A synthetic route to C(4/5)-bis(phosphinoyl)imidazole-2-thiones (7d,e) (d: R(1) = (n)Bu, R(2) = Me; e: R(1) = n-dodecyl, R(2) = Me) and C(4/5)-bis(thio/selenophosphinoyl)imidazole-2-thiones (8b,c), (9a,b,e) and 10a (a: R(1) = R(2) = Me; b: R(1) = R(2) = Ph, c: R(1) = (i)Pr, R(2) = Me) is presented that employs initial C(5) lithiation of mono-phosphinoyl/thiophosphinoyl substituted imidazole-2-t...

The activity of Prunus dulcis (sweet almond) β-glucosidase at the expense of p-nitrophenyl-β-d-glucopyranoside at pH 6 was determined, both under steady-state and pre-steady-state conditions. Using crude enzyme preparations, competitive inhibition by 1-5 mM imidazole was observed under both kinetic conditions tested. However, when imidazole was added to reaction mixtures at 0.125-0.250 mM, we d...

Nine Candida strains (one C. dublinienses , six Candida albicans, two C. tropicalis, and one C. krusei ) isolated from human genital specimens were characterized based on their susceptibility to amphotericin B and imidazole (done by an adaptation of the National Clinical Laboratory Standards Broth Macrodilution method). All the nine strains were susceptible to amphotericin B with minimum inhibi...

When aqueous solutions of DNA were treated with 10-500 grays of gamma-rays, the imidazole rings of some adenine and guanine residues underwent scission, resulting in the conversion of these purines to formamidopyrimidines. It was found that formamidopyrimidine-DNA glycosylase, known to remove imidazole-ring-opened 7-methylguanine from DNA, did not excise the radiation-induced non-alkylated form...

An easy and versatile Cu-catalyzed propargylic substitution process is presented. Using easily prepared prochiral dichloro substrates, readily available Grignard reagents together with catalytic amount of copper salt and chiral ligand, we accessed a range of synthetically interesting trisubstituted chloroallenes. Substrate scope and nucleophile scope are broad, providing generally high enantios...

The intramolecular alpha-arylation of aldehydes via organo-SOMO catalysis was investigated using density functional theory (B3LYP and M06-2X functionals). The geometries, spin densities, Mulliken charges, and molecular orbitals of the reacting enamine radical cations were analyzed, and the nature of the resulting cyclized radical cation intermediates was characterized. In agreement with experim...

Polysubstituted pyridinium salts are valuable pharmacophores found in many biologically active molecules. Their synthesis typically involves the use of multistep procedures or harsh reaction conditions. Here, we report water-based phosphate mediated reaction conditions that promote the condensation of arylacetaldehydes with amines to give 1,3,5-pyridinium salts. The reaction, carried out at pH ...

The inability to meet the desired outcomes of anticancer treatment and decrease in success bacterial fungal infections accelerated research these areas. Our group has conducted numerous studies, especially on benzimidazole ring systems’ antiproliferative antimicrobial activities. In this study, activity compounds was tested against A549, A498, HeLa, A375, HepG2 cancer cell lines by MTT assay. A...