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Abstract

TECHNOLOGY DEVELOPMENT AND DESIGN OF NOVEL 1, 3, 5-TRI SUBSTITUTED-1H-INDOLE-2, 3-DIONE HIV-1 INHIBITORS WITH DISPLAYS STRATEGIC NANOMOLAR CYTOTOXICITY.

Rahul Hajare*, Smita Kulkarni, Madhuri Thakar and Ramesh Paranjape

ABSTRACT

Model speeds drug discovery a series of novel, twenty 1,3,5-tri substituted-1H- indole 2,3-dione scaffold on a putative „U shape‟ molecular recognition of novel HIV-1 inhibitors were designed and synthesized using a parallel synthesis unit processes technology. Among synthesized and tested compounds 1A, 1B, 1C, 1D, 1E, 1F, 1G and 1H found good quality of IC50 ranges from 4.91 to 32.01μg. One among those, compound 1C is the most potent inhibitor as a target compound against HIV-1. Target compound N-[(3Z) 5-methoxy-1-(morpholin-4-ylmethyl)-2-oxo-1,2-dihydro-3H-indol-3ylidene]amino} benzene sulfamethaxazole (1C) tactically very low cytotoxicity (CC50>1mM). It is reported 7.15 ug/ml to engineered cell lines, TZM- l (JC53BL-13).

Keywords: N-[(3Z) 5-methoxy-1-(morpholin-4-ylmethyl)-2-oxo-1,2-dihydro-3H-indol-3ylidene]amino.


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