- Medicinal Chemistry - Question No. 3. Define the Hammett Constant and the hydrophobic (Hansch) substituent constant. Comment on how inductive and mesomeric polar effects are treated in substituted aromatic systems. A quantitative structure-activity relationship (QSAR) is an equation which correlates measurable or calculable physical or molecular properties to some specific biological activity. Once this relationship has been determined, it is possible to predict the biological activity of related drug candidates before they are put through expensive and time-consuming biological testing. The electronic effects of a substituent have an effect on the ionisation or polarity of a drug. This in turn may affect how easily a drug can pass through …show more content…
The substituents should therefore be hydrophobic and electron donating for maximum activity. • log 1/C is the concentration of drug that has a defined biological activity. The bigger the value of log 1/C , the smaller the value of c, the better the drug. • P is a measure of overall hydrophobicity. • π is the substituent hydrophobicity constant and measures the hydrophobicity of a specific region on the drug’s skeleton. When π is negative, activity decreases with hydrophobicity. You want substituents therefore that are very hydrophilic When π is positive, activity increases with hydrophobicity. You want substituents therefore that are very hydrophobic • σ is the Hammett constant discussed above; a measure of the electronic effect of substituents When σ is positive, electron-withdrawing substituents add to activity When σ is negative, electron-donating substituents add to activity References [xxx] Medicinal Chemistry: An Introduction By Gareth
The HOMO and LUMO help to derive the chemical reactivity and kinetic stability of the molecule. The energy of the HOMO is directly related to the ionization potential, LUMO energy is related to the electron affinity. The conjugated
Identification of an Unknown Compound using Quantitative and Qualitative Analysis Lauren Tremaglio Chemistry 1011 Lab, Section 16 Instructor: Steven Belina October 3, 2014 Our signatures indicate that this document represents the work completed by our group this semester. Experimental Design and Discussion of Results The objective of this experiment was to identify an unknown compound through quantitative and qualitative analysis. In order to find the identity of the unknown compound, an initial qualitative test for solubility was performed.
Tales of a Shaman’s Apprentice by Mark J. Plotkin PhD Tales of a Shaman’s Apprentice chronicles the interesting journey of the Harvard graduate and ethnobiologist Mark J. Plotkin as he attempts to record what’s left of the slowly dying art of shamanism and traditional medicine, particularly in the northern part of South Africa. The book does an excellent job of relating important medicinal discoveries to their origins in nature and traditional medicine. In this way, the book cleverly mixes the subject of medicine and history in a way that I believe will be interesting for pharmacy students. Throughout my reading of the book, I enjoyed how it felt as though I as the reader got to go on this journey with him to all these interesting locations
Q2F: Minimum inhibitory concentration (MIC) - Minimum inhibitory concentration is the minimum concentration of the substance necessary to prevent microbial growth. Q2G: Lipopolysaccharide - Lipopolysaccharide is a complex lipid structure containing unusual sugars and fatty acids found in most gram-negative Bacteria and constituting the chemical structure of the outer membrane. Q2H:
The History and Science of Healing With Essential Oils Did you know that at least 30% of prescription drugs in the United States are based on naturally occurring compounds from plants? Each year, millions of dollars are spent searching for new, undiscovered, curative elements in the bark, roots, flowers, seeds and foliage of plants from every corner of the Earth. As the most powerful part of the plant, essential oils and plant extracts have been mankind 's first medicine. History has shown and science supports that these can be used medicinally to kill bacteria and viruses.
Natural product and its derivatives have been recognized as therapeutic agents (Lahlou, 2013). Due to adverse effects from modern medicine and synthetic product, there is increase interest on discovering alternative natural product as therapeutic agent and become alternative for modern medicine since natural product has lesser adverse
With this in mind, the student understands that these herbal products can be beneficial, but also understands that before incorporating into the medical field there needs to be research that proves the safety and efficacy of the
It is seven o’clock in the morning, school hasn’t even started, but AP Chemistry has. As the teacher explains the lab in the front of classroom, the perfect combination of math and restless nights takes its toll on the rows of students. Slowly, heads go down and phones come out. As the attention of the other students wanes, my fascination grows. I begin wondering, “Why do polyphenolic beta-dicarbonyls found in turmeric, seem to offer medicinal advantages in treating cancer and Alzheimer 's disease?”
