Lu, Rong-Jian published the artcileHeterobiaryl Human Immunodeficiency Virus Entry Inhibitors, Formula: C3H5BN2O2, the publication is Journal of Medicinal Chemistry (2009), 52(14), 4481-4487, database is CAplus and MEDLINE.
Previously disclosed HIV (human immunodeficiency virus) attachment inhibitors, exemplified by BMS 806 (formally BMS 378806), are characterized by a substituted indole or azaindole ring linked to a benzoylpiperazine via a ketoamide or sulfonamide group. In the present report, we describe the discovery of a novel series of potent HIV entry inhibitors in which the indole or azaindole ring of previous inhibitors is replaced by a heterobiaryl group. Several of these analogs exhibited IC50 values of less than 5 nM in a pseudotyped antiviral assay, and a methylisoxazolylphenyloxoacetyl piperazine was demonstrated to exhibit potency and selectivity similar to those of BMS 378806 against a panel of clin. viral isolates. Moreover, current structure-activity relation studies of these novel biaryl gp120 inhibitors revealed that around the biaryl, a fine crevice might exist in the gp120 binding site. Taken in sum, these data reveal a hitherto unsuspected flexibility in the structure-activity relationships for these inhibitors and suggest new avenues for exploration and gp120 inhibitor design.
Journal of Medicinal Chemistry published new progress about 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C3H5BN2O2, Formula: C3H5BN2O2.
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