Method for increasing polymerase chain reaction method sensitivity in diagnosing the cases of urogenital infection in patients with marked exudative inflammation
SUBSTANCE: method involves administering fluoroquinolone-series antibiotic like Ciproflaxin at a dose of 100-250 mg twice a day during 3-5 days and non-steroid anti-inflammatory preparation of Diclophenac at a dose of 75-150 mg/day during 3-7 days are sequentially introduced in preparing patient to diagnostic examination.
EFFECT: enhanced effectiveness in increasing method sensitivity.
Development relates to the field of medicine, in particular to urology, Nephrology, venereology, gynecology, pulmonology, obstetrics, neonatology, ophthalmology, may be used in medical biology that can be applied in veterinary medicine.
Known methods of mechanical removal of inflammatory exudate - cotton swabs, cotton swabs , the processing of the urethra sterile saline.
It can be insufficiently sensitive in patients with severe exudative inflammation. Scraping will be complicated and, in addition, this method nepriemlim in the diagnosis of Mycoplasma of the urine samples (with pyelonephritis and prostatitis (urine sample after the massage of the prostate gland).
For the best fence material on the intracellular microorganisms for PCR diagnostics use special cytometry[1, 2, 5].
Clinical methods of reducing the exudative inflammation prior to sampling, suggest mechanical leaching products of inflammation (such as urine), but this usually isn't enough to remove dismissed from the labor army related bacteria .
In addition, the known method pharmacologically provocation - prednizolonovuyu test to increase the sensitivity of diagnosis of urogenital infections .
There is a method of reducing the negative is osdate concomitant microflora on the sample microbiological samples by adding antibiotics to the environment taken by the material during transportation of samples to the laboratory polymerase chain reaction for reduction bacterial contamination . This method is used in the calculation to mitigate the impact of additional contaminaci microorganisms after specimen collection.
Previously used sample preparation methods did not reduce the effect of mixed infection involved in the inflammation along with Mycoplasma infection, namely contamination of samples extraneous DNA or RNA and the error amplification while .
In addition, severe exudative inflammatory reaction, represented by the white blood cells and their lysates, a large amount of mucus greatly complicate the selection of specific DNA of Mycoplasma, hominis and genitalium, therefore the results of the trial in patients with acute bacterial exudative inflammation can give a large number of false-negative results on specific intracellular pathogen[1, 12, 13].
These facts were motivated to use the method of concomitant elimination of the contaminating microflora to take the material for PCR diagnostics through the use of antibacterial agents in combination with anti-inflammatory drugs, eliminating exudative inflammation.
The essence of the invention is to increase the sensitivity of diagnosis of Mycoplasma hominis and Mycoplasma genitalium by polymerase chain reaction in patients with acute exudative (OS the eye) inflammation by eliminating concomitant DNA of bacterial pathogens and elimination of additional pollutant factor - lysates of bacteria in exudative inflammation with concomitant use of antibacterial drugs acting on the accompanying microflora, and anti-inflammatory drugs that reduce exudative inflammation.
The essence of the proposed development lies in the fact that the treatment is carried out until sampling with antibiotics and nonsteroidal anti-inflammatory drugs in the following ratio of ingredients:
the fluoroquinolone antibiotics row at a dose of 100-250 mg 2 times a day, 3-5 days,
- nonsteroidal anti-inflammatory drugs in medium-high therapeutic dose (diclofenac 75-150 mg/day) for 3-7 days.
The method proposed for patients with severe exudative (acute) inflammation, verified clinical manifestations: purulent, profuse mucous discharge, the number of cells in microscopy at low magnification - more than 30 in the field of view in the samples urethral swab, urine, juice prostate cancer, sputum, bronchoalveolar fluid. In addition, there may be a large content of bacterial microflora at sowing detachable - the more than 10,000 microorganisms in men and 100,000 women in 1 ml.
To eliminate nonspecific bacterial flora offered ofloxacin. The choice of this antibiotic is made on the basis that hvostastym on the most frequent concomitant organisms with this type of inflammation: E. coli., enterobacteria, Enterococcus spp., Staphyloccus saprophiticus, at the same time, the drug in the proposed scheme does not affect the DNA isolation of mycoplasmas, that is not difficult to identify.
The rationale for the doses of the components of the treatment.
It is proposed to use the dose of fluoroquinolones from 100 to 250 mg 2 times a day for 3-5 days.
