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1.
Eur Rev Med Pharmacol Sci ; 26(20): 7649-7655, 2022 10.
Article in English | MEDLINE | ID: mdl-36314336

ABSTRACT

OBJECTIVE: Recent literature suggests that tumor budding (TB) may have a significant clinical impact on colorectal cancers. Our study aims to reveal the effect of TB on the long-term outcomes of patients and to reveal whether there is a difference in tumor location and TB in colonic cancer. PATIENTS AND METHODS: A cohort of 100 patients with non-metastatic colon cancer was included in the study. The clinicopathological information of the patients was reviewed. Patients' preparations were re-evaluated to identify TB as: low, medium, and high and represent 0-4 buds, 5-9 buds, and 10 or more buds per 0.785 mm2, respectively. Long-term oncological outcomes of patients were analyzed. The recurrence, metastasis, and final status of the patients were determined during the follow-up period. RESULTS: Low TN was associated with <65 year (p = 0.048), absence of lymphatic metastasis (p = 0.003), and absence of perineural invasion (p = 0.023). High TB was associated with higher pT stage (p = 0.017) and tumor stage (p = 0.005). Additionally, right-sided tumors had a high TB score than left side (82.3% vs. 23.6%, p = 0.011). Patients with high TB had lower overall survival, but these were not statically significant. According to multiple regression analysis, mortality risk was associated with age (p = 0.046), pN status (p = 0.003) and TB (p = 0.040). CONCLUSIONS: High TB is associated with mortality in colon cancer and is more common in right colonic carcinoma.


Subject(s)
Colonic Neoplasms , Humans , Prognosis , Neoplasm Staging , Retrospective Studies , Colonic Neoplasms/pathology , Lymphatic Metastasis
2.
J Transl Sci ; 7(3)2021 Jun.
Article in English | MEDLINE | ID: mdl-34540270

ABSTRACT

BACKGROUND AND AIM: Hepatocellular carcinoma (HCC) biomarkers are limited, as even the best studied, alpha-fetoprotein (AFP), is elevated in no more than 50% of HCC patients. The aim was to evaluate several serum liver function tests in relation to survival and tumor characteristics in a large cohort of Turkish HCC patients. METHODS: We retrospectively examined the serum levels of gamma glutamyl transpeptidase (GGT) in relation to patient survival. RESULTS: Kaplan-Meier analysis showed that only GGT and albumin amongst liver function tests, were significantly associated with survival. Survival worsened with increase in GGT levels semi-quantitatively. Increase in GGT levels was also found to significantly correlate with an increase in maximum tumor diameter from 4.5 to 7 cm, a 20-fold increase in serum alpha-fetoprotein level, an increase in tumor multifocality from 20 to 54% of patients, and a doubling in percent of patients with portal vein thrombosis (PVT) from 20 to 40%. Serum GGT levels also showed significant survival differences for patients with low AFP levels. A doublet combination of serum GGT with albumin levels was associated with higher hazard ratios in a Cox regression analysis, as compared with single parameter GGT. The combination parameter pair was also prognostically useful in the low-AFP patient subcohort and was associated with significant differences in patient tumor characteristics. CONCLUSIONS: Serum GGT levels and especially combination serum GGT plus albumin levels, were significantly associated both with HCC patient survival and tumor aggressiveness characteristics, regardless of AFP levels in a large Turkish cohort. This might be especially useful since the majority of HCC patients do not have elevated levels of AFP.

