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PubMed2002

Biosynthesis of nodulisporic acid A: precursor studies.

Nodulisporic acid A (NAA) is an indole-diterpene natural product produced by an indeterminate species of the endophytic fungus Nodulisporium. NAA (Figure 1) is structurally related to the paspaline class of fungal metabolites. The biosynthetic origin proposed for these alkaloids involves the acetate/mevalonic acid pathway leading to geranylgeranyl pyrophosphate (GGPP). GGPP is then proposed to condense with tryptophan to form the basic indole-diterpene core. A washed cell procedure was devised to incorporate labeled precursors into NAA by a mutant Nodulisporium culture designated MF6244. Incorporation of 2-(13)C-acetate and 2-(13)C-mevalonolactone into NAA was found to occur in the classical mevalonic acid pattern. In addition to the four mevalonic acid units that form the eastern side of the molecule, three additional isoprenylations occur to form the western and southern regions of NAA. Contrary to published reports on related compounds, incubations of Nodulisporium MF6244 with (14)C- and (13)C-tryptophan showed no incorporation of label into NAA. However, high levels of incorporation into NAA were obtained with known tryptophan precursors (14)C-, (13)C-, and (15)N-anthranilic acid and (14)C- and (13)C-ribose. A novel pathway for the biosynthesis of NAA is presented.

Acetates↗
PubMed1974

Occurrence of N-formylkynurenine in extracts of Neurospora crassa: evidence for the activity of tryptophan pyrrolase.

N-formylkynurenine and kynurenine have been detected in extracts of tryptophan-grown Neurospora crassa. When the mycelia were grown in medium supplemented with l-[2-(14)C]tryptophan, the radioactivity was detected in N-formylkynurenine and N-formylanthranilic acid; with l-[beta-(14)C]tryptophan, radioactivity was detected in N-formylkynurenine, kynurenine, kynurenic acid, and xanthurenic acid. The occurrence of N-formylkynurenine in extracts of tryptophan-grown Neurospora is interpreted as direct evidence for the activity of tryptophan pyrrolase in this organism. The presence of this enzyme was expected on the basis of several earlier studies, but its activity in vitro has so far escaped detection. The in vivo evidence presented here suggests its presence and contributes importantly to our understanding of the tryptophan-anthranilic acid cycle.

Carbon Radioisotopes↗
PubMed2001

[Effect of feeding with a poisonous mushroom Clitocybe acromelalga on the metabolism of tryptophan-niacin in rats].

The poisonous mushroom Clitocybe acromelalga contains clitidine, which resembles nicotinic acid mononucleotide, and 4-amino-pyridine-2,3-dicarboxylic acid, which resembles quinolinic acid. Both are important intermediates in the tryptophan-niacin pathway. Therefore, we investigated the effect of feeding a niacin-free and tryptophan-limited diet containing the toadstool Clitocybe acromelalga on the metabolism of tryptophan to niacin in rats. The toadstool diet was fed to the rats for only one day (this day was designated day 0). Urinary excretion of intermediates in the tryptophan-niacin pathway, such as anthranilic acid, kynurenic acid, xanthurenic acid, 3-hydroxyanthranilic acid, quinolinic acid, nicotinamide, N1-methylnicotinamide, N1-methyl-2-pyridone-5-carboxamide, and N1-methyl-4-pyridone-3-carboxamide, was higher in the toadstool group than in the control on day 0-day 1 and day 1-day 2. The blood levels of tryptophan and NAD on day 1 were also higher in the toadstool group. Accordingly, intake of Clitocybe acromelalga appeared to increase the conversion of tryptophan to niacin.

Animals↗
PubMed2001

Purification, characterization and crystallization of thermostable anthranilate phosphoribosyltransferase from Sulfolobus solfataricus.

Anthranilate phosphoribosyltransferase (TrpD; EC 2.4.2.18) from the hyperthermophilic archaeon Sulfolobus solfataricus (ssTrpD) was expressed in Escherichia coli, purified and crystallized. Analytical gel permeation chromatography revealed a homodimeric composition of the enzyme. The steady-state kinetic characteristics suggest tight binding of the substrate anthranilic acid and efficient catalysis at the physiological growth temperature of S. solfataricus. Crystals of ssTrpD diffract to better than 2.6 A resolution and preliminary X-ray characterization was carried out. The crystals are suitable for structure determination.

