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About the Flu

Flu refers to illnesses caused by a number of different influenza viruses. Flu can cause a range of symptoms and effects, from mild to lethal.
Two strains of flu, seasonal flu and the H1N1 (Swine) flu, are currently circulating in the United States. A third, highly lethal H5N1 (Bird) flu is being closely tracked overseas.
Most healthy people recover from the flu without problems, but certain people are at high risk for serious complications.

Extensive efforts are underway to track and monitor the spread of all flu viruses. In the U.S., epidemiologists at the Centers for Disease Control (CDC) are working with states to collect, compile and analyze reports of flu outbreaks. More on the current situation.
Flu symptoms may include fever, coughing, sore throat, runny or stuffy nose, headaches, body aches, chills and fatigue. In H1N1 flu infection, vomiting and diarrhea may also occur.
Annual outbreaks of the seasonal flu usually occur during the late fall through early spring. Most people have natural immunity, and a seasonal flu vaccine is available. In a typical year, approximately 5 to 20 percent of the population gets the seasonal flu and approximately 36,000 flu-related deaths are reported.

 

 

 

 

 

This year, the H1N1 flu virus(Pharmaceutical Intermediates ) may cause a more dangerous flu season with a lot more people getting sick, being hospitalized and dying than during a regular flu season. H1N1 is a new virus first seen in the United States. It is contagious and spreads from person to person. Like seasonal flu, illness in people with H1N1 can vary from mild to severe.

A flu pandemic occurs when a new influenza A virus emerges for which there is little or no immunity in the human population; the virus causes serious illness and spreads easily from person-to-person worldwide. On June 11, 2009, the World Health Organization  (WHO) declared that a global pandemic of H1N1 flu is underway.

H5N1 (Bird) flu is an influenza A virus subtype that is highly contagious among birds. Rare human infections with the H5N1 (Bird) flu virus have occurred. The majority of confirmed cases have occurred in Asia, Africa, the Pacific, Europe and the Near East. Currently, the United States has no confirmed human H5N1 (Bird) flu infections, but H5N1 (Bird) flu remains a serious concern with the potential to cause a deadly pandemic.

 

 

from:timepharm

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The first approved for treatment of HIV

Zidovudine or azidothymidine (AZT) is Pharmaceutical Intermediates , the first approved for treatment of HIV. Zidovudine was the first drug approved for the treatment of AIDS and HIV infection. Like other reverse transcriptase inhibitors, AZT works by inhibiting the action of reverse transcriptase, the enzyme that HIV uses to make a DNA copy of its RNA. The viral double-stranded DNA is subsequently spliced into the DNA of a target cell, where it is called a provirus. Jerome Horwitz of Barbara Ann Karmanos Cancer Institute and Wayne State University School of Medicine first synthesized AZT in 1964, under a US National Institutes of Health (NIH) grant.

It was originally intended to anti-live cancer , but failed to show efficacy and had an unacceptably high side effect profile. In 1985, when Samuel Broder, Hiroaki Mitsuya, and Robert Yarchoan, three scientists in the National Cancer Institute (NCI), collaborating with Janet Rideout and several other scientists at Burroughs Wellcome (now GlaxoSmithKline), started working on it as an AIDS drug . After showing that this drug was an effective agent against HIV in vitro, the team conducted the initial clinical trial that provided evidence that it could increase CD4 counts in AIDS patients.

AZT does not destroy the HIV infection, but only delays the progression of the disease and the replication of virus, even at very high doses. During prolonged AZT treatment HIV has the ability to gain an increased resistance to AZT by mutation of the reverse transcriptase. A study showed that AZT could not impede the resumption of virus production, and eventually cells treated with AZT produced viruses as much as the untreated cells. So as to slow the development of resistance, it is generally recommended that AZT be given in combination with another reverse transcriptase inhibitor and an antiretroviral from another group, such as a protease inhibitor or a non-nucleoside reverse transcriptase inhibitor.