3.
J Transl Sci ; 7(3)2021 Jun.
Article in English | MEDLINE | ID: mdl-34457356

ABSTRACT

INTRODUCTION AND AIMS: Hepatocellular carcinoma (HCC) is a consequence of chronic liver disease, particularly from hepatitis B or C and increasingly from obesity and metabolic syndrome. Since lipids are an important component of cell membranes and are involved in cell signaling and tumor cell growth, we wished to evaluate the relationship between HCC patient plasma lipids and maximum tumor diameter and other indices of HCC human biology. METHODS: We examined prospectively-collected data from a multi-institutional collaborative Turkish HCC working group, from predominantly HBV-based patients, for plasma lipid profiles, consisting of triglycerides, total cholesterol, LDL-cholesterol (LDL) and HDL-cholesterol (HDL) and compared these with the associated patient maximum tumor diameter (MTD), portal vein thrombosis, alpha-fetoprotein (AFP) and also with patient survival. RESULTS: We found that both low HDL (p=0.0002) and high LDL (p=0.003) levels were significantly associated with increased MTD, as well as in a final multiple linear regression model on MTD. The combination of low HDL combined with high HDL levels were significant in a regression model on MTD, PVT and an HCC Aggressiveness Index (Odds Ratio 12.91 compared to an Odds Ratio of 1 for the reference). Furthermore, in a Cox regression model on death, the HDL plus LDL combination had a significantly higher Hazard Ratio than the reference category. CONCLUSIONS: Low plasma HDL, high plasma LDL and especially the combination, were significantly related to more aggressive HCC phenotype and the combination was significantly related to a higher Hazard Ratio for death.

4.
Acta Gastroenterol Belg ; 80(2): 263-270, 2017.
Article in English | MEDLINE | ID: mdl-29560692

ABSTRACT

BACKGROUND AND AIMS: The application of endoscopic retrograde cholangiopancreatography (ERCP) in the octogenarian population is limited. The aim of the study was to compare the clinical characteristics and outcomes of ERCP in octogenarian patients with non-octogenarian elderly patients. MATERIALS METHODS: A total of 1044 patients who underwent ERCP for the first time and are over the age of 65 were enrolled in this study. Data regarding demographic characteristics, medical history of patients, indications, technical success rate, final clinical diagnosis and complications were analyzed. 284 patients and 760 patients composed the octogenarian and non-octogenarian group, respectively. RESULTS: The mean ages in octogenarian and non-octogenarian groups were 83.99±3.85 and 71.50±4.27 years of age respectively. Both groups had similar values with regards to chronic concomitant diseases (96.6% vs. 96.5%). The most common indication of ERCP in the two groups was common bile duct stones. There was no significant difference in technical success and failure of cannulation in procedures of either group (p > 0,05). The duration of overall ERCP procedure was shorter in length in the non-octogenarian group in comparison to the octogenarian group (p = 0.004). The overall complication rate was similar in both groups (p > 0.177). The most common complication in either group was post-ERCP pancreatitis. CONCLUSIONS: ERCP is an effective and safe procedure in both octogenarian and non-octogenarian patients with naive papilla when performed by experienced endoscopists.


Subject(s)
Cholangiopancreatography, Endoscopic Retrograde , Gallstones/diagnosis , Pancreatitis , Age Factors , Aged , Aged, 80 and over , Cholangiopancreatography, Endoscopic Retrograde/adverse effects , Cholangiopancreatography, Endoscopic Retrograde/methods , Cholangiopancreatography, Endoscopic Retrograde/statistics & numerical data , Female , Humans , Male , Outcome and Process Assessment, Health Care , Pancreatitis/diagnosis , Pancreatitis/etiology , Risk Adjustment , Turkey
5.
Pak J Biol Sci ; 15(11): 506-16, 2012 Jun 01.
Article in English | MEDLINE | ID: mdl-24191624

ABSTRACT

Stress (abiotic and biotic) factors reflect and specify the plant morphology and called as "stress" and have negative effect(s) on growth, development, quality, quantity and can reduce average plant productivity by 65 to 87%, depending on the plants and stage(s) and also give various permanent or temporary damage(s) according to length of exposed period, violence/density, developmental stage, age, etc. Researches have revealed that despite the advanced technology levels the fundamental basis of stress have not been understood comprehensively. Firstly taken response(s) has/have not yet fully understood and secondly any "resistance" or "tolerance level of a variety/species" because of their complex structure(s). But, this point is clear that with the help or assistance of "multi-disciplinary" approaches, it will be able to get promising result(s) in near future. This review focuses some of the ecophysiological responses of plants to biotic and abiotic stresses.


