ChemInform Abstract: Anti‐AIDS Agents. Part 32. Synthesis and Anti‐HIV Activity of Betulin Derivatives.

Abstract

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Pyrazine-Fused Triterpenoids Block the TRPA1 Ion Channel in Vitro and Inhibit TRPA1-Mediated Acute Inflammation in Vivo

“…[12][13][14][15] There is also evidence of their therapeutic potential against cancer, HIV and protozoal diseases. [16][17][18][19][20][21][22][23][24][25] Based on our preliminary screening results, we postulated that some of the pharmacological features of triterpenoids might be attributable to blockade of TRPA1. In the present study, we utilized two in vitro protocols: the Fluo 3-AM intracellular Ca 2+ measurement and whole-cell patch clamp current recording, as well as an in vivo model of acute TRPA1-mediated inflammation to study the effects of betulin (1) and a series of its derivatives (2 -14) on TRPA1.…”

Synthesis and Cytotoxic Evaluation of Novel Ester Derivatives of Betulin with AZT, d4T, and 3TC

“…Betulin (1, Figure 1), one of the most well-known and well-studied triterpenes, has been reported to exhibit multiple biological activities, such as anti-HIV [1], anti-inflammatory [2], antibacterial [3], anticancer [4], and antitumor properties [5]. Modifications of the parent structure of betulin at C-3, C-20, and C-28 positions could produce potentially important derivatives, which were found to be more biologically effective than the staring one [6].…”

“…760 1. H NMR (CDCl 3 , 500 MHz) δ: 8.67 (1H, s, NH), 7.28 (1H, s), 6.14 (1H, t, J = 6.2 Hz), 4.68 (1H, s), 4.58 (1H, s), 4.30-4.26 (2H, m), 4.24-4.20 (1H, m), 4.27 (1H, d, J = 11 Hz), 4.07-4.03 (1H, m), 3.86 (1H, d, J = 11 Hz), 3.19-3.16 (1H, dd, J = 5.0, 11.5 Hz), 2.70-2.62 (4H, m), 2.48-2.35 (3H, m), 1.93 (3H, s), 1.67 (3H, s), 1.02 (3H, s), 0.97 (3H, s), 0.96 (3H, s), 0.82 (3H, s), 0.67 (3H, s).…”