Isosteric PowerPoint PPT Presentations

Neuraminidase post-mortem. Although this is a another. success, there is a caveat: ... HIV RT post-mortem. Only a single, but invariant, short-range electrostatic ...

Classical Electrostatics and Drug Design: Enumeration and Evaluation of Isosteric Analogs ... Gimble (PB Electrostatics) picks up the critical SAR ...

Statistical frequency = 1 in 46 or 1/4096 ... New clamp at the scissile phosphate. Isosteric substitution retains symmetry. Adaptive Binding ...

Synthetic compounds consisted of an N1 alkylated 1,4-dihydro-4-oxo-3 ... action of nalidixic acid and its congener is the result of the inhibition of DNA synthesis. ...

Structurally non-specific action results from accumulation of a drug in some ... Structural features of drugs and their pharmacological activity Stereochemistry: ...

Drugs Acting on CNS -

The Organic Chemistry of Drug Design and Drug Action Chapter 3 Receptors 1878 Langley Study of antagonistic action of alkaloids on cat salivary flow suggests the ...

Ex: effexor XR, lexapro, zoloft, prozac, wellbutrin XL. SSRI's: What is known: 5-HT at: ... 10: Lexapro, Forest, $2.10 billion. Serotonin selective reuptake inhibitor ...

Lead Optimization) Dissection & shearing Association Local manipulation

Reactive gas adsorption What can be measured using this technique? ... BET surface area, pore size distribution, true density, tapped density.

The Organic Chemistry of Drug Design and Drug Action Chapter 3 Receptors 1878 Langley Study of antagonistic action of alkaloids on cat salivary flow suggests the ...

DESIGNING CARRIER-LINKED PRODRUGS. Carrier-mediated prodrugs are designed with ... Generation of a toxic metabolite from the 'inert' carrier moiety. ...

Two parts to successful model building

Present study was performed so as to compare adsorptive removal efficiencies of low-cost adsorbent rice husk ash (RHA) and commercial granular activated carbon (GAC) for the removal of bisphenol-A (BPA), an endocrine disrupting chemical, from aqueous solution. Effect of variables such as initial concentration (C0), adsorbent dose (m), temperature (T), pH, and time (t) were studied. Optimized values at C0 = 100 mg/L were found to be: m = 30 g/L, t = 3 h for RHA whereas for GAC, optimum values were: m = 20 g/L and t = 2 h. Pseudo-second-order model best represented the adsorption kinetic data; and Freundlich and Temkin models best fitted the isotherm data. The adsorption of BPA onto GAC and RHA was found to be endothermic in nature. Value of change in entropy and enthalpy for BPA adsorption onto RHA was found to be: 21.38 J/mol K and 0.335 kJ/mol, respectively. Respective values for BPA adsorption onto GAC were found to be: 29.6 J/mol K and 4.03 kJ/mol, respectively

The manner in which chemical compounds recognize each other has far reaching ... Since material property is closely linked to the alignment of the fundamental ...

Reveal the affinity and effective concentration of a series of drug analogs ... Substrate or drug binding to the receptor induces 3 dimensional conformational ...

Lack of selectivity, leading to toxicity ... affinity and selectivity of interaction with ... a DNA sequence-selective vector. New distamycin-derived mustards ...

Regulation of biological activity through protein dimerization: Crystallographic analyses of primiti

Measure the current room temperature. Do not discuss your results with your ... In a dry adiabatic process potential temperature doesn't change, thus entropy is ...

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DRUG DESIGN (AN OVERVIEW) APPAJI B MANDHARE, Ph.D. TORRENT RESEARCH CENTRE (Gandhinagar, India) appajimandhare@torrentpharma.com Pharmaceutical R&D A Multi ...

... was officially adopted by the International Commission for the Exploration of ... These curves portray the temperature changes that occur upon a saturated air ...

ATMS 305 Atmospheric Thermodynamics and Statics. Today's lecture topics: ... http://www.hgtv.com/hgtv/ah_personal_care_safety/article/0,,HGTV_3149_13906 64,00. ...

Hilton Klein, Larry Handt. Antiviral & Vaccine Research. Daria Hazuda, Pete Felock, Abigail Wolfe, Kara Stillmock, Marc Witmer, Mike Miller, ...

The Organic Chemistry of Drug Design and Drug Action Chapter 5 Enzyme Inhibition and Inactivation Enzyme Inhibition and Inactivation Categories of Enzyme Inhibitors ...

Overproduction of Metabolites of Industrial Microorganisms MECHANISMS ENABLING MICROORGANISMS TO AVOID OVERPRODUCTION OF PRIMARY METABOLIC PRODUCTS THROUGH ENZYME ...

