Reactions with 2-hydrazinobenzothieno-pyrimidinone: synthesis of benozthienotriazolopyrimidines

The material used in this work was 2-hydrazino-5,6,7,8-tetrahydro- benzothieno [2,3-d] pyrimidine-4[3H] one 1. So, compound 1 reacted with some electrophiles, such as formic acid or carbon disulfide to yield 1,2,4-triazalo [4,3-a] pyrimidine derivatives 2 and 3, respectively. Treatment of compound 1 with the proper aldehydes led to formation of the corresponding hydrazones 4, which cyclized and spontaneously aromatized into 5. Furthermore, photooxidation of some derivatives with the same system was studied

Behaviour of 3,5-diaminopyrazoles towards activated double bond systems: novel synthesis of pyrazolo [1,5-a] pyrimidines

The synthesis of eighteen new pyrazolo [1, 5-a] pyrimidine derivatives containing substituted and naphthyl moieties was reported. They were characterized by their physical properties, elemental and spectral analyses. Some compounds were evaluated as anti-inflammatory agents and indicated a great effect. Other compounds were tested as antifungal and antibacterial agents and some of them indicated a high activity

Role of dietary calcium supplements or calcium channel blockers in protection against gentamcin nephrotoxixity in rats

A great deal of controversies is present about the effects of dietary calcium supplements or calcium channel blockers on gentamicin induced nephrotoxicity.The present study was designed to evaluated the protective effect of either of them against gentamicin nephrotoxicity in rats using the same experimental model Daily I.P. injection of gentamicin 40 mg/kgm/day for 2 weeks in albino rats produced the characteristic pattern of aminoglycosides nephrotoxicity in rats as judged by the significant increase in urine alkaline phosphatase excretion accompanied with a significant decrease in renal tissue alkaline phosphatase and succinic dehydrogenese activities meanwhile cortical renal tissue acid phosphatase activity was increased.Also there was significant glucosuria, albuminuria and increased urine sodium and potassium execretion. Histopathological examination revealed that gentamycin produced extensive tubular degenerative and necrotic changes which were almost restricted to the proximal convoluted tubules. In addition, gentamicin produced a significant elevation of serum creatinine with reduction of creatinine clearance meanwhile volume of urine output was maintained unchanged. Feeding rats a diet with high calcium content [4% calcium carbonate by weight] for 2 weeks before gentamicin and for another 2 weeks concurrently with gentamicin produced a significant protection against gentamicin induced nephrotoxicity as evidenced by the significant correction of all the laboratory measures estimated and almost complete normalization of the histopathological and histochemical alteration produced by gentamicin Oral administration of nifedipine 2 mg/ kgm/day for 2 weeks before gentamicin and for another 2 weeks concurrently with gentamicin injection produced similar protection to that produced by dietary calcium supplements. The possible clinical relevance of this observation is unclear. Patients prone to gentamicin nephrotoxicity may have deficiencies of dietary calcium, hypocalcaemia or hypocalciuria Conceivably, correction of these calcium abnormalities could decrease the likelihood or severity of the toxic injury. It is tempting to further speculate on a possible role of calcium or calcium channel blockers as a therapeutic modality. In this common nephrotoxic insult. However, any conclusion must await further informations concerning the specificity of the protective effect of calcium or calcium channel blockers

Some reactions of 2-chloroquinoline-3-carbaldehydes

It was reported earlier that the reaction of la with hydrazine hydrate in ethanol showed no tendency to cyclize and gave the corresponding hydrazone IIa. This was attributed presumably to unfavourable E-configuration of the hydrazone formed

Reactions of phosphorous oxychloride-amide adducts XIII A novel synthesis of 1-N,N-Dime-thylamino-1-ethoxyethylene

Meerwein et aL[1] succeeded in the preparation of l-N,N-dimethylamino-1-ethoxyethylene [1]. Bredereck and co-workers [2] obtained the ethoxyenamine from the reaction of N,N-dimethylacetamide- dimethylsulphate adduct with sodium ethoxide followed by distillation over calcium metal. Electrophilic addition to the double bond in the ethoxyenamine [1] has been reported. With acid chlorides, the enamine afforded the corresponding beta- ketoamides [3]. We would like to report a direct and simple method for the synthesis of the ethoxyenamine. This compound has now been prepared by the treatment of dimethylacetamide-ethyl chloroformate adduct [4] with triethylamine, whereby CO[2] is evolved