AZT may be used in combination with other antiretroviral medications to substantially reduce the risk of HIV infection following a significant exposure to the virus (such as a needle-stick injury involving blood or body fluids from an individual known to be infected with HIV). AZT is also recommended as part of a regimen to prevent mother-to-child transmission of HIV during pregnancy, labor and delivery. With no treatment, approximately 25% of infants whose mothers are infected with HIV will become infected.

AZT has been shown to reduce this risk to approximately 8% when given in a three-part regimen during pregnancy, delivery and to the infant for 6 weeks after birth. Use of appropriate combinations of antiretroviral medications and cesarean section when necessary can further reduce mother-child transmission of HIV to 1-2%. Common side effects of AZT include nausea, headache, changes in body fat, and discoloration of fingernails and toenails. More severe side effects include anaemia and bone marrow suppression. These unwanted side effects might be caused by the sensitivity of the γ-DNA polymerase in the cell mitochondria. AZT has been shown to work additively or synergistically with many anti-HIV agents; however, acyclovir and ribavirin decrease the antiviral effect of AZT.
Formal Chemical Name (IUPAC)
1-((2R,4S,5S)-4-azido-5-(hydroxymethyl)tetrahydrofuran-2-yl)-5-methylpyrimidine-2,4(1H,3H)-dione

 

 

from:timepharm

Tags: AIDS drug  
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The Link Between Obesity And Cancer

An enzyme that normally helps break down stored fats becomes highly active in some cancer cells and makes them more likely to spread, researchers have found.


When the enzyme, called monoacylglycerol lipase (MAGL), goes into overdrive in cancer cells, it breaks down stored fats to produce large amounts of free fatty acids, which are the building blocks of cell membranes and of fatty molecules that serve as signals between cells. These free fatty acids then produce other smaller molecules that promote cancer growth and progression, the study authors noted.
The finding that stored fats in cancer cells can cause them to become more aggressive offers a possible explanation for the reported link between obesity and cancer, according to the researchers at the Scripps Research Institute in California. They also said MAGL may offer a new target for treating aggressive forms of cancer or for preventing cancer progression.


“Historically, research has focused on the mechanisms leading to cancer formation, and therapies have focused on taking out cancer cells. But here we were looking for pathways that lead to cancer aggressiveness,” corresponding author Benjamin Cravatt, chair of the Scripps Research Department of Chemical Physiology, said in a news release.


He noted that people who eat high-fat foods are constantly introducing free fatty acids into their bodies.
“We have shown that cancer cells have their own pathways to produce free fatty acids, which will enable them to become more aggressive. Less malignant cancer cells do not appear to have adopted an autonomous pathway to increase their own pools of free fatty acids. Thus, taking free fatty acids from the diet could assist these cells in developing a more malignant phenotype,” Cravatt said.
The study was published in the Jan. 8 issue of the journal Cell.

 

N-Acetyl-D-glactosamine      CAS: 1811-31-0

 

Description: N-Acetyl-D-galactosamine
Synonyms: 2-Acetamido-2-deoxy D-galactose; D-GalNAC; N-Acetylchondrosamine
CAS No.: 1811-31-0
Assay: ≥97%
Appearance: White crystalline powder
molecular: C8H15NO6

 

from:timepharm|anti cancer

 

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HIV&anti-HIV

The human immunodeficiency virus (HIV) attacks the body's immune system. A healthy immune system is what keeps you from getting sick.
Because HIV damages your immune system, you are more likely to get sick from bacteria and viruses. It is also harder for your body to fight off these infections when you do get them, so you may have trouble getter better. HIV is the condition that causes acquired immunodeficiency syndrome (AIDS ).

HIV can only be passed from person to person through body fluids, such blood, semen and vaginal fluid. Children born to infected mothers can also become infected during pregnancy. The most common ways HIV is passed are:
1.By having unprotected anal, vaginal or oral sex with an infected person.
2.By sharing needles and syringes for injecting drugs with an infected person.

What happens after a person gets HIV?
After being infected with HIV, your body works hard to attack the virus. With your body fighting, the virus can't make as many copies of itself. Even though you still have HIV, you'll begin to look well and feel well again. The usual blood tests will be normal.

