Notes Archive

  • Proteins are working molecules of a cell that carry out the ‘program’ of activities encoded onto them by gene

    An Introduction To Protein Structure

    Proteins are working molecules of a cell that carry out the ‘program’ of activities encoded onto them by gene

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  • A summary of the medicinal chemistry of adrenergics and cholinergic drugs including biosynthesis of norepinephrine and biosynthesis of acetylcholine, metabolism of norepinephrine and metabolism of acetylcholine and the structure activity relationship of the adrenergic and cholinergic agents.

    Medicinal Chemistry of the Peripheral Nervous System – Adrenergics and Cholinergic their Biosynthesis, Metabolism and Structure Activity Relationships

    A summary of the medicinal chemistry of adrenergics and cholinergic drugs including biosynthesis of norepinephrine and biosynthesis of acetylcholine, metabolism of norepinephrine and metabolism of acetylcholine and the structure activity relationship of the adrenergic and cholinergic agents.

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  • Gene Therapy is a technique for correcting defective genes that are responsible for disease development

    Gene Therapy

    Gene Therapy is a technique for correcting defective genes that are responsible for disease development

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  • Multicomponent reactions (MCRs) are highly convergent reactions, with high atom efficiency, good bond forming capabilities and higher yields in comparison to a similar multistep reaction.

    Multicomponent Reactions

    Multicomponent reactions (MCRs) are highly convergent reactions, with high atom efficiency, good bond forming capabilities and higher yields in comparison to a similar multistep reaction.

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  • MET (mesenchymal-epithelial transition factor) is a proto-oncogene that encodes a protein MET, also known asc-Met or hepatocyte growth factor receptor (HGFR). MET is a membrane receptor that is essential for embryonic development and wound healing. Hepatocyte growth factor (HGF) is the only known ligand of the MET receptor. MET is normally expressed by cells of epithelial origin, while expression of HGF is restricted to cells of mesenchymal origin. Upon HGF stimulation, MET induces several biological responses that collectively give rise to a program known as invasive growth. Abnormal MET activation in cancer correlates with poor prognosis, where aberrantly active MET triggers tumor growth, formation of new blood vessels (angiogenesis) that supply the tumor with nutrients, and cancer spread to other organs (metastasis). MET is deregulated in many types of human malignancies, including cancers of kidney, liver, stomach, breast, and brain. Normally, only stem cells andprogenitor cells express MET, which allows these cells to grow invasively in order to generate new tissues in an embryo or regenerate damaged tissues in an adult. However, cancer stem cells are thought to hijack the ability of normal stem cells to express MET, and thus become the cause of cancer persistence and spread to other sites in the body.

    c-MET

    MET (mesenchymal-epithelial transition factor) is a proto-oncogene that encodes a protein MET, also known asc-Met or hepatocyte growth factor receptor (HGFR). MET is a membrane receptor that is essential for embryonic development and wound healing. Hepatocyte growth factor (HGF) is the only known ligand of the MET receptor. MET is normally expressed by cells of epithelial origin, while expression of HGF is restricted to cells of mesenchymal origin. Upon HGF stimulation, MET induces several biological responses that collectively give rise to a program known as invasive growth. Abnormal MET activation in cancer correlates with poor prognosis, where aberrantly active MET triggers tumor growth, formation of new blood vessels (angiogenesis) that supply the tumor with nutrients, and cancer spread to other organs (metastasis). MET is deregulated in many types of human malignancies, including cancers of kidney, liver, stomach, breast, and brain. Normally, only stem cells andprogenitor cells express MET, which allows these cells to grow invasively in order to generate new tissues in an embryo or regenerate damaged tissues in an adult. However, cancer stem cells are thought to hijack the ability of normal stem cells to express MET, and thus become the cause of cancer persistence and spread to other sites in the body.

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  • Malonic esters when reacted with alkyl halide (R-X) in the presence of base such as NaOH will produce ?-alkylated esters. However, reaction will not stop there. Over time, the reaction will also give disubstituted products as well as free acids.

    Malonic Ester Synthesis – Alkylation of Enolates

    Malonic esters when reacted with alkyl halide (R-X) in the presence of base such as NaOH will produce ?-alkylated esters. However, reaction will not stop there. Over time, the reaction will also give disubstituted products as well as free acids.

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  • Acetoacetic ester synthesis is similar to malonic ester synthesis.When ?-keto ester is reacted with a weak base such as Sodium Hydroxide (NaOH) in the presence of alkyl halide (R-X), it produces ?-alkylated ?-keto esters and also di-alkylated products. However, upon acidification the mixture will lose a molecule of carbon dioxide to get decarboxylated to give ketones as well. This will be further explained with the mechanism.

    Acetoacetic Ester Synthesis – Alkylation of Enolates

    Acetoacetic ester synthesis is similar to malonic ester synthesis.When ?-keto ester is reacted with a weak base such as Sodium Hydroxide (NaOH) in the presence of alkyl halide (R-X), it produces ?-alkylated ?-keto esters and also di-alkylated products. However, upon acidification the mixture will lose a molecule of carbon dioxide to get decarboxylated to give ketones as well. This will be further explained with the mechanism.

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  • As has been discussed previously - acetoacetic ester synthesis and malonic ester synthesis are non-selective, in that, they can produce dialkylated products. This particular property of these reactions can be made use of to synthesize cyclic compounds using a alkyl dihalide.

    Using the non-selective nature of acetoacetic ester synthesis and malonic ester synthesis to produce cyclic compounds

    As has been discussed previously - acetoacetic ester synthesis and malonic ester synthesis are non-selective, in that, they can produce dialkylated products. This particular property of these reactions can be made use of to synthesize cyclic compounds using a alkyl dihalide.