Anthranilate Phosphoribosyltransferase↗
PubMed2001

Investigation of the role of 3-hydroxyanthranilic acid in the degradation of lignin by white-rot fungus Pycnoporus cinnabarinus.

An aminophenol, 3-hydroxyanthranilic acid (3-HAA), has been proposed to play important roles in lignin degradation. Production of 3-HAA in Pycnoporus cinnabarinus was completely inhibited by a combination of tryptophan and S-(2-aminophenyl)-L-cysteine S,S-dioxide (APCD) while the fungus grew well and produced high amounts of laccase. The biosynthesis of 3-HAA is mainly through the metabolism of tryptophan in the kynurenine pathway. A minor pathway for 3-HAA synthesis is through the hydroxylation of anthranilic acid during the biosynthesis of tryptophan in the shikimic acid pathway. Through UV irradiation of wild-type P. cinnabarinus (WT-Pc) spores, a 3-HAA-less mutant was produced. Both WT-Pc, under the inhibitory culture condition, and the 3-HAA-less mutant were found to degrade lignin in unbleached kraft pulp as efficiently as the WT-Pc, which unambiguously demonstrated that 3-HAA does not play an important role in the fungal degradation of lignin.

Journal Article↗
PubMed1991

Oxygen-dependent catabolism of indole-3-acetic acid in Bradyrhizobium japonicum.

Some strains of Bradyrhizobium japonicum have the ability to catabolize indole-3-acetic acid (IAA). Examination of this catabolism in strain 110 by in vivo experiments has revealed an enzymatic activity catalyzing the degradation of IAA and 5-hydroxy-indole-3-acetic acid. The activity requires addition of the substrates for induction and is oxygen dependent. The highest activity is obtained when the concentration of inducer is 0.2 mM. Spectrophotometric data are consistent with the suggestion that the indole ring is broken during degradation of IAA. We hypothesize that the enzyme catalyzes an oxygen-consuming opening of the indole ring analogous to the one catalyzed by tryptophan 2,3-dioxygenase. The pattern of metabolite usage by known tryptophan-auxotrophic mutants and studies of metabolites by high-performance liquid chromatography indicate that anthranilic acid is a terminal degradation product in the proposed pathway.

Culture Media↗
PubMed1998

N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 3. Structure-activity relationship and optimization of the N-aryl substituent.

3-¿4-[2-(Benzoxazol-2-ylmethylamino)ethoxy]phenyl¿-(2S)-((2- benzoylph enyl)amino)propionic acid (1) and (2S)-((2-benzoylphenyl)amino)-3-¿4-[2-(5-methyl-2-phenyloxazol-4-y l)e thoxy]phenyl¿propionic acid (2) are peroxisome proliferator-activated receptor gamma (PPARgamma) agonists and have antidiabetic activity in rodent models of type 2 diabetes. As part of an effort to develop the SAR of the N-2-benzoylphenyl moiety of 1 and 2, a series of novel carboxylic acid analogues, 23-66, modified only in the N-2-benzoylphenyl moiety were synthesized from L-tyrosine and evaluated as PPARgamma agonists. In general, only modest changes in the N-2-benzoylphenyl moiety of 1 and 2 are tolerated. More specifically, the best changes involve bioisosteric replacement of one of the two phenyl rings of this moiety. Addition of substituents to this moiety generally produced compounds that are less active in the cell-based functional assays of PPARgamma activity although binding affinity to PPARgamma may be maintained. A particularly promising set of analogues is the anthranilic acid esters 63-66 in which the phenyl ring in the 2-benzoyl group of 1 and 2 has been replaced by an alkoxy group. In particular, (S)-2-(1-carboxy-2-¿4-[2-(5-methyl-2-phenyloxazol-4-yl)ethoxy]phen yl¿ ethylamino)benzoic acid methyl ester (63) has a pKi of 8.43 in the binding assay using human PPARgamma ligand binding domain and a pEC50 of 9.21 in the in vitro murine lipogenesis functional assay of PPARgamma activity. Finally, 63 was found to normalize glycemia when dosed at 3 mg/kg bid po in the Zucker diabetic fatty rat model of type 2 diabetes.

Administration, Oral↗
PubMedDate not supplied

Determination of methyl anthranilate in food samples by coupling stopped-flow mixing technique and time-resolved luminescence detection.

