71 research outputs found
Novel quinazoline and acetamide derivatives as safe anti-ulcerogenic agent and anti-ulcerative colitis activity
Two novel quinazoline derivatives named as; 3-[(4-hydroxy-3-methoxy-benzylidene)-amino]-2-p-tolyl3H-quinazolin-4-one
(5) and 2-p-Tolyl-3-[3,4,5-trimethoxy-benzylidene-amino]-3H-quinazolin-4-one
(6) in addition to one acetamide derivative named as 2-(2-Hydroxycarbonylphenylamino)-N-(4-
aminosulphonylphenyl) 11 were synthesized, and evaluated for their anti-ulcerogenic & AntiUlcerative
colitis activities.
All of the three compounds showed curative activity against acetic acid induced ulcer model at a dose
of 50 mg/kg, they produced 65%, 85% & 57.74% curative ratio for compounds 5, 6 & 11 respectively. The
effect of the tested compounds 5, 6 & 11 at dose 50 mg/kg were significantly (P < 0.01) more effective
than dexamesathone (0.1 mg/kg) in reducing all parameters.
Compounds showed curative activity of for peptic ulcer (induced by absolute alcohol (at a dose of 50
mg/kg, it produced Curative of control ulcer 56.00%, 61.70% & 87.1% for compounds 5, 6 & 11 respectively
at dose 50 mg/kg, while the standard drug (Omeprazole 20 mg/kg) produced 33.3%. In both tests, the
activity of our target compounds were higher than the standard drugs used for treatment of peptic ulcer
and ulcerative colitis. No side effects were reported on liver and kidney functions upon prolonged oral
administration of this compounds
Anti-ulcerogenic and anti-ulcerative colitis (UC) activities of seven amines derivatives
The Novel target compounds (CP-1-7) were synthesized and tested at doses up to 1000mg/kg for their entitled activities. They exerted promising results without any behavioral changes and mortality in mice. Therefore, according to the results obtained in our study, it could be categorized as highly safe agents for treating UC since substances possessing LD50 higher than 50mg/kg are considered nontoxic. They also possessed a potent anti-ulcerogenic activity with different potentials. The most effective compound was CP-4, it produced 97.7% ulcer protection of control followed by CP-3, which produced 90.3% protection, while the standard drug ranitidine (100mg/kg) produced 49.2% protection. Compound CP-1 showed lowest activity among the current series, it produced 55.5% protection. The target compounds were significantly more effective than the standard in reducing ulcer index. The anti-ulcerative colitis activity was tested using acetic acid induced colitis model. The curative effect of the tested compounds at a dose of 50mg/kg oral administration on rats showed a potent anti-ulcerative colitis activity with different potentials. They induced a significant decrease in ulcer score, ulcer area, ulcer index and weight/length of the colon specimens.The percent protection of control colitis ranged from 66.8% for CP-7 to 22.3% for CP-5; however the percent protection for dexamesathone (0.1. mg/kg) was 59.3%. The effect of the tested compounds CP-7 and CP-3 at dose 50. mg/kg were significantly more effective than dexamesathone (0.1. mg/kg) in reducing all parameters.Liver functions were not affected as there is no effect on the activity of both AST and ALT in animals that received the compounds, so the compounds didn't reveal hepatotoxic manifestation. Although, the results on kidney functions showed that, CP-1 slightly elevated blood urea concentration and CP-3 & CP-4 slightly elevated serum creatinine; no apparent nephrotoxic manifestations were recorded
Novel essential amino acid-sulfanilamide hybrid as safe anti-ulcerogenic agent with anti-helicobacter pylori activity
A novel and safe essential amino acid (Leucine) incorporating sulfanilamide was synthesized, and evaluated for its anti-ulcerogenic activity and in vitro anti-Helicobacter pylori activity. The new molecule showed a dose dependent activity against absolute ethanol-induced ulcer in rats, it produced percent protection of control ulcer by 66.7 at dose 100 mg/kg. In addition it showed a potent anti-Helicobacter pylori activity in vitro against 7 clinically isolated strains. The minimum inhibitory concentration (MIC) ranged from 12.5 to 50 Îźg/ml. The preliminary safety studies and toxicity profile are optimistic and encouraging
Synthesis 4-[2-(2-mercapto-4-oxo-4H-quinazolin-3-yl)-ethyl]-benzenesulfonamides with subnanomolar carbonic anhydrase II and XII inhibitory properties
Condensation of substituted anthranilic acids with 4-isothiocyanatoethyl-benzenesulfonamide led to series