However, during this time, the virus is still attacking your lymph nodes. Lymph nodes are the centers of your body's immune system. The virus may also attack your brain tissue and slowly cause damage there.
Over 10 to 15 years, HIV kills so many CD4 cells that your body can no longer fight off infections. When your CD4 cell count is 200 or less per mL, you have AIDS (a normal count is 600 to 1000). Once you have AIDS (which stands for acquired immunodeficiency syndrome), you can easily catch many serious infections.

Now, Here will introduce  4-Nitrophenyl Chloroformate (CAS:7693-46-1 ) to you.

 


This is used as a pharmaceutical Intermediates of anti-HIV. If you are interested in this pharmaceutical Intermediates, you can have more information at www.timepharm.com .

 

from:News|timepharm

Tags: anti-HIV  
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carboxylic acid esters were performed with Bis(4-nitrophenyl) carbonate HPLC 99%

A novel beta-cyclodextrin dimer, 1,10-phenanthroline-2,9-dimethyl-bridged-bis(6-monoammonio-beta-cyclodextrin) (phenBisCD, L), was synthesized. Its zinc complex (ZnL) has been prepared, characterized, and applied as a new catalyst for diester hydrolysis. The formation constant (logK(ML)=9.56+/-0.01) of the complex and deprotonation constant (pK(a)=8.18+/-0.04) of the coordinated water molecule were determined by a potentiometric pH titration at (298+/-0.1) K. Hydrolytic kinetics of carboxylic acid esters were performed with Bis(4-nitrophenyl) carbonate HPLC 99%   (BNPC) and 4-nitrophenyl acetate (NA) as substrates. The obtained hydrolysis rate constants showed that ZnL has a very high rate of catalysis for BNPC hydrolysis, giving a 3.89x10(4)-fold rate enhancement over uncatalyzed hydrolysis at pH 7.01, relative to only a 42-fold rate enhancement for NA hydrolysis. Moreover, the hydrolysis second-order rate constants of both BNPC and NA greatly increases with pH. Hydrolytic kinetics of a phosphate diester catalyzed by ZnL was also investigated by using bis(4-nitrophenyl) phosphate (BNPP) as the substrate. The pH dependence of the BNPP cleavage in aqueous buffer shows a sigmoidal curve with an inflection point around pH 8.11, which was nearly identical to the pK(a) value from the potentiometric titration. The k(cat) of BNPP hydrolysis promoted by ZnL was found to be 9.9x10(-4) M(-1) s(-1), which is comparatively higher than most other reported Zn(II)-based systems. The possible intermediate for the hydrolysis of BNPP, Bis(4-nitrophenyl) carbonate HPLC 99%, and NA catalyzed by ZnL is proposed on the basis of kinetic and thermodynamic analysis.

Description: Bis(4-Nitrophenyl) Carbonate
Synonym: Bis(p-Nitrophenyl) Carbonate; p,p'-Dinitrodiphenylcarbonate
CAS: 5070-13-3
Assay: ≥99% (HPLC)
Appearance: white to off-white solid
Molecular: C13H8N2O7
Application: Anti-HIV as Pharmaceutical Intermediates

 

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Pharmaceutical intermediates market

Pharmaceutical intermediates market, "China still optimistic about the prospects for the development of pharmaceutical intermediates," This is a reporter in 2006 in the recently held second session of the progress and the development of pharmaceutical intermediates market outlook seminar, experts from the participants learn about information. In recent days, including the SFDA Information Center Wang Pu good researcher, China Pharmaceutical University, Professor Liao Qingjiang, SFDA Southern Medicine Economic Institute Tao Jianhong, deputy director and other experts, and pharmaceutical intermediates from China more than 70 professionals in the industry participated in the seminar .
 
Expert opinion, 1: With the market stronger conference, experts revealed that a group of exciting data: 2005 1 ~ 12 months total industrial output value of China's chemical raw materials reached 116.277 billion yuan, an increase of 33.51%; profit the amount of 6.78 billion yuan, up 27.5%; in particular exports, reaching 7.903 billion U.S. dollars, representing growth of 27.55 percent a year earlier. From these economic indicators, pharmaceutical industry remains a fairly clear trend of increase. Experts believe that prospects for the pharmaceutical market is bound to push the upper reaches of the strength of pharmaceutical intermediates.
 