Doses less than 100 mg insufficient for eradication of bacterial pathogens, and a dose of more than 250 mg can potentially lead to the eradication of Mycoplasma antigen, removing Mycoplasma DNA or decline
Duration of use of ciprofloxacin or ofloxacin - 3-5 days, the application is less than 48 hours is not enough to erradicate gram-negative microorganisms , at the same time, the use of the drug 5 days or more prior to the sampling of the material for the diagnosis of mycoplasmal antigen can greatly reduce the amount, and consequently, adversely affect the detection of DNA of Mycoplasma.
To reduce the appearance of exudative inflammation, which makes difficult the separation of DNA of Mycoplasma, it is proposed to use non-steroidal anti-inflammatory drug. As a last choice fell on diclofenac, a drug with maximum anti-inflammatory effect of the means of this group, better portability when using comparable doses, with protivovospalitelnym [14, 15, 16]. To solve the task the application within 5 days can provide a pronounced anti-inflammatory effect. It is proposed to use the medium to high therapeutic doses - doses less than 1 mg/kg not able to provide the task for 2-3 days (approximately less than or equal to 75 mg/day), doses of more than 1.5 mg/kg can cause side effects (water retention) and, importantly, adverse interaction with fluoroquinolone drugs . Therefore, clinical testing was conducted at doses of diclofenac 75-100 mg
The results of the experiment.
In the following table 1 presents the results of the diagnosis of mycoplasmosis according to polymerase chain reaction in patients with acute exudative inflammation before and after the proposed combination of anti-inflammatory therapy in patients with urogenital mycoplasmosis (verified by results of culture diagnostics on the specific environment to highlight with arginine-fermenting mycoplasmas)
|The patient's ID||Leukocytes in smear BEFORE applying the proposed method to improve sample preparation||The results of the DNA diagnosis of Mycoplasmosis before applying the proposed method to improve about is podgotovki.*||Leukocytes in smear after applying the proposed method to improve sample preparation||The results of the DNA diagnosis of mycoplasmosis when sampling at 5 days of combined anti-inflammatory and therapy|
|3.||Cover the field of view||-||25-30||-|
|8.||Cover the field of view||-||25-30||+|
|* + positive rez is ltate analysis on Mycoplasma|
- negative test result for Mycoplasma
Thus, the original on the background of exudative inflammation in the urethra mycoplasmosis PCR diagnosis was detected in 6 of 12 patients. After the proposed method improve the preparation of the Mycoplasma was detected in 10 of 12 patients. That is, the proposed method improved sample preparation has improved the sensitivity of the method chain reaction (PCR) from 50 to 83%.
Comparison with previously known
Table 2 presents the results of the diagnosis of mycoplasmosis according to polymerase chain reaction in patients with acute exudative inflammation before and after the implementation of the method of mechanical removal urination and processing cotton swab with saline solution 0.9% NaCl in patients with urogenital mycoplasmosis (verified by results of culture diagnostics on the specific environment to highlight with arginine-fermenting mycoplasmas)
|The patient's ID||The original number of cells in the smear from the urethra||The results of the HRC-diagnosis of mycoplasmosis||The number of cells in the smear from the urethra after machining||The results of PCR diagnostic micop is Osmose after machining|
|3.||Cover the field of view||-||40-50||-|
|8.||Cover the field of view||-||40-50||-|
Effect: machining increases the detection of the pathogen additional 2 patients mycoplasmosis of 12 (from 41%to 58%, i.e. by 17%).
The result of the experiment using combined anti-inflammatory treatment of patients with severe exudative inflammation mo is eolovogo Department managed to find the cause of disease, another 4 people (from 50 to 83%). The proposed method improve the sample preparation can further increase the sensitivity of detection of DNA of Mycoplasma in patients with exudative inflammation by 33%, as compared to previously used methods of mechanical treatment by 16%.
The experiment was carried out in outpatient departments and PCR laboratory of the Institute of Microbiology of the Ministry of defense Kirov and Kirov state medical Academy, Department of dermatology and Department of therapy qualification development Department.
The program will increase the sensitivity of the PCR method to clarify the etiological diagnosis using the proposed method of sample preparation conducted in 60 patients with neonorange urethritis.
The proposed method improve the sample preparation has improved the sensitivity of PCR-based diagnostics in patients with severe exudative inflammation in an average of 33%.
1. Encyclopedia of clinical laboratory tests. Ed Nautica, editor-in-chief of the Russian edition Won. "Labelform", Moscow, 1997.