Subject(s)
Plant Physiological Phenomena , Plants/metabolism , Stress, Physiological , Adaptation, Physiological , Ions , Light , Temperature
6.
Acta Anaesthesiol Scand ; 52(10): 1353-9, 2008 Nov.
Article in English | MEDLINE | ID: mdl-19025527

ABSTRACT

INTRODUCTION: The aim of the study is to evaluate the analgesic efficiency of perioperative magnesium sulphate infusion in patients undergoing laparoscopic cholecystectomy (LC). METHODS: In a randomized, double-blind trial study, 83 patients were divided into two groups. Group MT received 50 mg/kg i.v. magnesium sulphate in 100 ml of 0.9% normal saline and Group T received the same volume of isotonic saline during the intraoperative period. The cumulative post-operative tramadol consumption was measured to assess the analgesic effect using a patient-controlled analgesia device. Pain intensities at rest and while coughing were evaluated at 0, 2, 4, 8, 12, and 24 h post-operatively. RESULTS: The pain scores in Group MT were significantly lower than Group T at 0, 4, and 12 h post-operatively. The average of visual analogue scale at rest and during cough during 24 h post-operatively was found to be statistically significant between groups. The total dose of tramadol the 24-h period in Group MT and Group T was found to be 281.34 +/- 90.82 and 317.46 +/- 129.59, respectively. CONCLUSION: Per-operative 50 mg/kg magnesium sulphate infusion is effective in reducing post-operative pain in patients undergoing LC.


Subject(s)
Analgesics/administration & dosage , Cholecystectomy, Laparoscopic/adverse effects , Magnesium Sulfate/administration & dosage , Pain, Postoperative/drug therapy , Analgesia, Patient-Controlled , Double-Blind Method , Female , Humans , Infusions, Intravenous , Intraoperative Care/methods , Male , Middle Aged , Pain Measurement , Tramadol/administration & dosage , Treatment Outcome
7.
Physiol Res ; 55(1): 25-31, 2006.
Article in English | MEDLINE | ID: mdl-16083313

ABSTRACT

The purpose of this study is to analyze the protective effect of combining N-acetylcysteine (NAC) and hyberbaric oxygen (HBO) treatment in the lung tissue during acute pancreatitis. Sixty Sprague-Dawley male rats were randomly divided into five groups; Group I; Control group (n=12), Group II; pancreatitis group (n=12), Group III; pancreatitis + NAC treatment group (n=12), Group IV; pancreatitis + HBO treatment group (n=12), Group V; pancreatitis + HBO + NAC treatment group (n=12). HBO was applied postoperatively for 5 days, twice a day at 2.5 fold absolute atmospheric pressure for 90 min. Lung tissue was obtained for measuring malondialdehyde (MDA), superoxide dismutase (Cu/Zn-SOD) and glutathione peroxidase (GSH-Px) levels along with histopathological tissue examinations. This study showed that all three treated groups (HBO alone, NAC alone and combined HBO+NAC treatment) had pulmonary protective effects during acute necrotizing pancreatitis.


Subject(s)
Acetylcysteine/therapeutic use , Hyperbaric Oxygenation , Pancreatitis, Acute Necrotizing/therapy , Respiratory Distress Syndrome/prevention & control , Animals , Ceruletide , Glutathione Peroxidase/metabolism , Lung/drug effects , Lung/metabolism , Lung/pathology , Male , Malondialdehyde/metabolism , Oxidative Stress , Pancreatitis, Acute Necrotizing/etiology , Pancreatitis, Acute Necrotizing/pathology , Rats , Rats, Sprague-Dawley , Respiratory Distress Syndrome/etiology , Respiratory Distress Syndrome/pathology , Superoxide Dismutase/metabolism
8.
Int J Clin Pract ; 59(2): 206-9, 2005 Feb.
Article in English | MEDLINE | ID: mdl-15854198

ABSTRACT

The hepatitis G virus (HGV) and transfusion-transmitted virus (TTV) are recently defined hepatitis viruses that the pathogenic roles in liver diseases are still not clear. It has been well known that some hepatitis virus, such as hepatitis C, might have an affinity to pancreatic islet cells. To investigate the relationship between the newly defined hepatitis viruses and diabetes mellitus (DM), we studied the prevalence of TTV and HGV in a type 2 diabetic patient population. Serum samples of 60 patients with DM and 45 healthy volunteers as control were taken. HGV RNA and TTV DNA was investigated by polymerase chain reaction. HGV was detected in none of diabetic patients (0%) and only one in control group (2.2%). However, TTV DNA was detected in 16 patients with DM (26%) and in five controls (11%). TTV was more prevalent in diabetic patients, but the difference between groups was not statistically significant (p > 0.05). These results revealed that TTV is more common in diabetic patients than in controls. At present, we don't know if this result is only a coincidence or a sign of potential association between TTV and DM. Further studies are certainly needed to elucidate a potential relationship.