A sensitive and fast approach for the determination of methyl anthranilate in grape must and honey samples, using time-resolved luminescence measurements, has been reported for the first time. The method involves the alkaline hydrolysis of the ester to anthranilic acid and the formation of a chelate with terbium(III) and tri-n-octylphosphine oxide in presence of Triton X-100. Kinetic and equilibrium measurements were obtained in 0.1 and 15 s, respectively, by using a stopped-flow mixing technique. The dynamic ranges of the calibration graphs of the kinetic and equilibrium methods were 21.9 nmol/L-29.2 micromol/L and 19.7 nmol/L-21.9 micromol/L, respectively, and the detection limits were 7.3 and 6.6 nmol/L, respectively. The precision, expressed as relative standard deviation, was less than 3%. Although both-kinetic and equilibrium methods exhibited very similar analytical features, only the better selectivity of the former allowed the content of methyl anthranilate to be determined in the samples, as the initial rate measurements avoided the negative effect that the sample matrix caused in the equilibrium measurements. The analytical recoveries obtained by applying the kinetic method to the analysis of grape must and flower honey samples were in the range 92.5-105.0%.

Chelating Agents↗
PubMed2000

Validation of a LC method for the determination of 5-aminosalicylic acid and its metabolite in plasma and urine.

The choice of a proper analytical method for the quantification of drugs and/or their metabolites in biological samples plays a significant role in the evaluation and interpretation of bioavailability, bioequivalence and pharmacokinetic data. The aim of this study was validation of a method for the identification and quantitative determination of 5-aminosalicylic acid (5-ASA) and its metabolite N-acetyl-5-aminosalicylic acid in human plasma and urine. According to previous studies on the disposition of 5-ASA (mesalazine) in a patient with inflammatory bowel diseases, we have developed a rapid, sensitive method for the determination of 5-ASA and its acetylated metabolite, N-acetyl-5-aminosalicylic acid (Ac-5-ASA). The advantage of this method is that it measures both compounds, and is more rapid, reproducible and credible than the previous studies [C. Fischer, K. Maier, U. Klotz, J. Chromatogr. Biomed. Appl. 225 (1981) 498-503; P.N. Shaw, A.L. Sivner, L. Aarons, J.B. Houston, J. Chromatogr. Biomed. Appl. 274 (1983) 393-397; B. Norlander, R. Gotthard, M. Strom, Aliment. Pharmacol. Ther. 3 (1989) 333-342; U. Klotz, G.L. Stracciari, Arzneim.-Forsch. Drug Res. II 43 (12) (1993) 1357-1359]. 5-ASA was quantitatively determined in human plasma and urine samples by liquid chromatography following prior derivatization to its acetylated metabolite (Ac-5-ASA). N-Acetyl-anthranilic acid was used as the internal standard. The detection was performed with a spectrofluorimetric detector, excitation at 311 nm, cut-off at 449 nm. The method was validated for the following parameters: linearity, recovery, sensitivity, precision, accuracy, selectivity and stability, limits of quantification and of detection. It showed good linearity (r2 > or = 0,996) in the range 0.1 ng/ml to 8 microg/ml using a Lichrospher 60 RP-select B column. The lower limit of detection was 20 ng/ml in plasma and urine. The within-run relative standard deviations (R.S.D.) were below 6.7% at all concentration levels and the between-run R.S.D. were below 25.4% at all concentration levels.

Adult↗
PubMedDate not supplied

Open pore block of connexin26 and connexin32 hemichannels by neutral, acidic and basic glycoconjugates.

The mechanisms of molecular discrimination by connexin channels are of acute biological and medical importance. The availability of affinity or open-pore blocking reagents for reliable and specific study of the connexin permeability pathway, would make possible the rigorous cellular and physiological studies required to inform, in molecular terms, the underlying role of intercellular communication pathways in development and disease. Previous work utilized a series of glucosaccharides labeled with an uncharged fluorescent aminopyridine (PA-) group to establish steric constraints to permeability through connexin hemichannels. In that work, the smallest probe permeable through homomeric Cx26 and heteromeric Cx26-Cx32 channels was the PA-disaccharide, and the smallest probe permeable through homomeric Cx32 channels was the PA-trisaccharide. The larger impermeable probes did not block permeation of the smaller probes. Building on this work, a new set of glucosaccharide probes was developed in which the label was one of a homologous series of novel anthranilic acid derivatives (ABG) that carry negative or positive formal charge or remain neutral at physiological pH. When the PA-label of the smallest impermeant PA-derivatized oligosaccharides was replaced by ABG label, the resulting probes acted as reversible, high-affinity inhibitors of large molecule permeation through connexin pores in a size and connexin-specific manner.

