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KI0984Clotrimazole100 mg$90

Chemical Characteristic

Product NameClotrimazole
SynonymsLotrimin, Bay b 5097
CAS No.23593-75-1
Molecular Weight 344.837
FormulaC22H17ClN2
Chemical Name1-?[(2-?chlorophenyl)?diphenylmethyl]?-1H-?imidazole
SmilesC(c1ncc[nH]1)(c1ccccc1)(c1ccccc1)c1c(cccc1)Cl
Chemical Structure

Biological activities

Clotrimazole is a synthetic antifungal drug with in vitro activity against Candida spp., Torulopsis glabrata, and Saccharomyces spp.. The MIC of clotrimazole for the majority of Candida spp. is 1.56 µg/mL.[1] In vitro, clotrimazole effectively and rapidly inhibits parasite growth in five different strains of P. falciparum. Clotrimazole inhibits parasite growth with IC50 values between 0.2 and 1.1 µM, irrespective of the chloroquine sensitivity of the strain. Clotrimazole alters P. falciparum morphology and interferes with parasite development and replication. [2] Clotrimazole is a potent and specific inhibitor of the Ca2+-activated K+ channel of sickle erythrocytes. Clotrimazole blocks almost completely Ca2+-activated K+ transport in homozygous hemoglobin S cells, with IC50 of 29 nM in isotonic 20 mM salt solution and 51 nM in normal saline. Clotrimazole markedly reduces K+ permeability with IC50 of 33 and 208 nM, in low ionic strength conditions and in normal saline, respectively. Oral administration of clotrimazole prevents red cell dehydration with sickle cell anemia.[3]

References

[1] Burgess MA, et al. Clotrimazole (Bay b 5097): in vitro and clinical pharmacological studies. Antimicrob Agents Chemother. 1972, 2(6): 423-246.
[2] Tiffert T, et al. Potent antimalarial activity of clotrimazole in in vitro cultures of Plasmodium falciparum. Proc Natl Acad Sci U S A. 2000, 97(1): 331-336.
[3] Brugnara C, et al. Inhibition of Ca(2+)-dependent K+ transport and cell dehydration in sickle erythrocytes by clotrimazole and other imidazole derivatives. J Clin Invest. 1993, 92(1): 520-526.

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