Subject(s)
Circoviridae Infections/complications , Diabetes Mellitus, Type 2/complications , Flaviviridae Infections/complications , GB virus C , Hepatitis, Viral, Human/complications , Torque teno virus , Adult , Case-Control Studies , Female , GB virus C/genetics , GB virus C/isolation & purification , Humans , Male , Middle Aged , RNA, Viral/blood , Torque teno virus/genetics , Torque teno virus/isolation & purification
9.
Acta Chir Belg ; 104(3): 335-7, 2004 Jun.
Article in English | MEDLINE | ID: mdl-15285550

ABSTRACT

The Muir-Torre syndrome is characterized by cutaneous neoplasms and visceral malignancies. At least one sebaceous adenoma, epithelioma or carcinoma and at least one internal malignancy are required to make a reliable diagnosis. According to medical literature only two cases of Muir-Torre syndrome with jejunal carcinoma have been reported to date and there is no reported case with intestinal obstruction. Here, we report an unusual case of jejunal carcinoma presenting with ileus.


Subject(s)
Ileus/etiology , Jejunal Diseases/etiology , Jejunal Neoplasms/diagnosis , Neoplasms, Multiple Primary/diagnosis , Skin Neoplasms/diagnosis , Humans , Jejunal Neoplasms/complications , Male , Middle Aged , Neoplasms, Multiple Primary/complications , Skin Neoplasms/complications , Syndrome
10.
Int J Tuberc Lung Dis ; 7(8): 771-6, 2003 Aug.
Article in English | MEDLINE | ID: mdl-12921154

ABSTRACT

SETTING: Pulmonary department of a university hospital in Ankara, Turkey. OBJECTIVE: To investigate the usefulness of neopterin in pulmonary tuberculosis (PTB) as a rapid diagnostic tool. DESIGN: Neopterin concentrations in bronchoalveolar lavage fluid (BAL), serum and urine were measured in patients with PTB, with lung cancer and with pneumonia and in a healthy control group. RESULTS: In the BAL of PTB patients, serum and urine levels of neopterin were significantly higher than all the other groups (P < 0.001). Compared with the lung cancer group, PTB patients had higher neopterin in BAL and urine (P < 0.05). The PTB group had higher levels not only in BAL and urine, but also in serum, than the pneumonia group (P < 0.05). Compared with the pneumonia group and the healthy controls, neopterin levels in serum and urine were significantly higher in the lung cancer group (P < 0.05). In the PTB group, patients with moderately advanced PTB according to radiographic extent had higher levels of urine neopterin than patients with minimal disease (P = 0.01). CONCLUSION: Neopterin levels in BAL, serum and particularly in urine may reflect PTB activity before exact diagnosis of the disease by culture results, and correlates with radiological extent.


Subject(s)
Neopterin/urine , Tuberculosis, Pulmonary/diagnosis , Tuberculosis, Pulmonary/urine , Adult , Aged , Bronchoalveolar Lavage Fluid/chemistry , Humans , Lung Neoplasms/blood , Lung Neoplasms/urine , Male , Middle Aged , Plasma/chemistry , Pneumonia/blood , Pneumonia/urine , Tuberculosis, Pulmonary/blood , Urine/chemistry
11.
New Microbiol ; 26(3): 243-8, 2003 Jul.
Article in English | MEDLINE | ID: mdl-12901419

ABSTRACT

Hepatitis G virus (HGV) is transfusion-transmissible and has a global distribution. However, its frequency and clinical impact have not been well established in extrahepatic cancer patients. In this study, we determined the prevalence of HGV RNA positivity, and its relationship with history of transfusion, amount of transfusion, age and sex in patients with hematological and solid malignancies in Southeastern Turkey. Sixty-one patients (35 males and 26 females) followed up for various malignancies and 60 healthy subjects were included in the study. HGV RNA was investigated by the reverse transcription polymerase chain reaction. HGV RNA was detected in none of the patients with cancer (0%) and only one person (1.6%) in the control group. There was no difference between the groups. This observation indicates that the prevalence of HGV is very low in cancer patients and healthy people in our geographical area. In addition, the role of HGV in the pathogenesis of extrahepatic malignancies seems insignificant.


