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Understanding Oral Bioavailability Challenges Associated With
Understanding Oral Bioavailability Challenges Associated With

... Lower solubility means that intestinal microbiome will be exposed to the unabsorbed compounds Microbiome can mediate highly different metabolic pathway that may not be well conserved ...
SERIES ‘‘CONTROVERSIAL ISSUES IN TUBERCULOSIS’’ Number 5 in this Series
SERIES ‘‘CONTROVERSIAL ISSUES IN TUBERCULOSIS’’ Number 5 in this Series

... for pansusceptible tuberculosis has been found to be adequate for persons with or without HIV infection [15]. This same regimen is the recommended form of treatment in the 2003 guidelines of the World Health Organization (WHO) [16]. Tuberculosis treatment is highly effective, but cumbersome because ...
PhD thesis
PhD thesis

... their  effect  on  the  sex  steroid  hormone  balance  in  more  complex  test  systems.  The  H295R  cell  line  assay,  an  established  assay  developed  to  identify  compounds  that  can  disrupt steroidogenesis was used to evaluate the two SSRIs sertraline and fluvoxamine.  Male  rats  were  ...
Selective Inhibitors of Picornavirus Replication
Selective Inhibitors of Picornavirus Replication

... Numerous studies have been performed in the past decades on a series of compounds developed by Sterling-Winthrop, commonly known as ‘‘WIN compounds.’’ Following lead optimization of an accidentally discovered compound, a drug was developed that would meet most of the criteria of a successful anti-pi ...
Cox-2-Selective Inhibitors: The New Super Aspirins
Cox-2-Selective Inhibitors: The New Super Aspirins

... Fig. 3. A, ribbon diagram of the ovine Cox-1 dimer (Picot et al., 1994). Both Cox-1 and Cox-2 have been localized to the luminal surface of the endoplasmic reticular and nuclear membranes, where they anchored into a single leaflet of the lipid bilayer by a membrane binding domain (gold) composed of ...
The Widening Challenge: How to Learning
The Widening Challenge: How to Learning

... HA-MRSA is usuly designed and on an agar plate ally only treated approved for use with non-beta against MRSA. inoculated with S. aureus. lactam antibiotics specifically deVancomycin signed to be used First approved against MRSA, CA-MRSA is usually in 1958, vancomycin has long been susceptible to a w ...
PREEXPOSURE PROPHYLAXIS FOR THE PREVENTION OF HIV INFECTION IN THE UNITED
PREEXPOSURE PROPHYLAXIS FOR THE PREVENTION OF HIV INFECTION IN THE UNITED

... every day and those who did. Among the men who said they took most of their daily doses, PrEP reduced the risk of HIV infection by 73% or more, up to 92% for some. Among men and women in couples in which one partner had HIV infection and the other partner initially did not (“HIV-discordant” couples) ...
Insert Slide Title Here - Academy for Infection Management
Insert Slide Title Here - Academy for Infection Management

... • The frequency of detection of antibiotic-resistant pathogens in nosocomial infections has increased at an alarming rate over the past few years • 50–60% of the >2 million nosocomial infections occurring in the USA each year are caused by antibiotic-resistant bacteria • The high rate of antibiotic ...
Chemistry, Drugs and Clandestine Laboratories
Chemistry, Drugs and Clandestine Laboratories

... Substances” with restrictions such as: - age limit - limits on advertising • Later, following further local studies the EACD recommended rescheduling BZP and related piperazines as Class C ...
Discovery of PF-04457845: A Highly Potent
Discovery of PF-04457845: A Highly Potent

... central tissues, an irreversible inhibitor may be beneficial because the nonequilibrium binding mechanism limits the competition with high endogenous substrate concentrations leading to increased biochemical efficiency.24 Furthermore, the pharmacodynamic effect resulting from covalent inhibition oft ...
Structural Basis for Interaction of Inhibitors with Cyclin
Structural Basis for Interaction of Inhibitors with Cyclin

... Abstract: Cell cycle progression is tightly controlled by the activity of cyclin-dependent kinases (CDKs). CDKs are inactive as monomers, and activation requires binding to cyclins, a diverse family of proteins whose levels oscillate during the cell cycle, and phosphorylation by CDK-activating kinas ...
(embelin)-a second solid gold of india
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NON-STEROIDAL ANTIINFLAMMATORY DRUGS (NSAIDS)
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... Reye’s syndrome: This is seen in children who take an NSAID such as aspirin while recovering from mild viral infection. Although it occurs rarely there is a 20-30% mortality seen with this type of side effect. ...
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... In a drug interaction study, 42 healthy subjects were given alvimopan 6 mg twice daily for 30 days, with ciprofloxacin 500 mg twice daily on days 11 to 20. Ciprofloxacin almost totally abolished the plasma levels of the metabolite of alvimopan, and this effect partially persisted in some subjects 10 ...
enzyme induction and inhibition
enzyme induction and inhibition

