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http://nopr.niscpr.res.in/handle/123456789/22569| Title: | Synthesis and anti-HIV activity of novel macrocyclic benzamides with a disulphide bridge |
| Authors: | Jhaumeer-Laulloo, S Witvrouw, M |
| Issue Date: | Nov-2000 |
| Publisher: | NISCAIR-CSIR, India |
| Abstract: | A series of macrocyclic dilactams containing a disulphide bridge has been synthesized by the condensation of 2,2'-dithiodibenzoyl chloride with diamines. These compounds have been evaluated for their ability to inhibit reverse transcriptase (RT) of the human immunodeficiency virus HIV-1 (IIIB) and HIV-2 (ROD) in acutely infected MT-4 cells. The anti-HIV activity of these compounds depends on the ring size and also on the diamino counterpart. The dilactams with 12-membered rings 1 and 5 were found to be the most potent. The active analogues 1 and 5 inhibit the replication of HIV-1 (IIIB) and HIV-2 (ROD) with an EC50 between 1.2 to 4.4 μg/mL. The dilactam 7 shows comparable activity in C8166 cells. |
| Page(s): | 842-846 |
| ISSN: | 0975-0983(Online); 0376-4699(Print) |
| Appears in Collections: | IJC-B Vol.39B(11) [November 2000] |
Files in This Item:
| File | Description | Size | Format | |
|---|---|---|---|---|
| IJCB 39B(11) 842-846.pdf | 1.18 MB | Adobe PDF | View/Open |
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