Oligopeptide antiretroviral agents

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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548518, 514 18, 514 19, 530331, 530329, 530330, A61K 3700, C07C10352, C07K 706

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active

056166060

ABSTRACT:
Oligopeptide antiretroviral agents are represented by formula (I), wherein A is a moiety bearing a positive charge and of a size which avoids steric inhibition of binding of said compound to nucleic acid sequences associated with the cellular activity of retroviruses; R.sub.1 is a moiety derived from a dicarboxylic acid; Hew is a five-membered heterocyclic moiety; y and z are independently 0, 1, 2 or 3; and x is 0 or 1. These compounds exhibit antiretroviral activity, especially against Human Immunodeficiency Virus (HIV). ##STR1##

REFERENCES:
patent: 4912199 (1990-03-01), Lown et al.
J. Org. Chem. 1991, vol. 56, No. 2, "Sequence-Selective DNA Binding by Linked Bis-N-methylpyrrole Dipeptides: An Analysis by MPE Footprinting and Force Field Calculation", Ekambareswara et al, pp. 786-797.
J. Med. Chem. 1989, vol. 32, No. 10, "Novel Linked Antiviral and Antitumor Agents Related to Netropsin and Distamycin: Synthesis and Biological Evaluation", Lown et al, pp. 2368-2375.

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