Synthesis and antimicrobial activity of some 3-[1-phenylethyl]-5-substituted-2H-tetrahydro-1, 3, 5-thiadiazine-2-thione derivatives

In a search for potential antimicrobial compounds thirteen new 3-[1-phenylethyl,]-5- substituted-tetrahydro-2H-1, 3, 5-thiadiazine-2-thiones were synthesized by the reaction of alpha-phenethylamine with carbon disulfide and potassium hydroxide, followed by formaldehyde and the appropriate alkyl, aralkylamines, glycine or ethyl glycinate [Scheme 1]. The chemical structure of the synthesized compounds was elucidated by spectral data and elemental analysis. The title compounds were tested in vitro, for antimicrobial activity against Gram-positive, Gram-negative bacteria, and some fungi, using agar disc method. The antimicrobial activity was found to be affected by the bulkiness of the side chain and presence of polar group at N [5] position. The highest activity was obtained with compounds 41 and 4m [R = CH [2]-COOH, CH [2]- COOC [2] H [5]]

Formulation and evaluation of croconazol hydrochloride topical gels

This study was designed to evaluate different polymers for their suitability as a vehicles for topical drug delivery systems. Croconazol hydrochloride is an azol derivative used as antimycotic agent. It was incorporated in this vehicles as a gel forms in a concentration of 1.0% w/w. Polymers used in this study are methylcellulose [MC], Tylose [Ty], Polyvinyl alcohol [PVA,], Pluronic F-127 [pl. F-127], Polyethylene glycol [PEG], Carbopol 974P [Carb.] and Eudispert mv. [Eud]. They were used in a suitable concentration for gel formulation. In-vitro release characteristics of the drug from different gels were carried out using dialysis membrane in phosphate buffer pH 5.2. The release data were treated with various kinetic principles to assess the relevant parameters. The general rank order of Croconazol hydrochloride release from the prepared gel were MC > Ty > pl. F-127 > PVA > Carb > Eud > PEG. The results showed that, the release of drug from the prepared gels obeyed the diffusion model [Higuchi's equation]. Some kinetic parameters were calculated such as diffusion coefficient, permeability coefficient and the partition coefficient. The results indicated a direct dependence of the release rate on the diffusion coefficient. The influence of initial drug concentration [0.5, 1.0 and 2.0% w/w], and p1 F-127 concentratio,2 [20, 25, 30% w/w] on the release patterns was studied The obtained data revealed an inverse correlation between the drug release rate and the pluronic F-127 concentration and a direct correlation between the drug release rate and the initial drug concentration. The anti-fungal activity of the different gel formulations was evaluated by agar-cup plate technique using five fungal species. The results obtained indicated that, all gel formulations have good anti-fungal activities

Susceptibility of certain varieties and genotypes and control of wilt and root rot diseases of sesame attributed to fusarium oxysporum f sp sesami and macrophomina phaseoli.

Eight fungal isolates were obtained from naturally diseased sesame plants suffering from wilt and root rot diseases. These isolates were identified as Fusarium oxysporum f. Sp. Sesami and Macrophomina phaseoli. Fusarium isolates infected sesame plants causing wilt symptoms and Macrophomina isolates infected sesame plants causing root rot and charcoal stem rot. Varietal resistance on different varieties and genotypes revealed that Giza 32 was less susceptible to infection with F. oxysporum and M. phaseoli than other tested cultivars. Among the tested fungicides, Benlate was the most toxic in vitro. Furthermore, the application of Benlate and Rhizolex-T as soil treatment at concentrations of 0.04-0.1% decreased the percentage of wilt and root rot diseases. Additionally, in a field trial, Benlate proved to be a very effective fungicide in decreasing infection with M. Phaseoli and F. oxysporum when applied at 0.5 g/hill. Bacillus subtilis was isolated from the rhizosphere of sesame plants and showed inhibitory effect against the fungi tested in vitro. The antagonists were able to suppress wilt and root rot diseases when applied to artificially infested soil. Moreover, the addition of 1% organic manure resulted in a greater reduction in infection with wilt and root rot diseases