Heterocycles from 2-Amino-4-[3,4,5-trimethoxy-phenyl]-Naphtho[2,1-b]-4H-pyran-3-carbonitrile

The TITLE compound 1 was prepared and subjected to react with different electrophilic reagents such as phenyl isothiocyanate, benzoyl chloride, 2-cyanocinnamonitrile, ethoxymethylenediethyl- malonate, formamide and carbon disulphide to give the naphtha-pyranopyrimidine derivative 3, naphtha [2,1-b]-4H-pyran derivative 7-9, naphtha [2,1-b]-4H-pyranopyrimidine 10 and naphtha [2,1-b]-4H-pyrano-1,3-thiazine derivative 11, respectively. Treatment of 3 with ethyl bromoacetate and hydrazine hydrate afforded 4 and 5. The hydrazine derivative 5 reacted with benzoylacetone and yielded the pyrazole derivative 6. The IR, [1]H-NMR and Mass spectra of the synthesized compounds were discussed

Optimising liposome-encapsulated praziquantel formulations for treating and overcoming resistant isolates of schistosoma mansoni

Praziquantel [pzq.] liposomes of [DPPC: Cholesterol] molar ratio 7:2, neutral [N] and negatively [-ve] charged, were prepared by the vortex dispersion method yielding multilamellar vesicles [MLV]. Some MLV were sonicated yielding unilamellar vesicles [ULV]. Entrapped pzq. was measured using UV spectrophotometric analysis at 265 nm. [N] UL and ML liposomes exhibited higher percentage entrapment over the [-ve] liposomes. Swelling at 52° for 24 hours, led to increased percentage entrapment of UL pzq. liposomes. Transmission electron micrographing was employed to characterize ML liposomes. [N] pzq. liposomes, of higher percentage entrapment, were used in curative and prophylactic experiments against susceptible [S] and resistant [R] isolates of S. mansoni, in mice. Pzq. liposomes were injected subcutaneously [s.c.] to effect efficient targeting to the site of infection viz., the liver. The effect of pzq. liposomes, in half dose, was compared to the same dose of free pzq, administered orally and as s.c. injection, in addition to full oral free pzq. [1000 mg/kg]. The curative experiment showed best efficacy for full oral free pzq. On the other hand, [N] pzq. ML liposomes imparted the highest 7-days chemoprophylactic effect against both [S] and [R] isolates of S. mansoni, emphasizing the significant success of such a pharmaceutical formulation in conquering the [R] S. mansoni isolate [EE2] responsible for evolving resistance to pzq. curative effect, in the Egyptian population