Development of a convenient procedure for the synthesis of cyclic non-peptide analogues of the HIV-1 protease inhibitor and modeling their properties

The development of methods for obtaining new physiologically active substances is one of the most important areas for modern organic chemistry. Bis (α-aminoalkyl) phosphinic acids of the symmetric structure are known to be effective HIV-1 protease inhibitors, as well as intermediate products for the preparation of some non-peptide analogs of the HIV-1 protease inhibitor of the cyclic structure. We previously described a series of procedures for the synthesis of N-protected bis (α-aminoalkyl) phosphinic acids by double amino alkylation of hydrophosphoryl compounds. Also, the cyclization of free bis (α-aminoalkyl) phosphinic acids allowed us to obtain several non-peptide cyclic analogs of the HIV-1 protease inhibitor. The present work is devoted to the use of bis (α-aminoalkyl) phosphinic acids as “building blocks” in combination with a “structural water mimic” for the formation of potent non-peptide HIV protease inhibitors. Also, we conducted a predictive analysis of the obtained substances for physiological activity and toxicity.