Question

You are working in a Drug Discovery Center, and your group developed several active compounds for different cardiovascular disorders. After screening these compounds, two had better pharmacological effects in in vitro studies, and your group wants to test them in vivo. Before planning the in vivo study, your manager assigned you to study their long-term stability (at least two years) in solution and plasma at -4 °C, room temperature, and -20 °C. Please explain your inclusive proposals (experiment design, instrumental and analytical method, etc. and how you will collect the data and analyze them) for studying each of these compounds (10 points for each compound with a total of 20 points). Compound A: MW = 346 Lop P = 2.966 Solubility: DMSO 69 mg/mL Water < 1 mg/ml R = Small alkyl group Compound B: has a chiral center MW = 266 Lop P = 0.2 Solubility: Water 13.3mg/ mL, Freely soluble in Me OH, CH3COOH, DMSO Sparingly soluble in EtOH, Isopropyl Insoluble in ACN, Ethyl acetate, and CHCL3 R = Small alkyl group

          You are working in a Drug Discovery Center, and your group developed several active compounds for different cardiovascular disorders. After screening these compounds, two had better pharmacological effects in in vitro studies, and your group wants to test them in vivo. Before planning the in vivo study, your manager assigned you to study their long-term stability (at least two years) in solution and plasma at -4 °C, room temperature, and -20 °C. Please explain your inclusive proposals (experiment design, instrumental and analytical method, etc. and how you will collect the data and analyze them) for studying each of these compounds (10 points for each compound with a total of 20 points).

Compound A:
MW = 346
Lop P = 2.966
Solubility:
DMSO 69 mg/mL
Water < 1 mg/ml
R = Small alkyl group

Compound B: has a chiral center
MW = 266
Lop P = 0.2
Solubility:
Water 13.3mg/ mL,
Freely soluble in Me OH, CH3COOH, DMSO
Sparingly soluble in EtOH, Isopropyl
Insoluble in ACN, Ethyl acetate, and CHCL3
R = Small alkyl group

You are working in a Drug Discovery Center, and your group developed several active compounds for different cardiovascular disorders. After screening these compounds, two had better pharmacological effects in in vitro studies, and your group wants to test them in vivo. Before planning the in vivo study, your manager assigned you to study their long-term stability (at least two years) in solution and plasma at -4 °C, room temperature, and -20 °C. Please explain your inclusive proposals (experiment design, instrumental and analytical method, etc. and how you will collect the data and analyze them) for studying each of these compounds (10 points for each compound with a total of 20 points).

Compound A:
MW = 346
Lop P = 2.966
Solubility:
DMSO 69 mg/mL
Water < 1 mg/ml
R = Small alkyl group

Compound B: has a chiral center
MW = 266
Lop P = 0.2
Solubility:
Water 13.3mg/ mL,
Freely soluble in Me OH, CH3COOH, DMSO
Sparingly soluble in EtOH, Isopropyl
Insoluble in ACN, Ethyl acetate, and CHCL3
R = Small alkyl group

Added by Rachelle L.

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