222320-76-5

Upstream product

• 149-91-7 3,4,5-trihydroxybenzoic acid 
• 79-22-1 methyl chloroformate 

Downstream Products

• 149-91-7 3,4,5-trihydroxybenzoic acid 
• 861570-63-0 4-hydroxy-3,5-bis-methoxycarbonyloxy-benzoic acid 
• 141992-37-2 3,4,5-Trimethoxycarbonyloxybenzoylchlorid 
• 897932-09-1 (S)-2,6-Bis-(3,4,5-tris-methoxycarbonyloxy-benzoylamino)-hexanoic acid methyl ester 
• 897932-00-2 2,3-bis-(3,4,5-tris-methoxycarbonyloxy-benzoylamino)-propionic acid methyl ester 
• 897932-03-5 2,4-bis-(3,4,5-tris-methoxycarbonyloxy-benzoylamino)-butyric acid methyl ester 
• 897932-06-8 2,5-bis-(3,4,5-tris-methoxycarbonyloxy-benzoylamino)-pentanoic acid methyl ester 
• 222320-78-7 bis(diphenylmethyl) bis(3,4,5-trimethoxycarbonylbenzoyl)-L-tartrate 
• 536-08-3 digallic acid 
• 685876-41-9 4-galloyloxy-benzoic acid 

Relevant academic research and scientific papers

Novel HIV integrase inhibitors and HIV therapy based on drug combinations including integrase inhibitors

The present invention includes a group of novel compounds that are demonstrated to potently and selectively inhibit HIV integrase (IN) activity in vitro and to potently inhibit HIV replication in live, cultured cells at non-toxic concentrations. The novel

Structure-activity relationships: Analogues of the dicaffeoylquinic and dicaffeoyltartaric acids as potent inhibitors of human immunodeficiency virus type 1 integrase and replication

The dicaffeoylquinic acids (DCQAs) and dicaffeoyltartaric acids (DCTAs) are potent and selective inhibitors of human immunodeficiency virus type 1 (HIV-1) integrase. They also inhibit HIV-1 replication at nontoxic concentrations. Since integrase is an excellent target for anti-HIV therapy, structure-activity relationships were employed to synthesize compounds with: (1) improved potency against HIV-1 integrase, (2) improved anti-HIV effect in tissue culture, and (3) increased selectivity as indicated by low cellular toxicity. Thirty-four analogues of the DCTAs and DCQAs were synthesized and tested for cell toxicity, anti-HIV activity, and inhibition of HIV-1 integrase. Seventeen of the 34 analogues had potent activity against HIV-1 integrase ranging from 0.07 to > 10 μM. Seventeen analogues that were synthesized or purchased had no inhibitory activity against integrase at concentrations of 25 μM. Of the biologically active analogues, 7 of the 17 inhibited HIV replication at nontoxic concentrations. The most potent compounds were D-chicoric acid, meso-chicoric acid, bis(3,4- dihydroxydihydrocinnamoyl)-L-tartaric acid, digalloyl-L-tartaric acid, bis(3,4-dihydroxybenzoyl)-L-tartaric acid, dicaffeoylglyceric acid, and bis(3,4-dihydroxyphenylacetyl)-L-tartaric acid. Anti-HIV activity of the active compounds in tissue culture ranged from 35 to 0.66 μM. Structure- activity relationships demonstrated that biscatechol moieties were absolutely required for inhibition of integrase, while at least one free carboxyl group was required for anti-HIV activity. These data demonstrate that analogues of the DCTAs and the DCQAs can be synthesized which have improved activity against HIV integrase.