adenosine Triphosphate↗

PubMed2006

Metal complexes of Schiff base derived from sulphametrole and o-vanilin. Synthesis, spectral, thermal characterization and biological activity.

Metal complexes of Schiff base derived from condensation of o-vanilin (3-methoxysalicylaldehyde) and sulfametrole [N(1)-(4-methoxy-1,2,5-thiadiazole-3-yl)sulfanilamide] (H2L) are reported and characterized based on elemental analyses, IR, 1H NMR, solid reflectance, magnetic moment, molar conductance, mass spectra, UV-vis and thermal analysis (TGA). From the elemental analyses data, the complexes were proposed to have the general formulae [M2X3(HL)(H2O)5].yH2O (where M=Mn(II), Co(II), Ni(II), Cu(II), Zn(II) and Cd(II), X=Cl, y=0-3); [Fe2Cl5(HL)(H2O)3].2H2O; [(FeSO4)2(H2L)(H2O)4] and [(UO2)2(NO3)3(HL)(H2O)].2H2O. The molar conductance data reveal that all the metal chelates were non-electrolytes. The IR spectra show that, H2L is coordinated to the metal ions in a tetradentate manner with ON and NO donor sites of the azomethine-N, phenolic-OH, enolic sulphonamide-OH and thiadiazole-N. From the magnetic and solid reflectance spectra, it is found that the geometrical structures of these complexes are octahedral. The thermal behaviour of these chelates shows that the hydrated complexes losses water molecules of hydration in the first step followed immediately by decomposition of the anions and ligand molecules in the subsequent steps. The activation thermodynamic parameters, such as, E*, DeltaH*, DeltaS* and DeltaG* are calculated from the DrTG curves using Coats-Redfern method. The synthesized ligand, in comparison to their metal complexes also were screened for their antibacterial activity against bacterial species, Escherichia coli, Salmonella typhi, Bacillus subtillus, Staphylococcus aureus and Fungi (Aspergillus terreus and Aspergillus flavus). The activity data show that the metal complexes to be more potent/antimicrobial than the parent Shciff base ligand against one or more microbial species.

Bacteria↗

PubMed2006

14N nuclear quadrupole resonance of some sulfa drugs.

The 14N nuclear quadrupole double resonance spectra of different polymorphs of sulfanilamide, sulfadiazine, sulfamerazine and sulfamethazine have been measured and the 14N quadrupole coupling tensors have been determined. The obtained 14N spectra are compared with those of other sulfa drugs like sulfathiazole. It is shown that different polymorphs can be easily discriminated. The application of this technique for non-destructive analysis, polymorph determination and quality control in the production of pharmaceuticals is stressed.

Anti-Infective Agents↗

PubMedDate not supplied

Studies on aminopyrazoles: antibacterial activity of some novel pyrazol.

Hydrazones 2a-d were prepared from diazotiazation of sulfanilamide or its derivatives followed by coupling with ethyl cyanoacetate. 3-Aminopyrazoles 3a-d were obtained by refluxing of 2a-d with hydrazine hydrate in ethanol. [Bis(-methylthio)methylene]malononitrile (4) was reacted with aminopyrazoles 3a-d in refluxing DMF containing triethylamine to yield the novel pyrazolo[1,5-a]pyrimidines 6a-d. The anilino derivatives 8a-h were obtained by fusion of compounds 6a-d with aromatic amines. When compounds 6a,c,d were subjected to the reaction with hydrazine hydrate, the hydrazino derivatives 9a-c were isolated. Also, the aminopyrazoles 3 were reacted with some electrophiles such as arylidenemalononitriles, ethoxymethylene malononitrile and ethyl ethoxymethylene cyanoacetate to yield the novel substituted pyrazolo[1,5-a]pyrimidines 13, 17 and 19, respectively. Structures of the new compounds were established by their elemental analyses and spectral data. Most of these compounds were also tested in vitro for their antibacterial activity against some gram positive and gram negative bacteria.

Anti-Bacterial Agents↗

PubMed1975

The effect of sulfonamides on pain and swelling following removal of ectopic third molars.

A double-blind, placebo-controlled trial was carried out to study the value of cones containing sulfanilamide and sulfathiazole in the healing of third molar sockets. On the seventh postoperative day, 94 patients were examined regarding pain, swelling and the overall effect of the operation. Trials were run to compare sulfa cones directly with a placebo: in addition, the placebo and sulfa drugs were each compared with the effects of no medication. Pairs were made of the left and right mandibular third molars in the same patient and the results assessed by sequential analysis. It was found that although sulfa cones were better than the placebo, they themselves were no better or worse than leaving the socket alone.

Clinical Trials as Topic↗

PubMed1978

Antifibrinolytic prevention of alveolitis sicca dolorosa.