Animals↗
PubMed1991

Indole-3-acetic acid (IAA) synthesis in the biocontrol strain CHA0 of Pseudomonas fluorescens: role of tryptophan side chain oxidase.

Pseudomonas fluorescens strain CHA0 is an effective biocontrol agent against soil-borne fungal plant pathogens. In this study, indole-3-acetic acid (IAA) biosynthesis in strain CHA0 was investigated. Two key enzyme activities were found to be involved: tryptophan side chain oxidase (TSO) and tryptophan transaminase. TSO was induced in the stationary growth phase. By fractionation of a cell extract of strain CHA0 on DEAE-Sepharose, two distinct peaks of constitutive tryptophan transaminase activity were detected. A pathway leading from tryptophan to IAA via indole-3-acetamide, which occurs in Pseudomonas syringae subsp. savastanoi, was not present in strain CHA0. IAA synthesis accounted for less than or equal to 1.5% of exogenous tryptophan consumed by resting cells of strain CHA0, indicating that the bulk of tryptophan was catabolized via yet another pathway involving anthranilic acid as an intermediate. Strain CHA750, a mutant lacking TSO activity, was obtained after Tn5 mutagenesis of strain CHA0. In liquid cultures (pH 6.8) supplemented with 10 mM-L-tryptophan, growing cells of strains CHA0 and CHA750 synthesized the same amount of IAA, presumably using the tryptophan transaminase pathway. In contrast, resting cells of strain CHA750 produced five times less IAA in a buffer (pH 6.0) containing 1 mM-L-tryptophan than did resting cells of the wild-type, illustrating the major contribution of TSO to IAA synthesis under these conditions. In artificial soils at pH approximately 7 or pH approximately 6, both strains had similar abilities to suppress take-all disease of wheat or black root rot of tobacco. This suggests that TSO-dependent IAA synthesis is not essential for disease suppression.

Bacterial Proteins↗
PubMed1971

Physiological studies of biosynthetic indole excretion in Bacillus alvei.

Bacillus alvei excretes indole during early exponential growth in acid-hydrolyzed casein medium. l-Threonine is the amino acid responsible for "early" indole excretion, and the amount of indole excreted is directly related to the amount of l-threonine in the medium. "Early-indole" excretion can be prevented by the continuous addition of serine (3.1 mumoles per ml per hr) or by substituting a mutant with an impaired ability to degrade serine. The addition of serine to a culture during the period of indole excretion halts the excretion and stimulates indole utilization. Threonine is a competitive inhibitor of serine (K(i) = 0.6 m) in the tryptophan synthetase B reaction. The internal tryptophan concentration increases during the period of indole excretion, suggesting that threonine acts by increasing the activity of the tryptophan pathway. This view is supported by experiments demonstrating that anthranilic acid and indoleacrylic acid also stimulate indole excretion. A metabolic explanation is offered and discussed.

Acrylates↗
PubMed1989

N- and 2-substituted N-(phenylsulfonyl)glycines as inhibitors of rat lens aldose reductase.

A variety of N-(phenylsulfonyl)-N-phenylglycines 5, N-(phenylsulfonyl)-2-phenylglycines 6, and N-(phenylsulfonyl)anthranilic acids 7 were prepared as analogues of the N-(phenylsulfonyl)glycine 1 aldose reductase inhibitors. In the rat lens assay, several derivatives of 5 display greater inhibitory activity than the corresponding glycines 1, suggesting that N-phenyl substitution enhances affinity for aldose reductase. Enzyme kinetic evaluations of the 4-benzoylamino analogues of 5 and 1 demonstrate that these compounds produce inhibition by the same mechanism. However, the significant differences in relative inhibitory potencies between compounds of series 5 and 1 may indicate that these compounds do not interact with the inhibitor binding site in precisely the same manner. Evaluation of the individual enantiomers of series 6 reveals that the S isomers are substantially more active than the corresponding R isomers. Also, with the exception of the naphthalene analogue 6n, the S stereoisomers of this series display greater inhibitory potencies than the glycines 1. The anthranilates 7 generally are less active than the glycines 1, demonstrating that direct incorporation of an aromatic ring in the glycine side chain may result in a decrease in affinity for aldose reductase.

