Synthesis, antimalarial, antileishmanial, and antimicrobial activities of some 8-quinolinamine analogues

Primaquine revisited six decades after its discovery

“…Such effect would be similar to what occurs with CQ, i.e., inhibition of heme crystallization through formation of a drug-heme complex, preventing clearance of hemeassociated toxicity from the parasite [166]. These were also presented by Jain et al studies involving several 8AQ compounds obtained by insertion of substituents at the quinolinic ring of PQ [167], where 4-ethyl-5-pentyloxyprimaquine has also displayed promising results [51]. Overall, it seems that insertion of an appropriate substituent at the quinoline's carbon 2 leads to a small improvement in antimalarial activity along with a decrease in general systemic toxicity.…”

“…This produced almost 200 PQ derivatives (Tables 2-4) bearing diverse groups in one or more given positions of the ring [6,46,[161][162][163][164][165][166][167][168][169][170][171][172][173][174][175][176][177][178][179]. Globally, the most favourable substituent insertions towards anti-malarial activity where those of methyl groups at positions 4 and 2, tert-butyl at position 2, simultaneous insertion of ethyl substituents at positions 2 and 4 and pentyloxy at position 5, as well as insertion at position 5 of alkoxy, fluoro, and 3-or 4-substituted phenoxy groups [51,163].…”

Constituents of Nelumbo nucifera leaves and their antimalarial and antifungal activity

“…The assay was based on the determination of plasmodial LDH activity using Malstat ™ reagent and was performed in 96-well plates as described previously (Jain et al, 2005). The level of in vitro cytotoxicity of each sample was also determined towards mammalian kidney fibroblasts (VERO cells) as described earlier (Jain et al, 2005) and the selectivity index (SI) was calculated as the ratio of IC 50 in Vero cells and IC 50 in P. falciparum. Two standard antimalarial agents chloroquine and artemisinin were used as positive controls and DMSO was used as a vehicle control.…”

“…Susceptibility testing was performed using a modified version of the CLSI (formerly NCCLS) methods (NCCLS, 2002;Jain et al, 2005). C. albicans ATCC 90028 was obtained from the American Type Culture Collection (Manassas, VA).…”

Drug Design by Regression Analyses of Newly Synthesized Derivatives of 8-Quinolinol

“…The antibacterial activity of 8-hydroxyquinoline and its derivatives is long-known. The drugs from this group are used as chemotherapeutics in medicine for more than 120 years (9,10,11,21), and in analytical chemistry as chelators (8,12). In previous studies of ours, some newly synthesized derivatives of 8-Quinolinol were shown to exhibit a higher microbiological activity (4,5,15).…”