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  • In the presence of carbonyl functional group, the alpha-hydrogens of a molecule exhibit acidity i.e. in the presence of a base they can be abstracted very easily to yield a carbanion. The carbanion can be stabilized either with resonance to yield enolates.

    Chemistry of Enolates and Enols – Acidity of Alpha-Hydrogens

    In the presence of carbonyl functional group, the alpha-hydrogens of a molecule exhibit acidity i.e. in the presence of a base they can be abstracted very easily to yield a carbanion. The carbanion can be stabilized either with resonance to yield enolates.

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  • Copper catalyzed alkyne-azide cycloaddition (CuAAC) is one of the most reliable click reaction that has enabled the practical and efficient preparation of 1,4-disubstituted 1,2,3 triazoles from a wide range of substituted alkynes and azides which cannot be typically attained by the traditional Huisgen thermal cycloaddition reaction

    Catalytic Azide-Alkyne Cycloaddition: Reactivity and Application

    Copper catalyzed alkyne-azide cycloaddition (CuAAC) is one of the most reliable click reaction that has enabled the practical and efficient preparation of 1,4-disubstituted 1,2,3 triazoles from a wide range of substituted alkynes and azides which cannot be typically attained by the traditional Huisgen thermal cycloaddition reaction

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  • actor Xa is a zymogen of factor Xa, a serine protease, which occupies a pivotal position in the coagulation cascade. Factor Xa is found at the convergent point of extrinsic and intrinsic pathway leading to coagulation.

    Direct Factor Xa Inhibitors as Anticoagulants

    actor Xa is a zymogen of factor Xa, a serine protease, which occupies a pivotal position in the coagulation cascade. Factor Xa is found at the convergent point of extrinsic and intrinsic pathway leading to coagulation.

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  • Absorption is characterized by evaluating the absorption rate constant ka from plasma concentration versus time data graphs. Most pharmacokinetic models assume first order kinetics for the oral absorption of the drug; however zero-order assumption can also occur

    Determination of Absorption Rate Constant

    Absorption is characterized by evaluating the absorption rate constant ka from plasma concentration versus time data graphs. Most pharmacokinetic models assume first order kinetics for the oral absorption of the drug; however zero-order assumption can also occur

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  • Being pharmacy and pharmaceutical science students, we face concentrations all around us in some form or the other. This article is aimed to guide you better on how you can do the calculations and understand what is going on while calculating concentrations. We start off with the definition of Avagadro’s Number, cover gram molecular weight, moles, molarity etc. and will end with real life example problems with solutions which you can use to practice your calculations with.

    A Primer on Measuring Concentrations – Molarity, Moles and Other Confusing Stuff

    Being pharmacy and pharmaceutical science students, we face concentrations all around us in some form or the other. This article is aimed to guide you better on how you can do the calculations and understand what is going on while calculating concentrations. We start off with the definition of Avagadro’s Number, cover gram molecular weight, moles, molarity etc. and will end with real life example problems with solutions which you can use to practice your calculations with.

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  • Enolates can be very tricky to handle. Upon reaction with a base and in the presence of alkyl halide, the carbonyl compounds with ?-hydrogens can undergo a reaction to produce a mixture of c-alkylated product or o-alkylated product.

    Chemistry of Enolates – C vs O Alkylation

    Enolates can be very tricky to handle. Upon reaction with a base and in the presence of alkyl halide, the carbonyl compounds with ?-hydrogens can undergo a reaction to produce a mixture of c-alkylated product or o-alkylated product.

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  • A chemical reaction in which more than one product can be formed is generally governed by either laws of thermodynamics or kinetics. It can therefore yield either thermodynamic products or kinetic products.

    Thermodynamic Product vs Kinetic Product – with example of enolate formation of 2-methylcyclohexanone

    A chemical reaction in which more than one product can be formed is generally governed by either laws of thermodynamics or kinetics. It can therefore yield either thermodynamic products or kinetic products.

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  • Pharmacology is the science of drugs and its physical and chemical properties and their affect on the body and how they interact with other substances.

    Basic Concepts Of Pharmacology

    Pharmacology is the science of drugs and its physical and chemical properties and their affect on the body and how they interact with other substances.

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  • Drugs can be given to a person in a variety of formulations. Formulations is a mixture in a particular state that the drug is supplied to the patient. It can be either solid, semisolid or liquid formulations.

    Formulation and Routes of Administration of Drugs

    Drugs can be given to a person in a variety of formulations. Formulations is a mixture in a particular state that the drug is supplied to the patient. It can be either solid, semisolid or liquid formulations.

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  • Adverse drug reactions are reactions that occur apart from the normal drug action. Adverse drug reactions are unwanted reactions and are often seen if higher or inappropriate doses of medicines are taken. They are also known as side reactions.

    Adverse Drug Reactions

    Adverse drug reactions are reactions that occur apart from the normal drug action. Adverse drug reactions are unwanted reactions and are often seen if higher or inappropriate doses of medicines are taken. They are also known as side reactions.

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  • Phenolates are formed when a phenolic hydroxy group is reacted in the presence of base. The phenolate anion can react with alkyl halides to produce either O-alkylated or C-alkylated products.

    Phenolates- O-alkylation and C-alkylation

    Phenolates are formed when a phenolic hydroxy group is reacted in the presence of base. The phenolate anion can react with alkyl halides to produce either O-alkylated or C-alkylated products.

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  • Pharmacokinetics is the way the body acts on the drug once it is administered. The four processes involved are absorption, distribution, metabolism and elimination.

    Pharmacokinetics Basics- Absorption, Distribution, Metabolism and Excretion

    Pharmacokinetics is the way the body acts on the drug once it is administered. The four processes involved are absorption, distribution, metabolism and elimination.

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