2. Rasin, S., Yogev d, Naot Y. Molecular biology and pathogenicity ofmycoplasmas. Environ Mol Biol Rev, 1998; 1094-1156.
3. Encyclopedia of clinical laboratory tests. Ed Nautica, editor-in-chief of the Russian edition Won. "Labelform", Moscow, 1997.
4. New genetic technologies. Collection 1. Interregional Association for the development of new genetic technologies. P.32.
5. Not rology. A guide for physicians in 2 T. Ed. Yestereve, Moscow, "Medicine", 1995, Vol.2. C.119.
6. Taylor-Robinson, D Infections due to species of mycoplasma and ureaplasma: An update. Clin Infect Dis 1996; 23: 671.
7. Balows. A., Hausler. WJ, Hermann. K.L., et al. (Eds.): Manual of Clinical Microbiology, 5 th ed. Washington, DC, American Society for Microbiology, 1991.
8. Clyde, W.A., Kenny, G.E., and Schachter, J.: Cumitech 19: Laboratory Diagnosis of Chlamydial and Mycoplasmal Infections. Washington. DC, American Society for Microbiology, 1984.
9. Thomsen, AC, Undscov, HO. Diagnosis of mycoplasma hominis pyelonephritis by demonstration of antibodies in urine. J.Clin. Environ, 1979; 9:681.
10. Encyclopedia of clinical laboratory tests. Ed Nautica, editor-in-chief of the Russian edition Won. "Labelform", Moscow 1997. S (biomaterial and special requirements).
11. Encyclopedia of clinical laboratory tests. Ed Nautica, editor-in-chief of the Russian edition Won. "Labelform", Moscow 1997. S.
12. Encyclopedia of clinical laboratory tests. Ed Nautica, editor-in-chief of the Russian edition Won. "Labelform", Moscow 1997. 74.
13. Davia N. Gilbert, MD, Robert C. Moellering, Jr, MD, Merle A. Sande, MD. The Sanford Guide to Antimicrobial Therapy, Thirty - first Edition, 2001, p 23.
Method of increasing the sensitivity of PCR diagnosis of mycoplasmal infections in patients with acute exudative inflammation, characterized in that the patient in preparation for diagnosis injected antibiotic fluoroquinolone series - ciprofloxacin or ofloxacin dose of 100-250 mg 2 times a day, 3-5 days, and Nestea the command anti-inflammatory drug diclofenac at a dose of 75-150 mg/day, within 3-7 days.
SUBSTANCE: method involves taking material under study and inoculating it on selective nutrient medium. Pure culture of pathogenous or conditionally pathogenous microorganisms is selected. Their microbial suspensions are prepared and the chemotherapeutic means is added. Control samples are produced by adding physiologic saline. The case and control samples are incubated. The microbial suspensions are prepared with physiologic saline and human serum is added. The product is incubated, liquid nutrient medium is added and repeatedly subjected to incubation. Optical density of the cultures is determined. Growth inhibition in case sample being found more than 20% as large as in the control one, the chemotherapeutic means is considered to be effective.
EFFECT: simplified and accelerated method.
SUBSTANCE: method involves taking samples and diluting them with distilled water. Averaged substrate suspensions are precipitated, diluted with 95.5° ethyl alcohol and centrifuged in two stages. Monolayer smear is produced from the precipitate. The smear is dried at room temperature, fixed with 95.5° ethyl alcohol, Gram stained and micro-organism morphology is determined.
EFFECT: accelerated identification of plurality of microbial populations with Gram-positive and Gram-negative forms proportion concurrently determined.
SUBSTANCE: method involves recording and evaluating coagulating blood characteristics like response time r, spontaneous blood platelets aggregation intensity Ar, thrombin constant k, maximum amplitude MA, time required for forming fibrin-and-blood-platelets structure of blood clot T, total retraction and spontaneous clot lysis index F. r=3.19±0.41 min, Ar=-8.20±1.23 rel.units, k=2.57±0.41 min, MA=670.4±39.4 rel.units, T=48.61±7.88 min, F=18.43±1.63% being the case, acute pulmonary lesion syndrome development chance is predicted to be equal to 72.8% among the patients. r=8.76±1.42 min, Ar=-0.44±0.73 rel.units, k=10.52±1.89 min, MA=271.2±68.1 rel.units, T=77.8±10.04 min, F=32.40±6.91% being the case, acute pulmonary lesion syndrome development chance is predicted to be equal to 2.1% among the patients. r=7.26±0.73 min, Ar=-2.13±1.13 rel.units, k=6.84±0.60 min, MA=480.3±56.7 rel.units, T=62.08±2.52 min, F=24.87±4.41% being the case, acute pulmonary lesion syndrome development chance is predicted to be equal to 52.5% among the patients. r=3.53±0.48 min, Ar=-8.69±1.37 rel.units, k=2.60±0.48 min, MA=810.9±54.4 rel.units, T=37.78±3.25 min, F=31.14±3.54% being the case, acute pulmonary lesion syndrome development chance is predicted to be equal to 72.8% among the patients having acute hemorrhage.
