Origins of Drugs and Chemical Synthesis

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Questions and Answers

What are the origins of most drugs before the advent of synthetic drugs?

Herbal origins

Beyond herbal origins, what other type of drug was commonly developed?

Semi-synthetics

What percentage of drugs are estimated to have natural origins?

Approximately 50%

What does the 'retro-approach' refer to in chemical synthesis?

Biogenetic synthesis Signup and view all the answers

What is a key focus in the field of chemical synthesis regarding molecular structures?

Challenging molecular frameworks Signup and view all the answers

What is a characteristic of semi-synthetic drugs that makes them practical?

Cost-effective approach Signup and view all the answers

What is the role of natural products chemistry in understanding natural resources?

Chemical instrument to comprehend biological facet Signup and view all the answers

Name one field that is beginning to integrate with the study of natural products chemistry?

Metabolic engineering Signup and view all the answers

What are two primary origins of drugs, according to the text?

Synthetic and natural resource-based origins. Signup and view all the answers

Name at least three challenges associated with synthetically originated drugs in the text.

Perceived toxicities, requirements for advanced facilities, adherence to stricter regulations. Signup and view all the answers

What impact has the combination of synthetic and naturally-sourced drugs had on natural products chemistry?

It has been a significant contributor to advancements in the field. Signup and view all the answers

What is an important relationship that has been realized through the investigation of natural templates?

The structure-activity relationships (SAR) Signup and view all the answers

Name at least three non-conventional chromatographic techniques mentioned in the text.

Flash, UHPLC, MPLC (or any 3 from: Electrokinetic chromatography, droplet countercurrent, super-critical fluid, and circular chromatography). Signup and view all the answers

What role do techniques like gel filtration play in natural product research?

These techniques help in detection, isolation-purification, and chemical profiling (or instant constituents screening or dereplication) of natural products. Signup and view all the answers

What is the purpose of a neural-network-based descriptor model in chromatography, as described in the text?

To predict the chromatographic sequence of natural compounds in a gradient procedure. Signup and view all the answers

What has the development of drug templates from natural resources lead to?

The development of drug templates for various biological activities. Signup and view all the answers

What is a key goal when using combinatorial chemistry to synthesize analogs of natural products for anticancer drugs?

To increase the biological activity and pharmacological diversity of the hit template. Signup and view all the answers

Name three strategies that have been used to create diversity oriented synthesis of natural product-like substances?

Folding, branching pathways, and oligomer-based approaches. Signup and view all the answers

Besides increasing diversity, what do templated approaches to natural product synthesis accomplish?

They broaden the outreach and applicability of natural products chemistry. Signup and view all the answers

What is the role of Sp transcription factors in cancer development?

They regulate genes involved in cell growth, survival, angiogenesis, migration, and inflammation. Signup and view all the answers

What is the purpose of studying the biomechanics of natural products for cancer treatment?

To optimize the clinical applications of natural products and their combination drugs. Signup and view all the answers

What is aldehyde oxidase (AO)'s role in the context of drug development?

It is responsible for the biotransformation of drugs and xenobiotics. Signup and view all the answers

Name three flavonoids that demonstrated potent inhibition of aldehyde oxidase (AO)?

Myricetin, quercetin, and epicatechin. Signup and view all the answers

Why is it important to study the interaction of drugs with aldehyde oxidase (AO)?

To understand how they might alter the metabolism of drugs and xenobiotics. Signup and view all the answers

Study Notes

Natural Products Chemistry: Emerging Trends and Prospective Goals

Natural products chemistry plays a vital role in advancing physical and biological sciences, providing novel applications and a broader perspective for future research.
Emerging trends in the field include advancements in methodology, techniques, and potential applications in biomedicine, health, nutrition, and related areas.
The declining interest in natural products chemistry due to lack of prioritization, availability of tools, and financial resources has been revived.
Modern research into natural product chemistry is crucial for understanding biotic and abiotic processes in the environment.

Scope and Outreach

Renewed interest in natural products chemistry due to its impact on scientific knowledge, technical progress, and economic activities.
The field's importance in bioengineering, medicinal domains, and technological advancements is highlighted.
Natural products continue to play a significant part in drug discovery (~50% of modern drugs).

Synthetic and Semi-synthetic Drugs

Synthetic products revolutionized drug discovery in the 1980s, with more than one-third of current drugs derived from natural resources.
The adverse effects and regulatory requirements of synthetic drugs have spurred interest in naturally derived compounds.
Semi-synthetic analogs of natural products have been developed by modifying structural features to enhance biological activities.

Separation Sciences and Structure Elucidation

Advanced separation and detection techniques enhanced natural products research, enabling isolation and identification of minor-yield products.
Chromatographic techniques (e.g., Flash®, UHPLC, MPLC) are crucial in characterizing natural products.
Computational models allow for predicting chromatographic sequences aiding in compound identification.

Genomics, Combichem & HTS

Genomics research contributes to natural product identification and understanding their roles in various biological processes.
High-Throughput Screening (HTS) methods involving purified natural products and natural product libraries are utilized in template selection.
Libraries of natural products facilitate the discovery of novel bioactive compounds and potential drug candidates.

Biomechanics and Bioactivity

Chemical biology approaches aid in understanding the mechanisms of action of natural products, contributing to the development of complex disease therapies.
Natural products exhibit diverse bioactivities (e.g., anti-cancer, anti-microbial).
The ability to decipher biomechanics of natural products facilitates optimization of clinical potentials and formulations.

Ecology, Environment & Chemical Perspective

Environmental alterations in habitats and resources, authenticity, purity, contaminations, and toxicity, and the scope of phytopharmaceuticals and other derived products are significant concerns.
Natural approaches exist for resource protection, cultivation, and biodiversity maintenance to enhance sustainable systems from a chemical perspective.

Microbial, Marine, and Photochemistry

Microbial chemistry, particularly from marine sources, remains a rich source of bioactive compounds.
Photochemical reactions in natural products also provide insights into biogenesis and drug discovery potential.

Bioactive and Designer Foods, Plant Microbe Relations, etc.

The discovery and production of natural food supplements and formulations for enhanced nutritional values is in increasing demand.
Consideration of the impacts of plant-microbe relations on biosynthesis and biological activities is crucial for future research in the field.

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Description

Explore the various origins of drugs, focusing on natural and semi-synthetic sources. The quiz delves into the significance of natural products chemistry and the challenges faced by synthetic drugs. Test your knowledge on the retro-approach in chemical synthesis and its role in modern pharmacology.