SQ109 for the Treatment of Tuberculosis
... currently in clinical development for the treatment of adult pulmonary TB caused by drug sensitive or drug resistant strains of M. tuberculosis (IND #69,597, 2006). In three single and multi-‐dose ...
... currently in clinical development for the treatment of adult pulmonary TB caused by drug sensitive or drug resistant strains of M. tuberculosis (IND #69,597, 2006). In three single and multi-‐dose ...
Anti-viral agents
... induction of intracellular signals following binding to specific cell membrane receptors, resulting in inhibition of viral penetration. Treatment of Hepatitis B Virus Infection Entecavir is an orally administered guanosine nucleoside analog competitively inhibits all three functions of HBV DNA polym ...
... induction of intracellular signals following binding to specific cell membrane receptors, resulting in inhibition of viral penetration. Treatment of Hepatitis B Virus Infection Entecavir is an orally administered guanosine nucleoside analog competitively inhibits all three functions of HBV DNA polym ...
Tuberculosis Chemotherapy
... • Ethambutol should be avoided in in children below 5 years where it is difficult to asses visual activity & red – green color discrimination. • Ethambutol decreases renal excretion of urates & may precipitate gouty arthritis. • Mild GIT intolerance , rashes, fever & dizziness are also possible. ...
... • Ethambutol should be avoided in in children below 5 years where it is difficult to asses visual activity & red – green color discrimination. • Ethambutol decreases renal excretion of urates & may precipitate gouty arthritis. • Mild GIT intolerance , rashes, fever & dizziness are also possible. ...
Anti-viral drugs
... Nucleoside/Nucleotide Reverse Transcriptase Inhibitors • The first type of drug available to treat HIV infection ...
... Nucleoside/Nucleotide Reverse Transcriptase Inhibitors • The first type of drug available to treat HIV infection ...
ANTI VIRAL Agents
... which led to the diagnosis of herpes simplex infection, and a therapy with oral acyclovir was initiated. Two weeks later no improvement was seen and the dose of the drug was increased but without success. Which of the following was most likely the cause of failure of acyclovir therapy? A) Mutation o ...
... which led to the diagnosis of herpes simplex infection, and a therapy with oral acyclovir was initiated. Two weeks later no improvement was seen and the dose of the drug was increased but without success. Which of the following was most likely the cause of failure of acyclovir therapy? A) Mutation o ...
Medicinal chemistry
... relationship between chemical structure and pharmacological activity for a series of compounds. • Lead compound is a compound that has a desirable biological activity with therapeutic relevance, but typically has some shortcoming that is likely to be overcome through the development of analogs. ...
... relationship between chemical structure and pharmacological activity for a series of compounds. • Lead compound is a compound that has a desirable biological activity with therapeutic relevance, but typically has some shortcoming that is likely to be overcome through the development of analogs. ...
Interactions with HIV medications
... NRTIs : NRTIs are prone to pharmacodynamic interactions such as additive and synergistic toxicities, but because they are primarily eliminated by the kidneys, not the liver, they have little impact on the CYP450 system. As such, NRTIs have few known pharmacokinetic interactions with NNRTIs or PIs. A ...
... NRTIs : NRTIs are prone to pharmacodynamic interactions such as additive and synergistic toxicities, but because they are primarily eliminated by the kidneys, not the liver, they have little impact on the CYP450 system. As such, NRTIs have few known pharmacokinetic interactions with NNRTIs or PIs. A ...
Tina said you all learned ALOT last week
... enzymes, so that Kidneys can secrete more easily Different people have different enzymes in the liver, thus one may metabolize Zoloft well, but not Prozac. What are the implications for prescribing physicians? ...
... enzymes, so that Kidneys can secrete more easily Different people have different enzymes in the liver, thus one may metabolize Zoloft well, but not Prozac. What are the implications for prescribing physicians? ...