Aldehyde Reductase↗
PubMed2000

Isolation and symbiotic characterization of aromatic amino acid auxotrophs of Sinorhizobium meliloti.

Ten aromatic amino acid auxotrophs of Sinorhizobium meliloti (previously called Rhizobium meliloti) Rmd201 were generated by random mutagenesis with transposon Tn5 and their symbiotic properties were studied. Normal symbiotic activity, as indicated by morphological features, was observed in the tryptophan synthase mutants and the lone tyrosine mutant. The trpE and aro mutants fixed trace amounts of nitrogen whereas the phe mutant was completely ineffective in nitrogen fixation. Histology of the nodules induced by trpE and aro mutants exhibited striking similarities. Each of these nodules contained an extended infection zone and a poorly developed nitrogen fixation zone. Transmission electron microscopic studies revealed that the bacteroids in the extended infection zone of these nodules did not show maturation tendency. A leaky mutant, which has a mutation in trpC, trpD, or trpF gene, was partially effective in nitrogen fixation. The histology of the nodules induced by this strain was like that of the nodules induced by the parental strain but the inoculated plants were stunted. These studies demonstrated the involvement of anthranilic acid and at least one more intermediate of tryptophan biosynthetic pathway in bacteroidal maturation and nitrogen fixation in S. meliloti. The alfalfa plant host seems to provide tryptophan and tyrosine but not phenylalanine to bacteroids in nodules.

Amino Acids↗
PubMed2005

Synthesis and inhibitory effect of novel glycyrrhetinic acid derivatives on IL-1 beta-induced prostaglandin E(2) production in normal human dermal fibroblasts.

Olean-11,13(18)-dien-3beta,30-diol dihemiphthalate (3), which was derived from glycyrrhetinic acid (GA), has been reported to produce a potent of anti-inflammatory effect in in vivo assays. Using 3 as a lead compound, we attempted to synthesize some modified compounds which varied in the following; i) the position of a carboxyl group in the phthalate moiety, ii) the number of carboxyls attached to the benzoyl group, iii) conversion of benzene ring to another ring system, iv) the linkage form between the benzene ring and oleanene skeleton at position 3 and/or 30. These were screened for their inhibitory activity against interleukin-1 beta (IL-1 beta)-induced prostaglandin E(2) (PGE(2)) production in normal human dermal fibroblasts (NHDF). Although conversion of the ortho-carboxyl group of 3 into the meta-position or the para-position led to an increase in inhibitory activity, the elimination or increase of the carboxyl group resulted in loss of the inhibitory activity. Conversion of the ester bond to the amide bond at position 3 and/or 30 of 3 did not contribute to a significant increase in inhibitory activity. On the other hand, among the derivatives possessing an anthranilic acid moiety at position 30 of 3beta-O-acetyl-olean-11,13(18)-dien-30-oic acid (20), 3beta-hydroxy-30-nor-olean-11,13(18)-dien-20 beta-[N-(2-carboxyphenyl)]carboxamide (30) showed the most potent inhibitory activity (IC(50) 1.0 microM) in this series.

Cells, Cultured↗
PubMed1996

Hypochlorous acid interactions with thiols, nucleotides, DNA, and other biological substrates.