EFFECT: high accuracy and descriptive power of data; accelerated process.
1 dwg, 1 tbl
SUBSTANCE: method involves introducing to a mammal therapeutic dose of drug having at least one subunit or at least one oligomer of mannan-binding lectin comprising one mannan-binding lectin subunit.
EFFECT: reduced risk of infection development; enhanced effectiveness in acting upon agents resistant to usual therapy.
43 cl, 2 dwg
SUBSTANCE: method involves evaluating neurological status and crude protein and calcium level in cerebrospinal fluid after intrathecally introducing methotrexate in the amount of 5 mg in auto liquor in postoperative period before starting chemotherapy. 5 ml of liquor are taken in a day and methotrexate course dose is selected depending on neurological status and changes in crude protein and calcium level in cerebrospinal fluid in liquor. No changes in neurological status and crude protein and calcium level being observed, methotrexate dose is increased by 20% when compared to the test dose. No changes in neurological status and increased crude protein level by 100% or higher and reduced calcium level by a value between 20% and 40% being observed, methotrexate dose is reduced by 20% when compared to the test dose. Negative changes in neurological status and crude protein being increased more than by 200% and reduced calcium level by more than 40% and reduced crude protein and increased calcium content being observed, chemotherapy course is restricted to already introduced methotrexate test dose.
EFFECT: improved biochemical criteria.
SUBSTANCE: method involves determining thyroid gland node diameter and thyrotropic hormone by applying ultrasonic examination approach. Histological examination is carried out with conclusion concerning morphologic nature being obtained like nodular colloid proliferating goiter or thyroid gland adenoma. Diagnostic index Σ is calculated from formula Σ=0.49*K1+0.07*K2-0.5*K3+1.76*K4-1.53, where K1 is the thyroid gland node diameter; K2 is the TTH concentration; K3 is the nodular colloid proliferating goiter index equal to 1 or 0; K4 is the thyroid gland adenoma index equal to 1 or 0. Diagnostic index Σ being less than zero, conclusions concerning powerless labor threat is to be drawn.
EFFECT: provided individual treatment approach; improved mother or fetus chances.
FIELD: clinical medicine, laboratory diagnostics.
SUBSTANCE: one should carry out complex laboratory survey including daily urinary sampling by Zimnitsky and blood sampling for analysis just after finishing sampling the last urinary portion. In every urinary portion one should detect pH, protein and relative density, in total urinary volume it is necessary to detect concentration and quantity of uric acid, creatinine and daily proteinuria, calculate clearances of uric acid and creatinine and fractional clearance of uric acid. On detecting purine exchange disorders including high concentration of urinary uric acid at low daily diuresis one should recommend to widen drinking mode; at altering urinary reaction towards acidic side one should prescribe alkalizing preparations; in case of pronounced purine exchange disorders and severe accompanied pathology one should carry out extracorporal therapy. The innovation enables to considerably improve the quality of diagnostics and match the most optimal schemes of therapy.
EFFECT: higher efficiency of therapy.
5 cl, 3 dwg, 5 ex, 20 tbl
SUBSTANCE: method involves stimulating watering. The tears are heated at 35-37°C during 10-15 min and placed on degreased object-plate as a drop and dried during 35-60 min at room temperature. Isotropic foreign point inclusions and three-rayed cracks being observed in peripheral protein zone of the sample, the operation is advised to be done in the nearest time.
EFFECT: simplified method.
SUBSTANCE: method involves studying lachrymal fluid sample placed on degreased object-plate as a drop and then dehydrated. The laboratory test tube containing stimulated lachrymal fluid is preliminarily 10-15 min long hold in thermostat at 35-37°C. Then a lachrymal fluid drop is dehydrated during 45-60 min on degreased object-plate and studied with microscope by transmitted light. Isotropic foreign point inclusions being found in peripheral lachrymal fluid sample zone, senile cataract development is to be diagnosed.
