Table of Contents
- 1 What is the source of lead compound?
- 2 What are the different sources of lead compounds in drug discovery?
- 3 What is a lead compound in drug discovery?
- 4 Where is lead found?
- 5 What are drug sources?
- 6 What are the different methods of drug discovery?
- 7 What is lead identification and lead optimization?
- 8 What does lead optimization mean?
- 9 Are folk remedies a good source of lead compounds?
- 10 What level of exposure to lead is considered safe?
What is the source of lead compound?
Lead occurs naturally in the earth’s crust. It is also found in combined form in several minerals: galena, anglesite, pyromorphite and mimetite. Lead may be released as particles into the atmosphere or as dissolved compounds in water. Lead is also released from natural sources such as windblown dusts and forest fires.
What are the different sources of lead compounds in drug discovery?
The promising sources of lead compound and novel drugs are: Natural products. Chemical libraries. Computational Medicinal Chemistry.
What is a lead compound in drug discovery?
A lead compound (/ˈliːd/, i.e. a “leading” compound, not to be confused with various compounds of the metallic element lead) in drug discovery is a chemical compound that has pharmacological or biological activity likely to be therapeutically useful, but may nevertheless have suboptimal structure that requires …
What is lead optimization in drug discovery?
Lead optimization is a critical process that culminates in the identification of a preclinical candidate. The most promising hit series, once they are identified through hit-to-lead efforts, advance into the lead optimization stage of drug discovery.
What is the main source of lead pollution?
Thus, the main source of lead pollution is from leaded gasoline.
Where is lead found?
Lead can be found in all parts of our environment – the air, the soil, the water, and even inside our homes. Much of our exposure comes from human activities including the use of fossil fuels including past use of leaded gasoline, some types of industrial facilities and past use of lead-based paint in homes.
What are drug sources?
Sources of drugs may be natural, synthetic, and biosynthetic. Drugs of plant, animal, microbiological, marine, mineral, geographical origins constitute the natural sources. The entire plant, plant parts, secretion, and exudate of plants are the sources of plant drugs.
What are the different methods of drug discovery?
For drug discovery, two different complementary approaches can be applied: classical pharmacology, also known as phenotypic drug discovery, which is the historical basis of drug discovery, and reverse pharmacology, also designated target-based drug discovery.
What are the properties of a good lead compound?
It must bind selectively to the receptor site on the target and elicit the desired functional response from the target molecule. It must have sufficient bioavailability and distribution within the body to reach the receptor site, and it must elicit the desired responses in vivo, in animal models of the human disease.
Is lead a compound or element?
Lead is a chemical element with symbol Pb and atomic number 82.
What is lead identification and lead optimization?
Lead identification and optimization is a crucial step in the drug discovery program. Aim of lead optimization is to maximize bonded and non-bonded interactions with the active site of selected drug targets to increase selectivity, improve activity and reduce side effects.
What does lead optimization mean?
Lead optimization is the process by which a drug candidate is designed after an initial lead compound is identified.
Are folk remedies a good source of lead compounds?
The screening of local folk remedies (ethnopharmacology) has been a fruitful source of lead compounds and many important therapeutic agents. For example, the antimalarial quinine from cinchona bark, the cardiac stimulants from foxgloves (Fig. 1.5) and the antidepressant reserpine isolated from Rauwolfia serpentina.
What are the most common sources of lead exposure?
Today, however, the most common sources of lead exposure in the United States are: Lead-based paint in older homes Contaminated soil Household dust Drinking water Lead crystal Lead-glazed pottery
What is a hit molecule in early drug discovery?
Key in vitro assays in early drug discovery. Whatever the screening paradigm, the output of the hit discovery phase of a lead identification programme is a so-called ‘hit’ molecule, typically with a potency of 100 nM–5 µM at the drug target. A chemistry programme is initiated to improve the potency of this molecule.
What level of exposure to lead is considered safe?
There is no level of exposure to lead that is known to be without harmful effects. Lead exposure is preventable. Lead is a naturally occurring toxic metal found in the Earth’s crust. Its widespread use has resulted in extensive environmental contamination, human exposure and significant public health problems in many parts of the world.
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