Synthesis of diphenoxyadamantane alkylamines with pharmacological interest

Synthesis and Evaluation of Nifurtimox–Adamantane Adducts with Trypanocidal Activity

“…[3] Fexinidazole, which was recommendedb yt he European Medicines Agency in November 2018, is as uccessful example of the collaboration betweent he Drugs for Neglected Diseases initiative (DNDi)a nd the pharmaceuticalchemistry sector. [6] We have been interested in adamantane chemistry [7][8][9][10][11][12][13][14][15][16][17][18][19][20][21] and have prepared al arge number of analogues in an attemptt o exploit adamantane's role in bioactivity.W ep repared as eries of adamantane carbohydrazones [22] and showedt hat these derivatives are very potent trypanocidals. Following this work, we now describe the preparation of as eries of phenylhydrazone analogues, 1a-d and 2a-d,w hich in general have very promising antitrypanosomal activity.T he new derivatives share common structural features with nifurtimoxa nd also contain a phenyl-substituteda damantane ring.…”

“…[5] This has led the World Health Organization (WHO) to coordinate public sector and private partnerships as part of ag lobale ffort to develop new ands afer dugs. [6] We have been interested in adamantane chemistry [7][8][9][10][11][12][13][14][15][16][17][18][19][20][21] and have prepared al arge number of analogues in an attemptt o exploit adamantane's role in bioactivity.W ep repared as eries of adamantane carbohydrazones [22] and showedt hat these derivatives are very potent trypanocidals. [6] We have been interested in adamantane chemistry [7][8][9][10][11][12][13][14][15][16][17][18][19][20][21] and have prepared al arge number of analogues in an attemptt o exploit adamantane's role in bioactivity.W ep repared as eries of adamantane carbohydrazones [22] and showedt hat these derivatives are very potent trypanocidals.…”

Synthesis of New Indole and Adamantane Amido Derivatives with Pharmacological Interest

“…Based on the fact that 2‐indole carboxamides are targeting MmpL3 transporter functions of M. tuberculosis, we replaced the indole scaffold with the adamantane core in amides 2 c , d , g , h . Our laboratory has previously published various antimycobacterial adamantane adducts with diverse structures …”

Synthesis and evaluation of novel 2,4-disubstituted arylthiazoles against T. brucei

“…1, as potent trypanocidals. 6,7 Based on these findings and our involvement in the adamantane chemistry, [9][10][11][12][13][14][15][16][17][18][19][20] we report herein on the chemistry and biology of thiazole derivatives of the general type scaffold IV. The thiazole moiety is an important pharmacophore in many compounds used against several tropical infectious diseases.…”