Subject(s)
Flaviviridae Infections/complications , GB virus C/isolation & purification , Hepatitis, Viral, Human/complications , Neoplasms/virology , Female , Flaviviridae Infections/virology , GB virus C/genetics , Hepatitis, Viral, Human/virology , Humans , Male , Middle Aged , Neoplasms/epidemiology , Prevalence , RNA, Viral/chemistry , RNA, Viral/genetics , Reverse Transcriptase Polymerase Chain Reaction , Turkey/epidemiology
12.
New Microbiol ; 25(4): 399-404, 2002 Oct.
Article in English | MEDLINE | ID: mdl-12437218

ABSTRACT

Hepatitis G virus (HGV) may cause acute and chronic infection in humans but its role in liver injury and chronic hepatitis is unclear. In this study, the prevalence of HGV was investigated in patients with chronic liver diseases in an endemic area of hepatitis B and C virus. Sixty patients with chronic liver diseases, 11 with hepatitis B virus, 44 with hepatitis C virus and 5 patients with hepatitis of unknown etiology and 60 healthy blood donors as the control were included in the study. HGV RNA was investigated by the reverse transcription polymerase chain reaction. HGV RNA was detected in none of the patients with chronic liver diseases (0%) and only one patient (1.6%) in the control group. There was no difference between the groups. This observation indicated that the prevalence of HGV is very low in patients with chronic liver diseases and healthy people in our geographical area. The role of this novel virus in the pathogenesis of chronic liver injury seems insignificant.


Subject(s)
Flaviviridae Infections/epidemiology , GB virus C , Hepatitis, Viral, Human/epidemiology , Liver Diseases/virology , Adult , Chronic Disease , Female , Flaviviridae Infections/etiology , Hepatitis B/virology , Hepatitis C/virology , Hepatitis, Viral, Human/etiology , Humans , Liver Diseases/complications , Male , Middle Aged , Prevalence , RNA, Viral/blood
13.
New Microbiol ; 25(4): 463-8, 2002 Oct.
Article in English | MEDLINE | ID: mdl-12437226

ABSTRACT

Transfusion-transmitted virus (TTV) is a recently discovered transfusion-transmissible DNA virus. Its frequency and clinical impact has not been established in cancer patients in Turkey. In this study, we determined the prevalence of TTV DNA positivity, and its relationship with history of transfusion, amount of transfusion, age and sex in patients with hematological and solid malignancies. Sixty-one patients (35 male and 26 female) followed up for various malignancies and 45 healthy subjects were included in the study. ITV DNA was assayed by the polymerase chain reaction (PCR). TTV DNA was detected in 18 of 61 patients (29.5%) and in 5 of 45 control subjects (11.1%). In cancer patients, the prevalence of TTV DNA positivity was higher to comparison with control group. In addition, the prevalence of TTV DNA positivity was significantly higher in 22 patients who had a history of blood transfusion in the last 6 months than 39 patients who had no current or past history of transfusion (40.9% vs 23.0% respectively). These results suggest that the prevalence of TTV DNA is high and the parenteral route is an important mode of transmission for TTV in cancer patients. In addition, the high prevalence and persistence of TTV in cancer patients with parenteral risk exposure could be related to the immunodeficiency due to cancer and high viral loads by parenteral route.


