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Drug-Receptor Interaction of Peptidic HIV-1 Protease: The Hydrophobic Effect-I

Table 1

First set of peptidic HIV-1-PRIs with observed biological activities

Compd.No	Substiunts				o(log1/C)
Compd.No	R	X	Y	Z	o(log1/C)
1	Cbz^a	H	CHMe₂	Me	5.82
2	Cbz	H	CHMe₂	n-Bu	6.03
3	Qua^b	H	CHMe₂	n-Bu	6.90
4	Cbz	H	CHMe₂	n-Pr	6.29
5	Cbz	H	CHMe₂	Et	6.48
6	Cbz	H	CHMe₂	i-Pr	6.59
7	Cbz	H	CHMe₂	t-Bu	7.46
8	Qua	H	CHMe₂	t-Bu	8.22
9	Cbz	H	CH₂CHMe₂	t-Bu	7.89
10	Qua	H	CH₂CHMe₂	t-Bu	8.52
11	Cbz	H	C₆H₁₁	t-Bu	7.54
12	Qua	H	C₆H₁₁	t-Bu	8.30
13	Cbz	H	C₆H₅	t-Bu	7.72
14	Qua	H	C₆H₅	t-Bu	8.52
15^c	Cbz	Me	C₆H₅	t-Bu	5.19
16^d	Cbz	Me	C₆H₅	t-Bu	5.29
17	Cbz	H	4-Py	t-Bu	6.98
18	Qua	H	4-Py	t-Bu	7.72

^aCarbobenzyloxy. ^bQuinolinyl-2-carboxamide. ^cCHXY in R-configuration. ^dCHXY in S-configuration