广谱抗蠕虫新药—氟苯达唑的抗蠕虫作用与应用

本文综述了广谱抗蠕虫新药氟苯达唑的抗蠕虫活性、应用及其安全性,为我国动物蠕虫病的防治提供参考。     

Synthetic and biological studies on a cyclopolypeptide of plant origin

Objective： A natural cyclic peptide previously isolated from Citrus medica was synthesized by coupling of tetrapeptide units Boc-Leu-Pro-Trp-Leu-OMe and Boc-Ile-Ala-Ala-Gly-OMe after proper deprotection at carboxyl and amino terminals followed by cyclization of linear octapeptide segment. Methods： Solution phase technique was adopted for the synthesis of cyclooctapeptide-sarcodactylamide. Required tetrapeptide units were prepared by coupling of Boc-protected dipeptides viz. Boc-Leu-Pro-OH and Boc-Ile-Ala-OH with respective dipeptide methyl esters Trp-Leu-OMe and Ala-Gly-OMe. Cyclization of linear octapeptide unit was done by p-nitrophenyl ester method. The structure of synthesized cyclopolypeptide was elucidated by FTIR, ^1H NMR, ^13C NMR, FABMS spectral data and elemental analysis. The newly synthesized peptide was evaluated for dif- ferent pharmacological activities including antimicrobial, anthelmintic and cytotoxic activities. Results： Synthesis of sarcodactylamide was accomplished with 〉78% yield utilizing dicyclohexylcarbodiimide （DCC） as coupling agent. Newly synthesized peptide possessed potent cytotoxic activity against Dalton＇s lymphoma ascites （DLA） and Ehrlich＇s ascites carcinoma （EAC） cell lines, in addition to moderate anthelmintic activity against earthworms Megascoplex konkanensis, Pontoscotex corethruses and Eudrilus sp. Moreover, cyclopolypeptide displayed good antimicrobial activity against pathogenic fungi Candida albicans and Gram-negative bacteria Pseudomonas aeruginosa, in comparison to standard drugs griseofulvin and ciprofloxacin. Conclusion： Solution phase technique employing DCC and triethylamine （TEA） as base proved to be effective for the synthesis of natural cyclooctapeptide. N-methyl morpholine （NMM） was found to be a better base for the cyclization of linear octapeptide unit in comparison to TEA and pyridine.     

Anthelmintic activity of a benzimidazoline compound in sheep by abomasal infusion

Summary In vitro and in vivo data on the benzimidazoline compound indicate anthelmintic potential when introduced directly into the abomasum.     

Comparison of the effects of imidazo[1,2-a]pyridine-2-carbamates and benzimidazole-2-carbamates on the development ofHymenolepis nana inTribolium confusum

Summary The anthelmintic properties of several imidazo[1,2-a]pyridine carbamates and benzimidazole carbamates againstHymenolepis nana are compared. The results of this study, coupled with previous work, indicate that methyl 6-(trichloroethenyl)-imidazo[1,2-a]pyridine-2-carbamate has the potential of being a broad spectrum anthelmintic, effective against both nematodes and cestodes.Acknowledgments. We are indebted to Miss Marianne Hardy for excellent technical assistance. Our sincere thanks are extended to the Merck, Sharp & Dohme and Hoechst companies for the compounds tested in the present study.     

复合驱羊蠕虫药物对建昌黑山羊和绵羊增重影响的研究

本试验主要测定“晴天”、“体内外驱虫一次净”应用于羊蠕虫病感染羊驱虫后对建昌黑山羊生长和增重的影响,结果表明,这两类药物应用于羊蠕虫病感染羊驱虫后对羊只的生长发育有较好的促进作用,建昌黑山羊和绵羊试验组分别比对照组净增重5.72kg/只和5.36kg/只(平均增重5.54kg),增重效果显著。     

6—正丙氧基苯并噻唑—2—氨基甲酸甲酯的合成

以对硝基苯酚为原料,通过四步反应得到具有驱虫活性的标题化合物,总产率为70％。