Carbonic anhydrase inhibitors: Inhibition of Plasmodium falciparum carbonic anhydrase with aromatic/heterocyclic sulfonamides—in vitro and in vivo studies

Malaria parasite carbonic anhydrase: inhibition of aromatic/heterocyclic sulfonamides and its therapeutic potential

“…In this review, we discuss our extending the previous works for detecting potent sulfonamide CA inhibitors (CAIs) targeting malaria CAs. We focus the in vitro pfCA inhibition studies with the second library of aromatic/ heterocyclic sulfonamides possessing a large diversity of scaffolds [72] . The most effective CAIs for pfCA were also assayed in vitro, for the inhibition of the parasite growth in cell cultures, as well as in vivo, in an animal model of drug testing for human malaria, i.e., mice infected with P. berghei.…”

“…They showed no cytotoxicity in human KB and BC cells. [72] In vitro inhibition data of sulfonamides 1-34 against recombinant purified pfCA enzyme, in vitro data for the growth inhibition of P. falciparum in cell cultures as well as in vivo antimalarial data in mice infected with P. berghei, are shown in Table 3. Acetazolamide AZA has been included as standard sulfonamide CAI.…”

“…Chemical structures of aromatic/heterocyclic sulfonamide carbonic anhydrase inhibitors and AZA [72]. Coumarine sulfonamide derivatives are 21-32. antimalarial activity (Table 3).…”

Cloning, expression and purification of the complete domain of theη-carbonic anhydrase fromPlasmodium falciparum

“…Thus, targeting Plasmodium CA for blocking the pyrimidine metabolic pathways might provide a promising route for novel drug development with high affinity and selectivity for the Z-CAs over the human a-CAs 40,45,61,62 . The P. falciparum CA gene (accession number AAN35994.2, PlasmoDB: PF3D7_1140000) encodes a 600 amino acid polypeptide chain [63][64][65][66][67] . In 2004, Krungkrai et al 63 cloned a truncated form of this gene encoding for a polypeptide chain formed by the amino acid residues from position 211 to 445 (235 amino acid residues) and it was named PfCA1.…”

Study of reactivity of cyanoacetohydrazonoethyl-N-ethyl-N-methyl benzenesulfonamide: preparation of novel anticancer and antimicrobial active heterocyclic benzenesulfonamide derivatives and their molecular docking against dihydrofolate reductase

“…It is evident from the literature survey that benzenesulfonamides exhibited a significant anticancer and antimicrobial activity [1][2][3][4] . Furthermore, benzenesulfonamides derivatives having aromatic heterocyclic moiety possess a wide spectrum of pharmacological activities, such as anticancer [5][6][7] , anti-bacterial [8][9][10] , anti-inflammatory 11 and anti-viral 12 , hypoglycemic 13 , diuretic 14,15 , anticarbonic anhydrase 16 and anti-thyroid 17 , antimalarial 18 and antileprotic 19,20 activity. In addition, literature survey exhibited that some of the synthesized benzenesulfonamide derivatives were found to be dihydrofolate reductase (DHFR) inhibitors [21][22][23] .…”