Synthesis, in vitro and in silico studies of S-alkylated 5-[4methoxyphenyl]-4-phenyl-4H-1, 2, 4-triazole-3-thiols as cholinesterase inhibitors

The research was aimed to unravel the enzymatic potential of sequentially transformed new triazoles by chemically converting 4-methoxybenzoic acid via Fischer's esterification to 4-methoxybenzoate which underwent hydrazinolysis and the corresponding hydrazide [1] was cyclized with phenyl isothiocyanate [2] via 2-[4methoxybenzoyl]-N-phenylhydrazinecarbothioamide [3]; an intermediate to 5-[4-methoxyphenyl]-4-phenyl-4H-1,2,4triazol-3-thiol [4]. The electrophiles; alkyl halides 5[a-g] were further reacted with nucleophilic S-atom to attain a series of S-alkylated 5-[4-methoxyphenyl]-4-phenyl-4H-1,2,4-triazole-3-thiols 6[a-g]. Characterization of synthesized compounds was accomplished by contemporary spectral techniques such as FT-IR, 1H-NMR, 13C-NMR and EI-MS. Excellent cholinesterase inhibitory potential was portrayed by 3-[n-heptylthio]-5-[4-methoxyphenyl]-4-phenyl-4H-1,2,4triazole; 6g against AChE [IC50; 38.35 +/- 0.62?M] and BChE [IC50; 147.75 +/- 0.67micro M] enzymes. Eserine [IC50; 0.04 +/- 0.01?M] was used as reference standard. Anti-proliferative activity results ascertained that derivative encompassing long straight chain substituted at S-atom of the moiety was the most potent with 4.96 % cell viability [6g] at 25 micro M and with 2.41% cell viability at 50?M among library of synthesized derivatives. In silico analysis also substantiated the bioactivity statistics

Effect of Some Food Preservatives on the Lipolytic Activity of Beef Luncheon Fungi

Beef luncheon meat is one of the most popular meals in several countries in the world including Egypt. Thirty one fungal species and 3 species varieties were recovered from 30 samples of beef luncheon meat collected from different supermarkets in Qena. Alternaria, Aspergillus, Emericella, Mucor, Mycosphaerella, Penicillium and Rhizopus were the most common genera on the two types of media. From the above genera, the most prevalent species were Alternaria alternate, Aspergillus flavus, A. fumigatus, A. niger, A. terreus, Emericella nidulans, Mucor racemosus, Mycosphaerella tassiana, Penicillium chrysogenum and Rhizopus stolonifer. Screening of fungi for their abilities to produce lipase enzyme showed that, ten isolates represented 32.26% of total isolates appeared high lipase production, while sixteen isolates (51.61%) were moderate and 5 isolates (16.13%) were low producers. Aspergillus niger, Fusarium oxysporum and Nectria haematococca produced the highest amount of lipase enzyme, so these fungi were used in further studies. The incorporation of five food preservatives (Disodium phosphate, sodium benzoate, citric acid, potassium sorbate and sodium citrate) individually in the culture medium of lipase production exhibited an inhibitive effect on the mycelial growth and enzyme production by Aspergillus niger, Fusarium oxysporum and Nectria haematococca.