In a double-blind study dental cones containing the antifibrinolytically active propylic ester of p-hydroxybenzoic acid (PEPH), sulfanilamide and sulfathiazol or placebo were placed in dental sockets following removal of impacted mandibular third molars on 95 consecutive patients, 50 women and 45 men. The duration of the operation, the type of surgeon, preoperative symptoms and the use of peroral anticonception were recorded. The patients were asked to return to the clinic on the seventh postoperative day, and it was then noted whether the healing was disturbed by Alveolitis Sicca Dolorosa (ASD) or not. Statistical analysis showed a significantly prophylactic effect of PEPH against ASD. The prophylactic effect was most pronounced in the group of male patients without preoperative symptoms and in the group of patients operated by dental students. It could not be demonstrated that the sulfa drugs in the cones were of any benefit to the healing of the socket.

Adolescent↗

PubMed1975

Carbon-13 magnetic resonance spectroscopy of drugs. Sulfonamides.

The natural abundance 13C magnetic resonance spectra of a series of sulfonamide drugs(sulfanilamide, sulfaguanidine,sulfathiazole, sulfasuxidine, sulfadiazine, sulfamerazine, sulfamethiazine, and sulfapyridine) have been determined at 25.15 MHz employing the pulse Fourier transform technique. The chemical shefts have been assigned with the aid of off-resonance and selective proton decoupling techniques, as well as by long-range carbon-13 proton coupling patterns.

Chemical Phenomena↗

PubMed2003

Carbonic anhydrase inhibitors. Inhibition of tumor-associated isozyme IX by halogenosulfanilamide and halogenophenylaminobenzolamide derivatives.

Two series of halogenated sulfonamides have been prepared. The first consists of mono/dihalogenated sulfanilamides, whereas the second one consists of the mono/dihalogenated aminobenzolamides, incorporating equal or different halogens (F, Cl, Br, and I). These sulfonamides have been synthesized from the corresponding anilines by acetylation (protection of the amino group), chlorosulfonylation, followed either by amidation, or reaction with 5-amino-1,3,4-thiadiazole-2-sulfonamide (and eventually deacetylation). All these compounds, together with the six clinically used sulfonamide inhibitors (acetazolamide, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, and brinzolamide) were investigated as inhibitors of the transmembrane, tumor-associated isozyme carbonic anhydrase (CA) IX. Inhibition data against the classical, physiologically relevant isozymes I, II, and IV were also obtained. CA IX shows an inhibition profile which is generally completely different from those of isozymes I, II, and IV, with potent inhibitors (inhibition constants in the range of 12-40 nM) among both simple aromatic (such as 3-fluoro-5-chloro-4-aminobenzenesulfonamide) as well as heterocyclic compounds (such as acetazolamide, methazolamide, 5-amino-1,3,4-thiadiazole-2-sulfonamide, aminobenzolamide, and dihalogenated aminobenzolamides). This first detailed CA IX inhibition study revealed many interesting leads, suggesting the possibility to design even more potent and eventually CA IX-selective inhibitors, with putative applications as antitumor agents.

Antigens, Neoplasm↗

PubMedDate not supplied

Reactions of the bioregulatory agent nitric oxide in oxygenated aqueous media: determination of the kinetics for oxidation and nitrosation by intermediates generated in the NO/O2 reaction.

The reaction kinetics of nitric oxide autoxidation in aerobic solutions were investigated by direct observation of the nitrite ion product and by trapping the strongly oxidizing and nitrosating intermediates formed in this reaction. The rate behavior observed for nitrite formation [rate = k3[O2][NO]2, k3 = (6 +/- 1.5) x 10(6) M-2 s-1 at 22 degrees C] was the same as found for oxidation of Fe(CN)6(4-) and of 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) and as for the nitrosation of sulfanilamide. There was a slight decrease in k3 to (3.5 +/- 0.7) x 10(6) M-2 s-1 at 37 degrees C. The second-order dependency for NO was observed at NO concentrations as low as 3 microM. The results of the competitive kinetics studies suggest that the key oxidizing intermediates, species which are both strong oxidants and nitrosating agents, are not one of those commonly proposed (NO2, N2O3, NO+, or O2NO-) but are one or more as yet uncharacterized NOx species.

Aerobiosis↗

PubMed1975

R factor-mediated resistance to aminoglycoside antibiotics in Pseudomonas aeruginosa.