EFFECT: simplified method; easiness of operation; usability in screening studies.
SUBSTANCE: method involves taking punctate from retropancreatic cellular tissue by introducing 20 cm long needle of size equal to 0.64 mm with mandrin. The retropancreatic cellular tissue being reached, the mandrin is removed and active suction is carried out. Exudate is obtained in the amount of 0.1-0.2 ml and native preparation is produced. Microscopy examination is carried out. Leukocytes being found therein in the amount of 40 and higher in the vision field, purulent destructive pancreatitis phase is to be diagnosed and conclusion is drawn concerning surgical intervention being indicated.
EFFECT: reduced radiation loading; simplified examination method; reliability of obtained data.
FIELD: organic chemistry, antibacterial agents.
SUBSTANCE: invention relates to a novel heterocyclic compound, in particular, 3-(5-nitrofuryl)-7-(5-nitrofurfurylidene-3,3a,4,5,6,7-hexahydro-2H-indazole of the formula (1): that elicits an antibacterial activity with respect to bacterium of genus Staphylococcus and can be used in medicine. The compound of the formula 91) is prepared by reaction of 2,6-di-(5-nitrofurfurylidene)-cyclohexanone with hydrazine hydrate in propanol-2 medium. The yield is 80%, m. p. at 193-195°C, empirical formula is C16H14N4O6, LD50 value at intraperitoneal administration is 500 mg/kg. This compound exceeds activity of furacilinum and furazolidone by 16 and 2-31 times, respectively. Invention provides preparing compound possessing the higher and selective antibacterial activity and low toxicity.
EFFECT: valuable properties of compound.
1 cl, 3 tbl, 1 ex
FIELD: veterinary science.
SUBSTANCE: invention involves the combined use of antibacterial preparations and immunomodulator. Method involves complex of single and double RNA sodium salts from killer yeast Saccharomyces cerevisiae as an immunomodulator and synthetic polymer-carrier taken in the dose 0.3-0.4 mg/kg. Immunomodulator is administrated in animals in a single dose before onset of critical period, i. e. in 15-20 days of piglets growing. Method provides stimulation of factors of cellular and humoral immunity of animals without adverse reactions and complication due to selection of optimal dose of immunomodulator and its prolonged effect.
EFFECT: improved method for treatment and prophylaxis.
3 cl, 4 tbl, 3 ex
FIELD: veterinary science.
SUBSTANCE: invention proposes a preparation for treatment and prophylaxis of mastitis in cows at onset of the lactation period and in dry cows that comprises the following components, wt.-%: furacrylin, 0.4-0.6; dioxydin, 0.8-1.2; bee wax, 4-6, and sunflower oil, the balance. The preparation is heated to 38-40°C and administrated in cow mammary gland being in damaged and healthy lobules of udder through a nipple duct by using a syringe in the dose 5 ml. Using the preparation provides enhancing therapeutic and prophylactic effectiveness, decreasing labor intensity in treatment and prophylaxis of mastitis in cows at the lactation period and in dry cows.
EFFECT: enhanced and valuable properties of preparation.
3 tbl, 3 ex
FIELD: organic chemistry, antibiotics, pharmacy.
SUBSTANCE: invention relates to 9a-N-[N'-(phenylsulfonyl)carbamoyl]-derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerythromycin A and 5-O-desosaminyl-9-deoxo-9-dihydro-9a-aza-9a-homoerythronolide A that are new semisynthetic macrolide antibiotics relating to class of azalides showing antibacterial effect and describing by the general formula (1):
wherein R1 means hydrogen atom (H), (C1-C4)-alkyl or halogen atom; R means H or cladinosyl radical, and to their pharmaceutically acceptable salts. Also, invention relates to a method for their preparing and a pharmaceutical composition based on thereof.
EFFECT: improved preparing method, valuable medicinal properties of derivatives.
16 cl, 2 tbl, 14 ex
SUBSTANCE: method involves covering lesion focus with cell containing dialysis solution composed of Dimexid, antibiotic, 0.1% potassium furagin and 25% glucose solution taken in 1:4:3:2 proportion. The cell is fixed on teeth with ligature. Cell wall adjacent to gingiva is covered with semipermeable Cuprofan membrane and the opposite wall with latex rubber. Dialysis is carried out 20 min long twice a day.