Subject(s)
DNA Virus Infections/epidemiology , Neoplasms/virology , Torque teno virus/isolation & purification , Transfusion Reaction , Adult , DNA Virus Infections/blood , DNA Virus Infections/complications , DNA Virus Infections/transmission , DNA Viruses/genetics , DNA Viruses/isolation & purification , DNA, Viral/blood , Female , Humans , Immunocompromised Host , Infusions, Parenteral , Male , Middle Aged , Neoplasms/complications , Neoplasms/therapy , Polymerase Chain Reaction , Prevalence , Risk Factors , Turkey/epidemiology , Viral Load
14.
Arzneimittelforschung ; 51(10): 839-42, 2001 Oct.
Article in English | MEDLINE | ID: mdl-11715637

ABSTRACT

In this study, by starting from ethyl 4-amino-2,3-dihydro-3-methyl-2-thioxothiazole-5-carboxylate (1), the compounds having 2,3-dihydro-3-methyl-5-mercapto-6-methyl/ethyl-2- thioxothiazolo[4,5-d]pyrimidin-7(6H)-one (2a, 2b) structure and their 5-(4'-nonsubstituted/-substituted benzoylmethyl)thio derivatives (3a-h) were synthesized. The chemical structures of the compounds were proved by IR, 1H-NMR and elemental analysis data. In vitro antimicrobial activities of the synthesized compounds were investigated against some bacteria and yeasts using the microdilution method. In view of the antimicrobial activity results, a significant inhibitory effect was observed only for compound 2a against Gram-positive bacteria and yeasts, whereas the other compounds had no remarkable activity against the tested microorganisms.


Subject(s)
Anti-Infective Agents/chemical synthesis , Anti-Infective Agents/pharmacology , Antifungal Agents/chemical synthesis , Antifungal Agents/pharmacology , Bacteria/drug effects , Fungi/drug effects , Pyrimidines/chemical synthesis , Pyrimidines/pharmacology , Thiazoles/chemical synthesis , Thiazoles/pharmacology , Anti-Bacterial Agents , Candida/drug effects , Indicators and Reagents , Microbial Sensitivity Tests , Spectrophotometry, Infrared
15.
Arzneimittelforschung ; 50(12): 1115-9, 2000 Dec.
Article in English | MEDLINE | ID: mdl-11190778

ABSTRACT

In this study, by starting from ethyl 4-amino-2,3-dihydro-3-phenyl-2-thioxothiazole-5-carboxylate (1), three compounds having 2,3-dihydro-3-phenyl-5-mercapto-6-alkyl/phenyl-2-thioxothiazolo[4,5- d]pyrimidin-7(6H)-one (2a-c) structure and their 5-(4'-nonsubstituted/-substituted benzoylmethyl)thio derivatives (3a-l) were synthesized. The antimicrobial activities of the synthesized compounds were investigated against some bacteria and fungi using the microdilution method. 2,3-Dihydro-3,6-diphenyl-5-(4'-bromobenzoylmethyl)thio-2-thioxothiazolo [4,5-d]pyrimidin-7(6H) one (3k) possessing remarkable activity against Gram-positive bacteria and yeast like fungi was found to be the most active compound in this series.


Subject(s)
Anti-Infective Agents/chemical synthesis , Anti-Bacterial Agents , Anti-Infective Agents/pharmacology , Fungi/drug effects , Gram-Negative Bacteria/drug effects , Gram-Positive Bacteria/drug effects , Magnetic Resonance Spectroscopy , Microbial Sensitivity Tests , Spectroscopy, Fourier Transform Infrared
16.
Arzneimittelforschung ; 48(6): 658-62, 1998 Jun.
Article in English | MEDLINE | ID: mdl-9689423

ABSTRACT

Ten new compounds having 7-[(2,4-pentanedione-3-yl)alkyl]- and 7-[(3,5-dimethylisoxazole-4-yl)alkyl]-3,7-dihydro-1,3-dimethyl-1H- purine-2, 6-dione structures were synthesized and their bronchodilator activities investigated using the method based on inhibition of acetylcholine and histamine-induced contractions in guinea pig trachea. None of the compounds were effective on acetylcholine-induced contractions. However, the compounds 4d, 4e, 5d and 5c were potent inhibitors of the bronchospasm induced by histamine, whereas the others (4b, 4c, 5b and 5c) were weak inhibitors.


