AntiHIV activity

Of nearly 50 iminosugars probed for antiHIV activity [183], five were active at subcytotoxic levels. In particular, the a-glucosidase inhibitors 1-deoxynojirimycin 2 and the plant alkaloid castanospermine 4 were confirmed to be active at concentrations between 0.1 and 0.5 mg/ml. Even more pronounced were the activities of 1-deoxynojirimycin derivatives with enhanced lipophilic character such as V-methyl- 70, V-ethyl- 71 and, in particular, V-butyl-1-deoxynojirimycin 72 in the same concentration range [183,186]. 

Osawa Z., Morota X, Hatanaka K., Akaike X, Matsuzaki K., Nakashima H., Yamamoto N., Suzuki E., Miyano H., Mimura X, Kaneko Y., Synthesis of sulfated derivatives of curdlan and their antiHIV activity, Carbohyd. Polym., 21,1993, 283-288. 

Another dideoxypyrimidine nucleoside active against human immunodeficiency vims is 3 -azido-2/3 -dideoxyuridine [84472-85-5] (AZDU or CS-87, 64) C H N O. Since its synthesis, (167) CS-87 has been identified as a promising antiHIV agent (168) and is currentiy undergoing phase I clinical trials in patients with AIDS and AIDS-related complex. It appears to be less potent than AZT against HIV in a peripheral blood mononuclear (PBM) cell screening system and in MT-4 cell lines. This lower activity in PBM cells appears to be related to a lower affinity of CS-87 for the enzyme responsible for its initial phosphorylation (169). However, CS-87 has significantly lower toxicity on bone marrow cells than AZT (170) and penetration of the CNS as a 5 -dihydropyridine derivative. 

Source Caulophyllum acuminata. Molecular formula C22 Hie O 5. Biological activity AntiHIV. 

Major Applications Fluorescent brighteners, fungicides, cosmetics, antitrypanosomal, " anti-leishmanial activities, " antifungal," antibacterial," Antiinflammatory, 12 antiHIV, detection of microorganisms, - treatment of impaired neurotransmission disorders, Alzheimer s disease, vascular and lymphatic edema cancer, early diagnosis of stroke, " dental material, " drug-coated coronary stent system ... 

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