HOC1-induced one-electron oxidation of Fe(CN)(6)4- was used as a reference reaction to investigate the stoichiometry of interaction of HOCl with a variety of biological substrates. GSH and GSSG were both found capable of reacting with four and 2-mercaptoethanol with three HOCl molecules. Stopped-flow investigations, with HOCl in excess, indicate that very fast primary reactions of HOCl with GSH and DTPA are followed by slower secondary reactions. In the case of GSH we propose that one HOCl reacts at the terminal alpha-amino-group and three HOCl react at the -SH group to generate the sulfonylchloride GSO2Cl. This assignment is supported by the finding that reaction of HOCl (in excess) with 2-mercaptonaphthalene generates the absorption spectrum of authentic naphthalene-2-sulfonylchloride. NADH reacts with at least two HOCl molecules. A very fast primary reaction of HOCl was followed by a slower secondary reaction at HOCl/NADH > 2, but neither the primary nor the secondary reaction led to NAD+. Stopped-flow investigations of reactions of HOCl with nucleotides indicate that HOCl reacts slowly with the amino-groups of AMP, CMP, and GMP but very fast with the heterocyclic NH-groups of GMP, inosine, and TMP. AMP and CMP promote, but GMP, inosine, and TMP retard HOCl-induced oxidation of Fe(CN)(6)4-. At present we have no convincing evidence, however, that products of interaction of HOCl with nucleotides are capable of one-electron oxidation of Fe(CN)6(-4), with generation of free radical intermediates. HOCl causes slow but very efficient denaturation of native DNA, in our opinion not by oxidative fragmentation, but due to chlorination of amino- and heterocyclic NH-groups of the DNA-bases, which leads to dissociation of the double strand by the loss of hydrogen bonding. HOCl-induced oxidation of Fe(CN)(6)4- is promoted very efficiently by catalytic amounts of Cu2+. Catalysis is explainable by formation of a CuIFeIII(CN)(6)2- complex, with CuI acting as electron donor in a propagating Fenton-like reaction, CuIFeIII(CN)(6)2- +HOCl-->Cu2+ + Fe(CN)(6)3- + Cl- + OH, the rate constant of which was estimated as k = 1.8 x 10(5) M-1 s-1. HOCl is inactivated by Tris, but Hepes promotes HOCl-induced oxidation of Fe(CN)(6)4- very efficiently; this is a warning against application of such buffers in investigations of HOCl- or myeloperoxidase-induced reactions. Anthranilic acid was found to interact with four HOCl molecules to yield highly reactive (unidentified) one-electron oxidants.

Animals↗
PubMed2001

Electrophoretic sequencing of heparin/heparan sulfate oligosaccharides using a highly sensitive fluorescent end label.

The sequencing of heparan sulfate oligosaccharides has recently become possible using integral Glycan Sequencing, which utilizes a combination of chemical and enzymatic degradation steps followed by polyacrylamide gel electrophoresis. This technique has previously employed the fluorescent label, anthranilic acid, and has been used to sequence low nmol amounts of purified saccharides. Here, we present an improved method, which uses the alternative label, 7-aminonapthalene-1,3-disulfonic acid, the reducing agent sodium triacetoxyborohydride and optimizes the nitrous acid step in heparin/heparan sulfate degradation. These improvements increase the sensitivity at least ten-fold taking the amount of starting material required into the pmol range. We show that this label is compatible with the integral glycan sequencing methodology and demonstrate its application to the sequencing of chemically modified heparin derivatives. Advances in sequencing techniques for heparan sulfate saccharides will permit detailed structure-function studies and will in the future underpin novel proteomics-based approaches aimed at studying their diverse functional roles as protein regulators.

2-Naphthylamine↗
PubMed2002

Synthesis and antiinflammatory screening of some quinazoline and quinazolyl-4-oxoquinazoline derivatives.

Synthesis of some new derivatives of 2-aryl-4-oxo-1-(4-quinazolyl)quinazolines is described. Methyl N-(4-quinazolyl)anthranilate was allowed to react with phenyl iso(thio)cyanate to give 3-phenyl-1-(4-quinazolyl)-1, 2, 3, 4-tetrahydro-2, 4-dioxo- and 4-oxo-2-thioxoquinazolines (3a and 3b respectively) Alternatively, anthranilic acid amide derivatives were subjected to cyclization with aromatic aldehydes to give 2-aryl-4-oxo-1-(4-quinazolyl)-1, 2, 3, 4-tetrahydroquinazolines 5. On the other hand, 2-chloro-4-(4-substituted 1-piperazinyl)quinazoline derivatives were subjected to the same type of reactions at the 2-position to afford the corresponding quinazoline derivatives 8 and 10 respectively. Furthermore, the acid amide 4b cyclized with acid chlorides to give the corresponding 2-aryl-1-(2-chloro-4-quinazolyl)-4-oxo-1, 4-dihydroquinazolines 11 from which the triazoloquinazoline derivatives 13 and 15 were synthesized through the intermediate hydrazine derivatives 12. Most of the newly synthesized compounds were tested for their antiinflammatory activities. However, some of the novel compounds were found to exhibit good antiinflammatory potencies.

Animals↗