421581-70-6 Usage
Pharmaceutical effect on Membrance Permeability
The antifungal azoles prevent the synthesis of ergosterol in the fungal membrane. These compounds block ergosterol synthesis by interfering with the demethylation of its precursor, lanosterol. Lanosterol demethylase is a cytochrome P450 enzyme and, although azole antifungals have much less influence on analogous mammalian systems, some of the side effects of these drugs are attributable to such action. Antifungal azole derivatives are predominantly fungistatic but some compounds at higher concentrations, notably miconazole and clotrimazole, kill fungi apparently by causing direct membrane damage. Other, less well characterized, effects of azoles on fungal respiration have also been described.
Pharmaceutical Applications
A large group of synthetic agents, which includes drugs used in
bacterial and parasitic infections (5-nitroimidazoles;
benzimidazoles). Antifungal azoles have in common
an imidazole or triazole ring with N-carbon substitution. The
activity is essentially fungistatic, but some of the newer triazoles
exert fungicidal effects at therapeutic concentrations.
They are effective in the topical treatment of dermatophytoses
and superficial forms of candidosis; several are suitable
for systemic administration.
Several molecular mechanisms of resistance have been elucidated.
These include overexpression of efflux pump genes,
point mutations in the gene that encodes the target enzyme,
lanosterol demethylase, and overexpression of this gene.
Changes in other enzymes involved in ergosterol biosynthesis,
such as sterol desaturase, may also contribute to azole
resistance.
Check Digit Verification of cas no
The CAS Registry Mumber 421581-70-6 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 4,2,1,5,8 and 1 respectively; the second part has 2 digits, 7 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 421581-70:
(8*4)+(7*2)+(6*1)+(5*5)+(4*8)+(3*1)+(2*7)+(1*0)=126
126 % 10 = 6
So 421581-70-6 is a valid CAS Registry Number.
421581-70-6Relevant articles and documents
Microwave assisted synthesis of 3,5-disubstituted 1,2,4-oxadiazoles from substituted amidoximes and benzoyl cyanides
Kandre, Shivaji,Bhagat, Pundlik Rambhau,Sharma, Rajiv,Gupte, Amol
supporting information, p. 3526 - 3529 (2013/07/05)
We report herein the synthesis of 3,5-disubstituted 1,2,4-oxadiazoles from amidoximes and substituted or unsubstituted benzoyl cyanides under microwave irradiation. Substituted or unsubstituted O-carboxyphenyl amidoxime is a key intermediate of this alternative method developed for the synthesis of these heterocycles. These reactions employ simple synthetic protocols devoid of lengthy purification procedures and proceed with good yield.