General, the Pharmaceutical Intermediates manufacturers needs of the most originally produced by the pharmaceutical companies themselves. But in recent years as the deepening social division of labor and production and technological progress, a number of pharmaceutical intermediates production of a gradual shift from production of pharmaceutical isolated and transferred to the chemical industry enterprises. From the international point of view, pharmaceutical intermediates has now become an international chemical industry in a major industry. In China, pharmaceutical intermediates production enterprises are mostly private, the investment is small, the basic in a few 1000000-1 between 20 million yuan. As the profits of pharmaceutical intermediates production higher than the general chemical products, production process and also basically the same, so there are an increasing number of small chemical companies have joined the ranks of the production of pharmaceutical intermediates; production of bulk drugs intermediates than the low profit margins, while the APIs and intermediates production process also similar, therefore, some enterprises not only the production of intermediates, bulk drugs have also begun to extend.
 
After more than 30 years of development, China's medicine needed for the production of basic chemical raw materials and intermediates can be complementary, and only a small part of the need to import, and because our resources were more abundant, lower raw material prices, there are a number of intermediate to achieve a large number of export. Relative to the bulk drug and formulations, pharmaceutical intermediates by the importing country's restrictions on the export much less, but in recent years, the United States and Europe, many large pharmaceutical companies to cut production costs and the level of environmental protection requirements to consider the middle of its pharmaceutical production of the body gradually transfer to developing countries, or more than the quality of imports from developing countries, reliable Pharmaceutical intermediates. This gave pharmaceutical intermediate manufacturing enterprises in China has brought an excellent business opportunities. Experts believe that, due to years of accumulated technical advantages and the future of the pharmaceutical market in huge demand, China's pharmaceutical intermediates sector underlay the enormous potential for development. It is noteworthy that, with increasing emphasis on the state environmental protection, environmental protection and cost-to-intermediate for the manufacturing industry will be a problem can not be ignored.

from:blogigo
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Emergency treatment and disposal methods of 4-Nitrophenyl Chloroformate

A leakage contingency isolation leakage polluted area, located around the warning signs, the proposed emergency personnel wearing self-contained breathing apparatus to wear chemical protective clothing. Reasonable ventilation, do not direct contact with leakage, use a clean shovel collection in a dry Jingjie covered containers, transported to the waste disposal sites.
 
1.If large spills, recycling or collection of sound waste treatment. Waste disposal methods: incineration. The combustion process to be sprayed into the steam or methane, so as not to generate chlorine gas, incinerator emissions of nitrogen oxides by high temperature catalytic oxidation device or device removed.
 
2, protective measures for respiratory protection: concentration of 4-Nitrophenyl Chloroformate Titration 98% in air overweight, wearing gas masks. Emergency rescue or evacuation, they should wear self-contained breathing apparatus. Eye protection: wear safety glasses. Protective clothing: wearing tight sleeve clothing and long boots. Hand protection: wear rubber gloves. Other: work site prohibit smoking, eating and drinking. Timely washed clothes. Before and after the work is not drinking, bathing with warm water. The implementation of pre-employment and periodic medical examinations.
 

 
3, first-aid measures Skin contact with 4-Nitrophenyl Chloroformate : Remove contaminated clothing, use soap and water thoroughly washed. Eye contact: immediately filed eyelid, with a large number of flows of water or saline flushing. Inhalation: rapidly from the scene to fresh air. To the oxygen breathing difficulties. Breathing stops, artificial respiration immediately. Medical treatment. Fresh into: coverage to persons mouthwash, water, activated carbon oral after gastric lavage, or give to catharsis. Medical treatment. Fire fighting methods: mist of water, foam, carbon dioxide, dry powder, sand.
 
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How to degradation of 4-Nitrophenyl Chloroformate

Pseudomonas putida ZWL73 separated from 4-Nitrophenyl Chloroformate contaminated soil, can be 4CNB as the sole carbon and nitrogen source of growth, and the release of chloride ions from the substrate and ammonium ion.


