De-novo design, synthesis and evaluation of novel 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives as HIV-1 reverse transcriptase inhibitors

Table 1 In-vitro HIV-1 RT inhibition results of the test compounds

Compound code	R	% RT Inhibition^a	Compound code	R	% RT Inhibition^a
5a	H	34.32	8a	2-OCH₃	45.31
5b	2-CH₃	36.23	8b	3-OCH₃	51.32
5c	3-CH₃	39.51	8c	4-OCH₃	57.45
5d	4-CH₃	52.46	8d	3-F	48.37
5e	3-OCH₃	44.21	8e	4-F	53.93
5f	4-OCH₃	56.23	8f	2-Cl	61.38
5g	4-F	28.45	8g	3-Cl	63.74
5h	2-Cl	52.34	8h	4-Cl	74.82
5i	3-Cl	37.26	8i	2-Br	63.38
5j	4-Cl	33.65	8j	3-Br	60.46
5k	4-NO₂	42.78	8k	4-Br	68.63
5l	3-CF₃	30.64	8l	4-CN	72.58
5m	2,6-dimethyl	48.36	8m	3-Aceto	54.75
5n	3,4-dimethyl	58.12	8n	3-CF₃	66.74
5o	2-CH₃-5-Cl	53.76	8o	2,5 dimethyl	63.64
Efavirenz		98.12

^aData are indicated as percentage of inhibition of HIV-1 RT at 100 μM concentration

ISSN: 2661-801X