of heterocyclic benzenesulfonamides incorporating 2-mercapto-quinazolin-4-one tails. These sulfonamides
were investigated as inhibitors of the human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms hCA I
and II (cytosolic isozymes), as well as hCA XII (a transmembrane, tumor-associated enzyme also involved
in glaucoma-genesis). The new sulfonamides acted as medium potency inhibitors of hCA I (KIs of 28.5â
2954 nM), being highly effective as hCA II (KIs in the range of 0.62â12.4 nM) and XII (KIs of 0.54â
7.11 nM) inhibitors. All substitution patterns present in these compounds (e.g., halogens, methyl and
methoxy moieties, in positions 6, 7 and/or 8 of the 2-mercapto-quinazolin-4-one ring) led to highly effective
hCA II/XII inhibitors. These compounds should thus be of interest as preclinical candidates in
pathologies in which the activity of these enzymes should be inhibited, such as glaucoma (CA II and
XII as targets) or some tumors in which the activity of isoforms CA II and XII is dysregulated
Spatial, temporal, and demographic patterns in prevalence of chewing tobacco use in 204 countries and territories, 1990-2019: A systematic analysis from the Global Burden of Disease Study 2019
Background: Chewing tobacco and other types of smokeless tobacco use have had less attention from the global health community than smoked tobacco use. However, the practice is popular in many parts of the world and has been linked to several adverse health outcomes. Understanding trends in prevalence with age, over time, and by location and sex is important for policy setting and in relation to monitoring and assessing commitment to the WHO Framework Convention on Tobacco Control. Methods: We estimated prevalence of chewing tobacco use as part of the Global Burden of Diseases, Injuries, and Risk Factors Study 2019 using a modelling strategy that used information on multiple types of smokeless tobacco products. We generated a time series of prevalence of chewing tobacco use among individuals aged 15 years and older from 1990 to 2019 in 204 countries and territories, including age-sex specific estimates. We also compared these trends to those of smoked tobacco over the same time period. Findings: In 2019, 273¡9 million (95% uncertainty interval 258¡5 to 290¡9) people aged 15 years and older used chewing tobacco, and the global age-standardised prevalence of chewing tobacco use was 4¡72% (4¡46 to 5¡01). 228¡2 million (213¡6 to 244¡7; 83¡29% [82¡15 to 84¡42]) chewing tobacco users lived in the south Asia region. Prevalence among young people aged 15â19 years was over 10% in seven locations in 2019. Although global age-standardised prevalence of smoking tobacco use decreased significantly between 1990 and 2019 (annualised rate of change: â1¡21% [â1¡26 to â1¡16]), similar progress was not observed for chewing tobacco (0¡46% [0¡13 to 0¡79]). Among the 12 highest prevalence countries (Bangladesh, Bhutan, Cambodia, India, Madagascar, Marshall Islands, Myanmar, Nepal, Pakistan, Palau, Sri Lanka, and Yemen), only Yemen had a significant decrease in the prevalence of chewing tobacco use, which was among males between 1990 and 2019 (â0¡94% [â1¡72 to â0¡14]), compared with nine of 12 countries that had significant decreases in the prevalence of smoking tobacco. Among females, none of these 12 countries had significant decreases in prevalence of chewing tobacco use, whereas seven of 12 countries had a significant decrease in the prevalence of tobacco smoking use for the period. Interpretation: Chewing tobacco remains a substantial public health problem in several regions of the world, and predominantly in south Asia. We found little change in the prevalence of chewing tobacco use between 1990 and 2019, and that control efforts have had much larger effects on the prevalence of smoking tobacco use than on chewing tobacco use in some countries. Mitigating the health effects of chewing tobacco requires stronger regulations and policies that specifically target use of chewing tobacco, especially in countries with high prevalence. Funding: Bloomberg Philanthropies and the Bill & Melinda Gates Foundation
Use of SMS texts for facilitating access to online alcohol interventions: a feasibility study
A41 Use of SMS texts for facilitating access to online alcohol interventions: a feasibility study
In: Addiction Science & Clinical Practice 2017, 12(Suppl 1): A4
Search for a W ' boson decaying to a muon and a neutrino in pp collisions at âs =7 TeV