As a graduate student of medicinal chemistry, I hope to explore and bolster my skills in high throughput screening, small molecule synthesis, structure-activity relationship, mass spectrometry, in vivo animal studies, and molecular modeling. The ability to undertake such a vast array of studies and assays makes the process of drug discovery very exciting. Not only will I be concerned with the synthetic phase, but also I will be able to appreciate the effects that my work in the chemical hood will have on biological systems. I intend to devote my academic and professional lives to the discovery of novel approaches to mitigating degenerative disease states. The realms of anti-cancer and neural agents are of particular interest to me and are what I hope to center my career around.
The unknowns were all basic except for the acetylsalicylic acid which was an acid and pseudoephedrine hydrochloride which was a neutral pH when tested. We tested our unknowns and found that both had a basic pH when tested. When we tested the ingredients for acetone solubility we found that most of the ingredients were acetone soluble except for acetaminophen, cornstarch, and sugar. For unknown A we
Although both chapters include an examination of completely different ideas in the field of health and illness, Helman(2007) intertwines these chapters by emphasizing the importance of cultural and social factors in understanding complex methods and ideas today. A vital concept that must be understood through a sociocultural lens is pharmacology and the various aspects found within it. Throughout health and illness, the effect that chemical substances and medication has on the human body is critical to understand since the ideas behind health and medicine is consistently developing. In addition, the process of a drug from the drug itself, from the prescriber, to the recipient, and the setting the drug is in are all crucial sectors to understand by emphasizing the sociocultural background (Helman, 2007).
Drugs were an important part of medicine. There were two important drugs from the 17th and 18th century. One was cinchona bark from a plant in Peru that was used for malaria. Cinchona bark may be the first drug used to cure a specific disease. The other drug was digitalis, made from the foxglove plant, which was purified by William Withering and used to treat a swelling of the body, which could be caused by many different kinds of illnesses (46).
Philosophically, the importance of the willow tree has come a long way since the Assyrians (4000 BC) and Sumerians (3500 BC), who had seen its medicinal benefits. The first documented use of willow bark as an analgesic was recorded by Hippocrates in 4000 BC. The evolution of the willow tree’s use as a medicinal treatment occurred first with the question of the clinical potential of willow, then the discovery of the structure of salicin, and finally the chemical synthesis of salicylic acid and aspirin. The pharmacological component of willow bark, salicin, was discovered in 1838 by Raffaele Piria, an Italian chemist. Piria’s discovery of salicin led to further discoveries of the use of the compound and eventually to the synthesis of aspirin in 1893 by Felix Hoffman.
Herbal products have been used for treatments since ancient times, before the exploration of synthetic industrial drugs. Since herbs are natural, most of the consumers believes herbal products are completely safe and the product use continuously increased and is reported 10-19% growth in United States. In U.S.A any botanical product affects the structure and functions of the body belongs to either a drug or dietary supplement and FDA regulates the dietary supplement. The author of this paper selected St. John’s wort ,as the herbal supplement for this assignment of patient educational flyer. Product Description: St. John’s wort (SJW) is a yellow flowering plant, grows in the wild used for health purpose for long time .The
To optimize the RP-UPLC parameters and reach a good resolution and peak Tailing for Lamivudine,Abacavir and Dolutegravir, many chromatographic parameters were tested. Several mobile phases of different ratios were analysed to get that good resolution ,peak shape ,provided sufficient selectivity for the drugs. The phosphate buffer provided a higher sensitivity and selectivity than other buffers did. Using methanol and acetonitrile as organic components shown results in higher sensitivity, but varying the amounts of methanol and acetonitrile in the mobile phase affected the resolution , tailing factor theoretical plates and run time. Varying the pH of the mobile phase resulted in poor peak shapes, not showing good resolution.