252025-50-6Relevant articles and documents
Novel Fubinaca/Rimonabant hybrids as endocannabinoid system modulators
Stefanucci, Azzurra,Macedonio, Giorgia,Dvorácskó, Szabolcs,T?mb?ly, Csaba,Mollica, Adriano
, p. 1595 - 1605 (2018/09/14)
The discovery of novel modulators of the cannabinoid system is a current topic in medicinal chemistry. In this paper, we report nine novel carboxamides designed as hybrids of Fubinaca family compounds and Rimonabant. These hybrids were obtained by linking the 1-benzyl-2,5-dichloroindazole-3-carboxylic acid to different amino acids bearing a hydrophobic side chain and three different C-terminus. The new chemical entities were tested in vitro to evaluate their bioactivity by means of receptor binding assays and [35S]GTPγS stimulation assays to reveal their affinity and potency. We found that all compounds were able to bind to the cannabinoid receptors in the low nanomolar range with a marked selectivity towards the CB1 cannabinoid receptor. Some of them are full agonists, whereas the others act as partial agonists. These molecules could be potentially used as anti-obesity agents, antiemetic and analgesics.
Total syntheses of AF-2785 and gamendazole-experimental male oral contraceptives
Veerareddy, Arava,Surendrareddy, Gogireddy,Dubey
, p. 2236 - 2241 (2013/07/25)
Both AF-2785 and gamendazole are experimental male oral contraceptives. The total syntheses of these two compounds are achieved in good yields. Copyright
Lonidamine analogues and their use in male contraception and cancer treatment
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Page/Page column 25-26, (2008/06/13)
Novel compounds useful for inhibiting spermatogenesis and cancer treatment, and in particular as inhibitors of heat shock proteins and/or elongation factor 1 alpha.