This is the Pre-Print version of the Article. The official published version can be accessed from the link below - Copyright @ 2011 ElsevierA new heavy gauge boson, W', decaying to a muon and a neutrino, is searched for in pp collisions at a centre-of-mass of 7 TeV. The data, collected with the CMS detector at the LHC, correspond to an integrated luminosity of 36 inverse picobarns. No significant excess of events above the standard model expectation is found in the transverse mass distribution of the muon-neutrino system. Masses below 1.40 TeV are excluded at the 95% confidence level for a sequential standard-model-like W'. The W' mass lower limit increases to 1.58 TeV when the present analysis is combined with the CMS result for the electron channel.This work is supported by the FMSR (Austria); FNRS and FWO (Belgium); CNPq, CAPES, FAPERJ, and FAPESP (Brazil); MES (Bulgaria); CERN; CAS, MoST, and NSFC (China); COLCIENCIAS (Colombia); MSES (Croatia); RPF (Cyprus); Academy of Sciences
and NICPB (Estonia); Academy of Finland, ME, and HIP (Finland); CEA and CNRS/IN2P3
(France); BMBF, DFG, and HGF (Germany); GSRT (Greece); OTKA and NKTH (Hungary); DAE and DST (India); IPM (Iran); SFI (Ireland); INFN (Italy); NRF and WCU (Korea); LAS (Lithuania); CINVESTAV, CONACYT, SEP, and UASLP-FAI (Mexico); PAEC (Pakistan); SCSR
(Poland); FCT (Portugal); JINR (Armenia, Belarus, Georgia, Ukraine, Uzbekistan); MST and MAE (Russia); MSTD (Serbia); MICINN and CPAN (Spain); Swiss Funding Agencies (Switzerland); NSC (Taipei); TUBITAK and TAEK (Turkey); STFC (United Kingdom); DOE and NSF (USA)
Observation of a new Xi(b) baryon
The first observation of a new b baryon via its strong decay into Xi(b)^-
pi^+ (plus charge conjugates) is reported. The measurement uses a data sample
of pp collisions at sqrt(s) = 7 TeV collected by the CMS experiment at the LHC,
corresponding to an integrated luminosity of 5.3 inverse femtobarns. The known
Xi(b)^- baryon is reconstructed via the decay chain Xi(b)^- to J/psi Xi^- to
mu^+ mu^- Lambda^0 pi^-, with Lambda^0 to p pi^-. A peak is observed in the
distribution of the difference between the mass of the Xi(b)^- pi^+ system and
the sum of the masses of the Xi(b)^- and pi^+, with a significance exceeding
five standard deviations. The mass difference of the peak is 14.84 +/- 0.74
(stat.) +/- 0.28 (syst.) MeV. The new state most likely corresponds to the
J^P=3/2^+ companion of the Xi(b).Comment: Submitted to Physical Review Letter
Measurement of the charge ratio of atmospheric muons with the CMS detector
This is the pre-print version of this Article. The official published version can be accessed from the link below - Copyright @ 2010 ElsevierWe present a measurement of the ratio of positive to negative muon fluxes from cosmic ray interactions in the atmosphere, using data collected by the CMS detector both at ground level and in the underground experimental cavern at the CERN LHC. Muons were detected in the momentum range from 5 GeV/c to 1 TeV/c. The surface flux ratio is measured to be 1.2766 \pm 0.0032(stat.) \pm 0.0032 (syst.), independent of the muon momentum, below 100 GeV/c. This is the most precise measurement to date. At higher momenta the data are consistent with an increase of the charge ratio, in agreement with cosmic ray shower models and compatible with previous measurements by deep-underground experiments
Measurements of inclusive W and Z cross sections in pp collisions at root s=7 TeV
This is the pre-print version of the Published Article, which can be accessed from the link below - Copyright @ 2011 Springer VerlagMeasurements of inclusive W and Z boson production cross sections in pp collisions at sqrt(s)=7 TeV are presented, based on 2.9 inverse picobarns of data recorded by the CMS detector at the LHC. The measurements, performed in the electron and muon decay channels, are combined to give sigma(pp to WX) times B(W to muon or electron + neutrino) = 9.95 \pm 0.07(stat.) \pm 0.28(syst.) \pm 1.09(lumi.) nb and sigma(pp to ZX) times B(Z to oppositely charged muon or electron pairs) = 0.931 \pm 0.026(stat.) \pm 0.023(syst.) \pm 0.102(lumi.) nb. Theoretical predictions, calculated at the next-to-next-to-leading order in QCD using recent parton distribution functions, are in agreement with the measured cross sections. Ratios of cross sections, which incur an experimental systematic uncertainty of less than 4%, are also reported
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