Degradation of bacteria by enzymatic analysis of cell extracts to detect pairs of 4CNB nitro-reductase activity and speculated that the open-loop substrate 2 - amino -5 - chlorophenol (2A5CP) ring-opening dioxygenase activity, combined with growth substrate range of factors (such as the product of a full restoration can not be used for p-chloroaniline growth) and by GC-MS to detect pairs of chlorine sub-nitrobenzene in the medium, the generation and conversion results suggest that ZWL73 through some means of restoring degraded 4CNB.

Plasmid elimination and conjugative transfer showed degrading bacteria has the 100kb plasmid involved in the 4-Nitrophenyl Chloroformate GC 96% degradation, as evidenced from: plasmid elimination loss of wild-type bacteria possess 2A5CP nitro reductase and ring-opening dioxygenase activity; plasmid After the elimination of strains can not grow on the substrate medium, while the plasmid transfer into the recipient bacteria after the latter obtained a 4CNB the ability to grow on.

ZWL73 is the first one identified 4-Nitrophenyl Chloroformate Titration 98% the degradation pathway encoded in plasmid strains. By constructing plasmid DNA library was screened with a right 2A5CP activity of clones, obtained by subcloning a 4.9kb EcoRI fragment, sequenced fragment of the sequence analysis showed that the two genes encoding the inter-bit cnbCaCb were the open-loop pairs plus oxygenase β and α subunit; over-expressed in E. coli proteins show ...
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Development Trend of China Pharmaceutical Intermediates

Fluorine-containing pyridine intermediates into the hot At present,
 
China has developed and has been put into mass production of the quinolone antibacterial drugs are mainly norfloxacin, ciprofloxacin, ofloxacin, enoxacin, lomefloxacin and fluorine Rosa magnitude. Including norfloxacin, ciprofloxacin, ofloxacin produce the largest, accounting for fluoroquinolone antibacterial agents of domestic production of 98%.
 
Quinolones are generally synthetic fluorine-containing fluorine-containing benzene ring after quinoline piperazine compounds (or methyl piperazine) derived from condensation. Because China's abundant reserves of fluorite, which is the world's production of fluorine-containing drugs and intermediates, one of the largest countries, with more than 80% of the export supply of fluorine-containing intermediates. Overall, the development of China-fluorobenzene intermediate class early, the current excess production capacity generally; Benzotrifluoride the development of late pharmaceutical intermediates  class in recent years, fast development; while for heterocyclic aromatic compounds, especially fluorinated pyridine class, our present, only the individual research units and production plants have a fluorine-containing pyridine intermediate synthesis technology, therefore, fluorine-containing pyridine intermediates will be the next few years, the domestic development of fluorine-containing intermediates, one of the main directions.
 
For example: Chloromethyl Pivalate
 
 
Aminophenol big gap in China has become the world's largest Pharmaceutical Intermediates manufacturers of anti-inflammatory drugs, aspirin, paracetamol, and other types of output Junchao analgin million tons, phenacetin, aminopyrine, security other than the forest species for production of more than 1000 tons. At present, China's output of antipyretic analgesics has grown rapidly in the future will be expected to grow at a rate of about 8%. For the complete production of antipyretic analgesics intermediate output of large manufacturing enterprises more. With the growth of anti-inflammatory drugs, their intermediates have also gained considerable development.
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The use of pharmaceutical intermediates

Organocatalysis uses small organic molecules predominantly composed of C, H, O, N, S and P to accelerate chemical reactions. The advantages of organocatalysts include their lack of sensitivity to moisture and oxygen, their ready availability, low cost, and low toxicity, which confers a huge direct benefit in the production of pharmaceutical intermediates when compared with (transition) metal catalysts.

In the example of the N-BOC-4-Hydroxypiperidine,it is believed that piperidine forms a reactive iminium ion intermediate with the carbonyl compound:


Description: N-BOC-4-Hydroxypiperidine
Synonym: N-(Tert-Butoxycarbonyl)-4-Hydroxypiperidine
CAS: 109384-19-2
Assay: ≥98% (GC)
Appearance: white or off-white  powder
Molecular:  C10H19NO3
Application: Pharmaceutical Intermediates

 

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