EFFECT: enhanced effectiveness of treatment; retained natural protection factors; reduced edema and inflammation manifestations.
FIELD: organic chemistry of natural compounds, chemical technology, medicine.
SUBSTANCE: invention relates to the group of chitosan-containing compounds. Invention relates to synthesis of modified chitosan of the following structure: wherein n = 150-1400. The modified chitosan possesses the bactericidal activity, in particular, antituberculosis activity.
EFFECT: valuable medicinal properties of modified chitosan.
1 tbl, 1 dwg, 3 ex
SUBSTANCE: the present innovation deals with technique of revaccination in adults against diphtheria and tetanus under conditions of Far North. For this purpose one should form a group of people vaccinated more than 10 years ago to vaccinate them in February. The method leads to increased efficiency of vaccination due to decreased duration of vaccination period.
EFFECT: higher efficiency of revaccination.
FIELD: medicine, obstetrics.
SUBSTANCE: one should conduct antibacterial therapy 3 mo before planned pregnancy consisting of preparations of tetracyclinic group or macrolides in combination with nystatin and metronidasol to continue it since the first day of menstrual cycle and, also, it is necessary to perform correction of vaginal biocenosis, and about 3-4 wk after therapy carried out for 2 next mo before planned pregnancy starting, also, since the first day of menstrual cycle - metabolic therapy; At the onset of pregnancy one should conduct courses for preventing placental deficiency dealing with introduction of preparations that improve uterine-placental circulation, and preparations that improve rheological properties of blood and vitamin-metabolic therapy or the same preparations, and additionally - introduction of macrolides ad viferon rectally in case of activation of chlamydial infection. The present innovation enables to sanitize uterine cavity, improve uterine-placental circulation, restoration of placental tissue structure that, in its turn favors the birth of healthy generation.
EFFECT: higher efficiency of prophylaxis.
1 cl, 9 tbl
FIELD: medicine, pharmacy.
SUBSTANCE: medicinal formulation possessing the bacteristatic effect consists of a core comprising the following components, wt.-%: clarithromycin, 40.0-80.0; polyvinylpyrrolidone, 3.0-10.0; sodium lauryl sulfate, 2.0-5.0; sodium croscarmelose, 4.0-10.0; aerosil, 0.5-2.0; magnesium stearate, 0.5-2.0, and microcrystalline cellulose, 10.0-31.0. Also, the medicinal formulation consists of envelope comprising the following components, wt.-%: hydroxypropylmethylcellulose, 30.0-70.0; polyethylene glycol, 12.0-22.0; titanium dioxide, 11.0-20.0, hydroxypropylcellulose, 2.0-10.0, dye yellow quinoline, 1.0-4.0, and vanillin, 1.0-4.0. Also, invention describes a method for preparing the medicinal formulation by wet granulation followed by tableting and applying the envelope from an aqueous suspension. Prepared tablets show the necessary mechanical strength, insignificant scattering index by mass (± 3.5%) and dissolving 88-91% for 30 min.
EFFECT: improved and valuable properties of medicinal formulation.
3 cl, 2 tbl
FIELD: medicine, gynecology, surgery.
SUBSTANCE: one should introduce 3.5%-chitosan ascorbate gel into fistulous channel that contains metronidasol at the dosage of 2 mg/ml, at the volume up to 20 ml once/2 d till complete fistula's closing. The present innovation enables to activate reparative processes and fistulous epithelization that favors for closing fistulous channel in earlier terms.
EFFECT: higher efficiency of therapy conducted.
FIELD: organic chemistry, chemical technology, biochemistry, pharmacy.
SUBSTANCE: invention relates to methods for preparing 2-phenylamino-5-alkylphenylacetic acids of the general formula (I)
intermediate compounds for their preparing, their pharmaceutically acceptable salts and pharmaceutically acceptable prodrug esters wherein R, R1, R2, R3, R4 and R5 have corresponding values. Compound of the general formula (I) is prepared by splitting lactam of the formula (II): wherein symbols have values given in the description with a base, its precursors and methods for preparing these precursors. Abovementioned methods can comprise if necessary the temporal protection of all reaction groups showing effect followed by isolation of the prepared compound. Invention provides preparing compounds of the general formula (I) representing pharmaceutically active compounds that represent selective inhibitors of cyclooxygenase-2.
EFFECT: improved preparing method, valuable biochemical properties of compounds.
10 cl, 1 sch, 9 ex