... rifampicin (McInnes and Brodie, 1988). Given this limitation it is possible in man to compare drugs as enzyme inducers by the construction of doseresponse curves. The effect of phenobarbitone on warfarin and antipyrine metabolism has been found to be dose dependent as is the effect of rifampicin on ...
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... nitromidazole drugs such as metronidazole [1 - (2 - hydroxyethyl) - 2 - methyl - 5 ­ nitroimidazole] . Nitroimidazole have been shown several important problems such as mutagenic and toxic towards the host when they are used at high doses. Long term use of medication produces undesirable side effect ...
Macrolides and associated antibiotics based on similar mechanism
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... life cycle following antibiotic treatment in which the apicoplast genome fails to replicate [26]. Thus, similar to tetracyclines, the antiplasmodial action of this macrolide is therefore delayed [27, 28]; this phenomenon in which the parasite completes a full cycle before achieving growth inhibition ...
Isentress - Merck.com
Isentress - Merck.com

...  Chewable Tablets o 100 mg pale orange, oval-shaped, orange-banana flavored, chewable tablets scored on both sides and imprinted on one face with the Merck logo and "477" on opposite sides of the score. o 25 mg pale yellow, round, orange-banana flavored, chewable tablets with the Merck logo on one ...
Smoking Cessation in Psychiatric Patients
Smoking Cessation in Psychiatric Patients

... withdrawal associated with smoking cessation but provides nicotine levels lower than those associated with smoking. Table 1 lists the various forms of NRT that will be available on hospital formularies as of 1st January 2008. NRT should only be used for those who smoke more than 10 cigarettes per da ...
s sanoFi avent 4  -6'  Lt ~,,'  2i
s sanoFi avent 4 -6' Lt ~,,' 2i

... thought to kill the cell. In non-dividing cells, toxicity may be caused by damage to the cell membranes, inactivation of critical enzymes, or inhibition of transcription . 1 4 In addition, the presence of platinum-DNA complexes (adducts) has been postulated to trigger apoptosis 16,17 Once again; thi ...
A Mechanistic Approach to Understanding the Factors Affecting
A Mechanistic Approach to Understanding the Factors Affecting

... layer.14 In examining the relative contribution of these various components, it was noted that lipid constituents such as phosphatidyl choline, cholesterol, and linoleic acid significantly retard the diffusion of small lipophilic molecules such as propranolol and hydrocortisone. Conversely, small hy ...
INHIBITORY EFFECTS OF ACTIVE CONSTITUENTS AND EXTRACTS OF ANDROGRAPHIS
INHIBITORY EFFECTS OF ACTIVE CONSTITUENTS AND EXTRACTS OF ANDROGRAPHIS

... The positive inhibitors, extracts and active constituents were tested in preliminary screening to determine IC 50 values by using a single concentration of enzyme and substrate that had been optimized by manufacturer [25]. For each experiment, negative and positive control incubations were performed ...
Macrocycles in new drug discovery
Macrocycles in new drug discovery

... Macrocycles in new drug discovery The use of drug-like macrocycles is emerging as an exciting area of medicinal chemistry, with several recent examples highlighting the favorable changes in biological and physicochemical properties that macrocyclization can afford. Natural product macrocycles and th ...
Updated US Public Health Service Guidelines for the Management
Updated US Public Health Service Guidelines for the Management

... Occupational Exposures to HIV and Recommendations for Postexposure Prophylaxis.6 The PHS working group was comprised of members from the CDC, the FDA, the Health Resources and Services Administration, and the National Institutes of Health. Names, credentials, and affiliations of the PHS working grou ...
C 5  P450
C 5 P450

... induced LPS-stimulated release of TNF- from human monocytic THP-1 cells (26). TAK715 was advanced to clinical Phase II trials for rheumatoid arthritis, but was discontinued as it did not satisfy criteria for further development (27). However, recently Verkaar et al. showed that TAK-715 is able to i ...
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Discovery and development of non-nucleoside reverse-transcriptase inhibitors



Non-nucleoside reverse-transcriptase inhibitors (NNRTIs) are antiretroviral drugs used in the treatment of human immunodeficiency virus (HIV). NNRTIs inhibit reverse transcriptase (RT), an enzyme that controls the replication of the genetic material of HIV. RT is one of the most popular targets in the field of antiretroviral drug development.Discovery and development of NNRTIs began in the late 1980s and in the end of 2009 four NNRTI had been approved by regulatory authorities and several others were undergoing clinical development. Drug resistance develops quickly if NNRTIs are administered as monotherapy and therefore NNRTIs are always given as part of combination therapy, the highly active antiretroviral therapy (HAART).
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