Conjugal transferability of drug resistance was examined, in eleven Pseudomonas aeruginosa strains which were isolated in Frankfurt. Four R factors were demonstrated from three strains using P. aeruginosa as recipients but they were nontransferable to Escherichia coli K12. Two R factors, i.e., Rms146 and Rms147, mediated resistances to tetracycline (TC), streptomycin (SM), sulfanilamide (SA), kanamycin (KM), lividomycin (LV), gentamicin C complex (GM) and 3', 4'-dideoxykanamycin B (DKB). They mediated the formation of aminoglycoside-inactivating enzymes, i.e., SM phosphotransferase, SM adenylyltransferase, KM and LV phosphotransferase l, and GM and DKB 6'-N-acetyltransferase. TC resistance conferred by these R factors was due to impermeability of the drug. P. aeruginosa Ps 142 carried two kinds of R factor in one cell, Rms148 (SM) and Rms149 (SM-SA-GM-CPC) (CPC, carbenicillin). Rms148 (SM) was transferable at a high frequency of 10-1 and mediated the formation of SM phosphotransferase. Rms149 mediated the formation of drug-inactivating enzymes, ie., GM 3-N-acetyltransferase and beta-lactamase, but did not inactivate SM. SM resistance was probably due to impermeability of the drug.

Acetyltransferases↗

PubMed1976

Characterization and replication control of plasmids from Enterobacter cloacae DF 13.

It has been shown previously that Enterobacter clocacae DF13 harbours at least five different size classes of plasmids. A 45 x 10(6)-Mr self-transmissible R factor determining resistance against tetracyclin, sulfanilamide, streptomycin and chloramphenicol, a 6.0 x 10(6)-Mr bacteriocinogenic factor without sex factors activity and cryptic plasmids in the size classes of Mr 1.3 x10(6), 2.8 x 10(6) and 8.0 x 10(6) respectively. The present work deals with the determination of the homogeneity and molecular relationship of 1.3 x 10(6)-Mr (mini) and 2.8 x 10(6)-Mr (midi) cryptic plasmids and the 6.0 x 10(6)-Mr (maxi) bacteriocinogenic factor, their kinetics of replication and their replication control in response to inhibition of protein synthesis.

Base Sequence↗

PubMed1981

Drug resistance and R plasmids of Escherichia coli strains isolated from pigs, slaughterers, and breeders of pigs in Japan.

We isolated 1,120 drug-resistant Escherichia coli strains from pigs, slaughterers, breeders of pigs, and urban residents and examined their drug resistance. With reference to resistance to tetracycline (Tc) chloramphenicol (Cm), streptomycin (Sm), and sulfanilamide (Su), Tcr, Smr, and Sur strains were most frequently isolated from pigs (57.9%), followed by slaughterers (50.2%) and breeders (42.4%). By contrast, the isolation frequencies of Tcr, Smr, and Sur strains from urban residents were low (12.0%). The isolation frequencies of R plasmids from resistant strains were more than 50% in the case of pigs, slaughterers, and breeders, whereas they were only 13.8% in urban residents. Kanamycin-resistant strains were frequently isolated from pigs (40.3%), slaughterers (22.6%), and breeders of pigs (25.4%), but seldom (only 3.4%) from urban residents. With ampicillin resistance, the frequencies of strains from pigs, slaughterers, breeders, and urban residents were 30.0, 21.5, 5.6, and 13.8%, respectively. R plasmids specifying these latter resistances were frequently seen from pigs (24.0%), slaughterers (23.6%), and breeders (21.1%), but they were not isolated from urban residents. The results suggest that the porcine gut can function as a reservoir of antibiotic resistance plasmids which can then be directly transferred to humans, with the highest frequency of such plasmids appearing in people in the most immediate contact with these animals.

Abattoirs↗

PubMed1974

Factors affecting selectivity of brilliant green-phenol red agar for salmonellae.

Commercial brilliant green (BG)-sulfa agar was found to be nonselective toward a test series of Enterobacteriaceae. Various formulations of BG were prepared by using Trypticase soy agar (BBL) as a base. Results were more reproducible when BG dye was added after sterilization than before. Sulfonamides improved selectivity as compared with brilliant green alone. Sulfanilamide (SN) was slightly more selective for salmonellae than other sulfonamides tested. Bile salts and sodium dodecyl sulfate markedly reduced the toxicity of BG to all the test bacteria. Enterobacter strains were most difficult to inhibit. A combination of 5 mg of BG and 1 g of SN/liter prevented growth of Proteus mirabilis and Escherichia coli and retarded growth of Enterobacter strains. The BG-SN agars were superior in selectivity to a series of commercial agars tested, and numbers of salmonellae recovered on BG-SN agar and Trypticase soy agar (BBL) were the same. Brilliant green agars with various degrees of selectivity are described.

Agar↗

PubMed1970

Genetic stability of various resistance factors in Escherichia coli and Salmonella typhimurium.