Instantaneous Inhibitory Potential and Inhibitory Quotient Show a
... of drugs compared in 17 randomized clinical trials. The IQ has been shown to correlate modestly with virologic outcome [3]; it is the ratio of trough drug concentration to the amount of drug necessary to inhibit viral activity by 50% in vitro (IC50). Recently, another measure of antiretroviral activ ...
... of drugs compared in 17 randomized clinical trials. The IQ has been shown to correlate modestly with virologic outcome [3]; it is the ratio of trough drug concentration to the amount of drug necessary to inhibit viral activity by 50% in vitro (IC50). Recently, another measure of antiretroviral activ ...
Anti-HIV drugs: 25 compounds approved within 25 years after the
... In these early days of anti-HIV drug research, it could hardly be foreseen that within 25 years of the virus being discovered we would now, in 2008, have at hand 25 anti-HIV compounds licensed (thus formally approved) for the treatment of AIDS (Table 1). These compounds fall within different categor ...
... In these early days of anti-HIV drug research, it could hardly be foreseen that within 25 years of the virus being discovered we would now, in 2008, have at hand 25 anti-HIV compounds licensed (thus formally approved) for the treatment of AIDS (Table 1). These compounds fall within different categor ...
4-Unit 4 Power Standards Ionic Compounds
... All molecular and ionic compounds have unique names and formulas that are determined systematically. The mole is the standard unit for counting atomic and molecular particles. Molar mass and Avogadro’s number are used when converting masses of compounds or elements into either moles or representativ ...
... All molecular and ionic compounds have unique names and formulas that are determined systematically. The mole is the standard unit for counting atomic and molecular particles. Molar mass and Avogadro’s number are used when converting masses of compounds or elements into either moles or representativ ...
Soft Drug
... approach, which uses information about the structure of a drug receptor or one of its natural ligands to identify or create candidate drugs. • The three-dimensional structure of a protein can be determined using methods such as X-ray crystallography or nuclear magnetic resonance ...
... approach, which uses information about the structure of a drug receptor or one of its natural ligands to identify or create candidate drugs. • The three-dimensional structure of a protein can be determined using methods such as X-ray crystallography or nuclear magnetic resonance ...
HIV treatment
... • Protease inhibitors: Protease inhibitors have a high affinity for the active site of HIV-1 protease and thus bind to the active site irreversibly. This binding to the active site impairs the catalytic activity of HIV-1 protease resulting in immature viral particles that don’t properly package into ...
... • Protease inhibitors: Protease inhibitors have a high affinity for the active site of HIV-1 protease and thus bind to the active site irreversibly. This binding to the active site impairs the catalytic activity of HIV-1 protease resulting in immature viral particles that don’t properly package into ...
1. An introduction to drugs, their action and discovery
... • The nature of the structures of leads and analogues will determine their ability to bind to receptors and other target sites. • Binding forces between a drug and a receptor – electrostatic bonds, such as hydrogen bonds ...
... • The nature of the structures of leads and analogues will determine their ability to bind to receptors and other target sites. • Binding forces between a drug and a receptor – electrostatic bonds, such as hydrogen bonds ...
Isentress® (raltegravir)
... The HIV virus is sloppy when it makes copies of its genetic code (RNA). Many new copies of HIV are mutations: they are slightly different from the original virus. Some mutations can continue to multiply even when you are taking an antiviral drug. When this happens, the drug will stop working. This i ...
... The HIV virus is sloppy when it makes copies of its genetic code (RNA). Many new copies of HIV are mutations: they are slightly different from the original virus. Some mutations can continue to multiply even when you are taking an antiviral drug. When this happens, the drug will stop working. This i ...
No Slide Title
... C (yellow), G (green), A (red), and T (blue). Mukherjee, A.; Lavery, R.; Bagchi, B.; Hynes, J. T. On the molecular mechanism of drug intercalation into DNA: A computer simulation study of the intercalation pathway, free energy, and DNA structural changes. J. Am. Chem Soc. 2008, 130, 9747. Reprinted ...
