Give a rational approach to drug design and drug development of oxamniquine and cimetadine. The answer should be handwritten in about 10-12 pages
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- Suppose you were given the structural formula of compound B but only the molecular formulas for compound A and the starting bicyclic amine. Given this information, is it possible, working backward, to arrive at an unambiguous structural formula for compound A? for the bicyclic amine?¨ What other types of analgesics are on the market? How does their action compare with aspirin and why are these alternative drugs necessary? Discuss the differences among the following compounds by drawing their structures: Acetylsalicylic acid, Acetaminophen (Paracetamol), Ibuprofen, Paracetamol and Phenacetin.Briefly describe the activities that occur in each step of the drug discovery and development process (i.e. preclinical, clinical, NDA review, post-marketing). What is the purpose of the IND and the NDA and when are they filed with the FDA?
- What metabolic reaction is illustrated by the image below? * СООН СООН -OCOCH3 CH,COOH он + Ester hydrolysis Decarboxylation Nitro- reduction Deamination Azo reductionpropanoic acid + methanol (in concentrated sulfuric acid)Estrogens are female sex hormones, the most potent of which is B-estradiol. OH AYA Но B-Estradiol In recent years, chemists have focused on designing and synthesizing molecules that bind to estrogen receptors. One target of this research has been nonsteroidal estrogen antagonists, compounds that interact with estrogen receptors and block the effects of both endogenous and exogenous estrogens. A feature common to one type of nonste- roidal estrogen antagonist is the presence of a 1,2-diphenylethylene with one of the benzene rings bearing a dialkylaminoethoxyl substituent. The first nonsteroidal estrogen antagonist of this type to achieve clinical importance was tamoxifen, now an important drug in the treatment of breast cancer. Tamoxifen has the Z configuration shown here. NMeg A B NMeg ? ОН Tamoxifen Propose reagents for the conversion of A to tamoxifen. Note: The final step in this synthesis gives a mixture of E and Z isomers.
- Is it possible to classify primary, secondary, and tertiary amines through the quinhydrone test? Explain the basis of your result.What are the present Functional Groups in the drug molecule below. Show complete solution with appropriate labels. Thanks!(i)What class of drug is Ranitidine? (ii)If water contains dissolved Ca2+ ions, out of soaps and synthetic detergents, which will you use for cleaning clothes? (iii)Which of the following is an antiseptic? 0.2% phenol, 1% phenol
- Alkaloids are basic nitrogen-containing compounds of plant origin, many of which are physiologically active when administered to humans. Ingestion of coniine, isolated from water hemlock, can cause weakness, labored respiration, paralysis, and eventually death. Coniine is the toxic substance in the “poison hemlock” used in the death of Socrates. In small doses, nicotine is an addictive stimulant. In larger doses, it causes depression, nausea, and vomiting. In still larger doses, it is a deadly poison. Solutions of nicotine in water are used as insecticides. Cocaine is a central nervous system stimulant obtained from the leaves of the coca plant.Classify each amino group in these alkaloids according to type (primary, secondary, tertiary, aliphatic, aromatic, heterocyclic).classify the molecules of interest (i.e. para-aminophenol, acetaminophen, phenacetin) in increasing order of polarity? Rationalize these observations based on molecular interactions.Write structural formulas for all the amines of molecular formula C4H11N. Give an acceptable name for each one, and classify it as a primary, secondary, or tertiary amine.