Subject(s)
Bronchodilator Agents/chemical synthesis , Bronchodilator Agents/pharmacology , Isoxazoles/pharmacology , Theophylline/analogs & derivatives , Theophylline/pharmacology , Acetylcholine/antagonists & inhibitors , Acetylcholine/pharmacology , Animals , Bronchi/drug effects , Chemical Phenomena , Chemistry, Physical , Female , Guinea Pigs , Histamine/pharmacology , Histamine Antagonists/pharmacology , In Vitro Techniques , Isoxazoles/chemical synthesis , Male , Muscle Contraction/drug effects , Muscle, Smooth/drug effects , Theophylline/chemical synthesis
17.
Arzneimittelforschung ; 48(1): 39-42, 1998 Jan.
Article in English | MEDLINE | ID: mdl-9522029

ABSTRACT

Some novel 7-substituted theophylline derivatives have been investigated for quantitative structure-activity relationship (QSAR). For this purpose, their bronchodilatory activities (in vitro), which were examined by the inhibition of acetylcholine induced contraction in tracheae isolated from guinea pigs, have been correlated with various quantum chemical and physicochemical parameters.


Subject(s)
Bronchodilator Agents/pharmacology , Theophylline/analogs & derivatives , Theophylline/pharmacology , Acetylcholine/pharmacology , Animals , Bronchodilator Agents/chemistry , Chemical Phenomena , Chemistry, Physical , Guinea Pigs , In Vitro Techniques , Male , Muscle, Smooth/drug effects , Structure-Activity Relationship , Theophylline/chemistry
18.
Boll Chim Farm ; 135(11): 648-52, 1996 Dec.
Article in English | MEDLINE | ID: mdl-9138461

ABSTRACT

The synthesis of a series of thiazolo[3,2-a]pyrimidine derivatives were described. The structures of the compounds were elucidated by IR, 1H-NMR, 13C and elementary analysis. The compounds were evaluated for their calcium antagonistic activities using nifedipine as standard compound. All of the compounds were found to be less potent than nifedipine.


Subject(s)
Calcium Channel Blockers/chemical synthesis , Pyrimidines/chemical synthesis , Thiazoles/chemical synthesis , Animals , Calcium Channel Blockers/pharmacology , Female , Guinea Pigs , Ileum/drug effects , Ileum/metabolism , In Vitro Techniques , Male , Nifedipine/pharmacology , Pyrimidines/pharmacology , Thiazoles/pharmacology
19.
Farmaco ; 51(8-9): 589-94, 1996.
Article in English | MEDLINE | ID: mdl-8930112

ABSTRACT

Ten new compounds having 3-[(2-naphthyloxy)alkyl]-2,4-pentanedione and 4-[(2-naphthyloxy)alkyl]-3,5-dimethylisoxazole structures were synthesized and their cytotoxicities and antiviral activities investigated. 3-[6-(2-Naphthyloxy)hexyl]-2,4-pentandione possessing inhibitory activity on the replication of both adenovirus type 5 and poliovirus type 1 at 20 micrograms/ml was the most active compound in the series.


Subject(s)
Antiviral Agents/chemical synthesis , Isoxazoles/chemical synthesis , Antiviral Agents/pharmacology , Humans , Isoxazoles/pharmacology , Tumor Cells, Cultured
20.
Pharmazie ; 47(9): 687-8, 1992 Sep.
Article in English | MEDLINE | ID: mdl-1475316

ABSTRACT

Some new thiazolo[3,2-a]pyrimidine derivatives were prepared refluxing 2-thioxo-1,2,3,4-tetrahydropyrimidine derivatives with phenacyl bromide in glacial acetic acid. Calcium antagonistic activities of these compounds were evaluated in K(+)-depolarized rat aorta, using nifedipine as reference compound.


Subject(s)
Calcium Channel Blockers/chemical synthesis , Pyrimidines/chemical synthesis , Thiazoles/chemical synthesis , Animals , Calcium Channel Blockers/pharmacology , In Vitro Techniques , Isradipine/metabolism , Magnetic Resonance Spectroscopy , Male , Muscle Relaxation/drug effects , Muscles/drug effects , Muscles/metabolism , Rats
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