... C (yellow), G (green), A (red), and T (blue). Mukherjee, A.; Lavery, R.; Bagchi, B.; Hynes, J. T. On the molecular mechanism of drug intercalation into DNA: A computer simulation study of the intercalation pathway, free energy, and DNA structural changes. J. Am. Chem Soc. 2008, 130, 9747. Reprinted ...
Novel Low Molecular Weight Lignins for use as an Anticoagulant
... Researchers at VCU have developed a novel low-molecular weight (LMW) lignin that exhibits high selectivity and potency as an anticoagulant. These lignins, which are naturally occurring biopolymers, act as functional macromolecular mimetics of low-molecular weight heparins. However, these do not inhi ...
... Researchers at VCU have developed a novel low-molecular weight (LMW) lignin that exhibits high selectivity and potency as an anticoagulant. These lignins, which are naturally occurring biopolymers, act as functional macromolecular mimetics of low-molecular weight heparins. However, these do not inhi ...
39- Antituberculosis drugs
... 2. Isoniazid : 1952, the most active drug for the treatment of tuberculosis （1）Mechanism of action Inhibit the synthesis of mycolic acid which is essential components of mycobacterial cell walls （2）Antimicrobial activity High activity against both extracellular and intracellular tubercle bacilli （3） ...
... 2. Isoniazid : 1952, the most active drug for the treatment of tuberculosis （1）Mechanism of action Inhibit the synthesis of mycolic acid which is essential components of mycobacterial cell walls （2）Antimicrobial activity High activity against both extracellular and intracellular tubercle bacilli （3） ...
Rilpivirine: A second-generation nonnucleoside reverse
... with efavirenz in HIV-infected adults not previously treated with an antiretroviral. The investigators concluded that rilpivirine, when combined with two nucleoside or nucleotide reverse transcriptase inhibitors, was noninferior to efavirenz for reaching the endpoint of confirmed virological respons ...
... with efavirenz in HIV-infected adults not previously treated with an antiretroviral. The investigators concluded that rilpivirine, when combined with two nucleoside or nucleotide reverse transcriptase inhibitors, was noninferior to efavirenz for reaching the endpoint of confirmed virological respons ...
Study guide for research assistants
... Note that all 220,000 compounds were initially screened at a single concentration (3 µM) and that hits from this first round of screening were then tested over a range of concentrations. This is a pretty standard approach. The paper says, "A number of other inhibitors from unique structural classes ...
... Note that all 220,000 compounds were initially screened at a single concentration (3 µM) and that hits from this first round of screening were then tested over a range of concentrations. This is a pretty standard approach. The paper says, "A number of other inhibitors from unique structural classes ...
Assessing Drug Substances to Identify “Highly Hazardous
... categories of concern often overlooked other characteristics of the API such as pharmacologic potency and mechanism of action, which might also trigger specific requirements for safe handling and disposal. Drug manufacturers are often asked by contract manufacturing organizations whether or not APIs ...
... categories of concern often overlooked other characteristics of the API such as pharmacologic potency and mechanism of action, which might also trigger specific requirements for safe handling and disposal. Drug manufacturers are often asked by contract manufacturing organizations whether or not APIs ...
Design and Synthesis of Small Molecule Inhibitors of
... directed inhibition, or gene knock-out, has been shown to increase levels of HDL-C in rabbits and mice on both normal and high-fat diets. Because the active site of EL contains serine-protease like achitecture, we hypothesized that boronic acids could be used as small molecule inhibitors. Indeed, se ...
... directed inhibition, or gene knock-out, has been shown to increase levels of HDL-C in rabbits and mice on both normal and high-fat diets. Because the active site of EL contains serine-protease like achitecture, we hypothesized that boronic acids could be used as small molecule inhibitors. Indeed, se ...
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).