... Arg urea + ornithine ornithine increased velocity of the UREA CYCLE = detoxification of NH3 from degrad. of prot. General ...

Antiepileptic Drugs Gisvold s book Barbiturates Hydantoins Oxazolidinedienos Succinimides Phenacemides Glutethemides Miscellaneous Benzodiazepines ...

Title: PowerPoint Presentation Author: AMIN KAMEL Last modified by: Eisai Created Date: 4/12/2005 3:44:51 PM Document presentation format: On-screen Show

The state of most homogeneous substances is completely described by two independent ... FIRST LAW OF TD: If a system changes state by adiabatic means only then ...

WABE: Sudoku for Chemists. MGMS Meeting, Dublin, September 2005. Shapes of molecules ... 'Simple, Intuitive Calculations of Free Energy of Binding for Protein ...

Patrick An Introduction to Medicinal Chemistry 3/e Chapter 19 CHOLINERGICS, ANTICHOLINERGICS & ANTICHOLINESTERASES Part 1: Cholinergics & anticholinesterases

Qualitative properties formalized in ... Study the concentration of chemical substances in a biological system as ... the system of ODEs over variables {A1 , ...

Drug Design Optimizing Target ... based drug design Procedure Crystallize target protein ... activity Crystallise a promising analogue with the target protein and ...

Nanostructured Carbide-Derived Carbons. for Energy-Related and Biomedical ... Specific gravimetric and volumetric capacitances change versus the chlorination ...

X.Q.Lewell et al. J.Chem.Inf.Comput.Sci. 38 (1998) 511. * Siehe auch C.S.Siebert Ch.i.u.Zeit 38 (2004) 320 Benzol = Thiophen (S entspricht r umlich C=C) ...

Heterogeneous catalysis Lec 9 week 12

HIV

SAR Antidiabetic Agents X = O, S, or N

exploiting the similarity concept is a sign of immature science (Quine) ... carcinogenesis; Mnt, in vivo induction of micronuclei; Sal, Salmonella ...

'You are here to learn the subtle science and exact art of potion making. As there is little foolish wand-waving here, many of you will hardly believe this is magic. ...

Drug Discovery, Development, and Design. Chapters 9, 10, and 12. History ... 2.23 meperidine (Demerol) 2.24 dextropropoxyphene (Darvon) 2.25 methadone. back ...

quantum chemical bonding situation. The desorption reaction - Kinetics and ... Especial simple is the Redhead analysis [P.A. Redhead, Vacuum 12 (1962) 201] ...

At present, anti-HIV drugs are aimed at two targets: reverse transcriptase and HIV protease. ... Nucleoside/Nucleotide Reverse Transcriptase Inhibitors ...

V8 Protein-Liganden-Wechselwirkung anschaulich betrachtet Beispiele f r Protein-Liganden Komplexe Wo ist das aktive Zentrum? (Docking wird hier nicht behandelt ...

Chapter 14 Pharmacokinetics Getting a drug to the target in the body Dopamine Useful in treating Parkinson s Disease Too polar to cross cell membranes and BBB ...

Named after natural products showing receptor selectivity ... Selective for muscarinic receptors over nicotinic receptors ... Selective for the muscarinic receptor ...

What does the transition state of the neuraminidase-catalyzed reaction look like? Homework Questions: Describe the methods used for diagnostic testing for HSV.

Advanced Medicinal Chemistry Lecture 3: Molecular Interactions and Drug Potency Barrie Martin AstraZeneca R&D Charnwood Advanced Medicinal Chemistry Barrie Martin ...

Fewer than five H-bond donating functions. Fewer than 10 H-bond ... Increase hydrophobicity, decrease water solubility. Increase conformational flexibility ...

* * Biosynthesis of Indole Alkaloids Indole indole ... Indole alkaloid Indole ...

Prodrugs and Drug Delivery Systems. Prodrug - a pharmacologically inactive compound that is converted to an active drug by a metabolic biotransformation

NRTIs are sometimes called the

PHARMACOKINETICS Prof. Dr. Basavaraj K. Nanjwade M. Pharm., Ph. D Department of Pharmaceutics KLE University s College of Pharmacy BELGAUM-590010, Karnataka, India

Patrick An Introduction to Medicinal Chemistry 3/e Chapter 13 QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIPS (QSAR) 10. Free-Wilson Approach The biological activity of ...

ALTERATION OF PHYSICOCHEMICAL PROPERTIES BY INTRODUCTION OR ... Halogen. Catechol. 24. NONCLASSICAL. BIOISOSTERES. Exchangeable Groups. Thioether. Thiourea ...