Genetic stability of R factors was studied in Salmonella typhimurium LT-2 and Escherichia coli K-12. It was found that fi(+) R [or R(f)] factors were unstable in LT-2, losing their drug-resistance markers at high frequencies, and were stable in K-12; fi(-) R [or R(i)] factors were stable in both hosts. Both fi(+) and fi(-) R factors were genetically stable also in recombination-deficient mutants of K-12. An fi(+) R factor, which was unstable in S. typhimurium LT-2 wild type, was relatively stable in a recombination-deficient mutant of LT-2. In the spontaneous loss of the drug-resistance markers of fi(+) R factors in LT-2, the markers for sulfanilamide, streptomycin, and chloramphenicol resistance were lost together at high frequencies and the tetracycline marker was retained stably. The remaining drug-resistance markers of the spontaneous segregants of LT-2 were transmissible to K-12 by mixed cultivation, indicating that they were still in the form of R factors.

Bacteriological Techniques↗

PubMed1974

Genetic location of two mutations affecting the lysyl-transfer ribonucleic acid synthetase of Bacillus subtilis.

Two mutations (lysS1 and lysS2), each independently resulting in a thermosensitive, lysyl-transfer RNA synthetase (l-lysine: tRNA ligase [adenosine 5'-monophosphate] EC 6.1.1.6), have been mapped on the Bacillus subtilis chromosome between purA16 (adenine requirement) and sul (sulfanilamide resistance). They are linked by transformation with sul (70 to 74% cotransfer) in the order purA16-lysS1-lysS2-sul. The mutant loci are either in the same gene or in two closely linked genes. They are not linked to the tryptophanyl-tRNA synthetase structural gene or to the lys-1 locus.

Adenine↗

PubMed1982

A chromosomally located transposon in Pseudomonas aeruginosa.

A new transposon, Tn2521, coding for carbenicillin, streptomycin, spectinomycin, and sulfanilamide resistance, has been identified in Pseudomonas aeruginosa. The transposon occurs naturally in the chromosome of clinical strains of P. aeruginosa isolated in geographically separated hospitals. This has been demonstrated by its transductional linkage to the pur-136 marker and also by Southern hybridization. Tn2521 is 6.8 kilobases, can transpose from the chromosome to both IncP-1 and IncP-2 plasmid genomes, and has a pattern of restriction endonuclease sites unlike that of any previously described transposon. The carbenicillin resistance carried by Tn2521 is due to the PSE-4 type of beta-lactamase.

Anti-Bacterial Agents↗

PubMed1966

Gene recombination and segregation of resistance factor R in Escherichia coli.

Hashimoto, Hajime (Osaka University, Osaka, Japan), and Yukinori Hirota. Gene recombination and segregation of resistance factor R in Escherichia coli. J. Bacteriol. 91:51-62. 1966.-Independent chloramphenicol-sensitive (CM(s)) mutants of the drug-resistance factor R were isolated. Introduction of two different R factor CM(s) mutants into a single bacterium, by conjugation or transduction, gave chloramphenicol-resistant (CM(r)) colonies when such strains were plated on a medium containing chloramphenicol (Cm). These CM(r) colonies resulted from recombination between two R factors contained within the same cell. Most of the CM(r) colonies were heterogeneous, and segregation of drug-resistance markers was observed among the progeny. Segregated bacteria which still carried the recombinant R factor were stable for resistance to Cm as well as for other markers of R. All the markers of recombinant R factors were cotransducible with high coincidence and at the same frequency as wild-type R. Sensitive mutants of R which had lost all the resistance markers of the R factor were found also. A mutation of R, referred to as SMA, which was sensitive to streptomycin and sulfanilamide, was capable of reverting to resistance to both of these drugs simultaneously. The sensitive alleles for SMA, CM, and TC were shown to be recessive to the resistance alleles. Mutants of R having multisite mutations or deletions in the CM gene were isolated and used to analyze the pattern of linked segregation of unselected markers of the recombinant R factor. The drug resistance factor R was shown to have two linkage groups, CM-SMA and TC-m.

Chloramphenicol↗

PubMed1967

Drug resistance of enteric bacteria. 13. Distribution of R factors in Escherichia coli strains isolated from livestock.

Escherichia coli strains isolated from 151 swine and 108 fowl, which were kept at the Animal Health Center, Maebashi, Japan, were surveyed for drug resistance and distribution of R factors. All of the swine and 38% of the fowl excreted E. coli strains resistant to tetracycline, chloramphenicol, streptomycin, and sulfanilamide, or certain combinations thereof. Among 278 resistant cultures isolated from swine, 13% were found to be resistant to one antibiotic, whereas 87% were resistant to more than one antibiotic. Among these resistant strains, 40% carried R factors which were transferable by the usual conjugal process. The resistance patterns of these R factors included 36% which were singly resistant and 64% which were multiply resistant. Among 54 resistant cultures isolated from fowl, 24% were singly resistant and 76% were multiply resistant. Of the resistant strains from fowl, 22% carried R factors. The resistance patterns of R factors included 50% of the singly resistant type and 50% which were multiply resistant. In spite of feeding with dairy products containing only tetracycline, a high incidence of multiple resistance was observed in the E. coli strains and the R factors isolated from these animals.

Animals↗