3- and 4-Carbazole dialkylaminocarbinols as potential antimalarial agents

Identification and Optimization of an Aminoalcohol-Carbazole Series with Antimalarial Properties

“…Interestingly, carbazole scaffolds are found in nature with reported antimalarial activity. 20,21 Furthermore, synthetic carbazoles were also described as potential antimalarial agents, 22 Bax channel modulators, 23 and neuroprotective agents. 24,25 Thus, we thought that TDR30137 was a good starting point for a medicinal chemistry program.…”

“…Although the hit exhibited good in vitro potency, it did not show any activity in the in vivo P. Berghei mouse model used. Interestingly, carbazole scaffolds are found in nature with reported antimalarial activity. , Furthermore, synthetic carbazoles were also described as potential antimalarial agents, Bax channel modulators, and neuroprotective agents. , Thus, we thought that TDR30137 was a good starting point for a medicinal chemistry program. Herein, we report the stucture–activity relationship (SAR) study, the physicochemical and in vitro and in vivo DMPK profiling, the in vivo efficacy, and finally the preliminary safety profile of a selected series of compounds that led quickly to the identification of an antimalarial lead.…”

Inhibition of Plasmodium falciparum Hsp90 Contributes to the Antimalarial Activities of Aminoalcohol-carbazoles

“…CBZ derivatives have been known for their antimalarial potency for some time. , N-Substituted CBZ derivatives were first identified as potent antimalarials with a phenotypic screen against the chloroquine-resistant Pf strain K1 . More recently, an extensive SAR analysis of the derivatives bearing modifications at the 3- and/or 6-positions and the N -alkyl of the CBZ core led to the identification of several N-CBZ derivatives with promising antimalarial and pharmacokinetic characteristics .…”

One-pot and metal-free synthesis of atropisomeric carbazolyl-indoles by a facile [4 + 2]-benzannulation in ethanol and investigation of their photoluminescence property

“…5 Carbazole, serving as another distinctive scaffold, also frequently appears in the core structure of various bioactive molecules, such as the antitumor drug Celiptium® (Fig. 1b), 6 as well as in antiviral, 7 antimalarial, 8 and antituberculosis lead drugs. 9 Moreover, due to the merits of favourable donor ability, good planarity, rich photophysical properties and excellent biocompatibility of carbazole derivatives, the rapid advancement of small molecular fluorescent probes based on this scaffold has found widespread application in bioimaging, providing valuable insights into crucial life processes.…”