New praziquantel derivatives containing NO-donor furoxans and related furazans as active agents against Schistosoma mansoni.
New praziquantel derivatives containing NO-donor furoxans and related furazans as active agents against Schistosoma mansoni.
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DOI：
10.1016/j.ejmech.2014.07.007
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发表时间：
2014-09-12
影响因子：
6.7
通讯作者：
Gasco A
中科院分区：
文献类型：
--
作者：
Guglielmo S;Cortese D;Vottero F;Rolando B;Kommer VP;Williams DL;Fruttero R;Gasco A
将吡喹酮（PZQ）和氧化呋咱（Furoxan）结合在一起，合成了一系列NO供体吡喹酮杂合化合物。NO供体性质的氧化呋咱衍生物进行了评价，通过检测亚硝酸盐孵育后的产品在7.4 pH缓冲溶液中的L-半胱氨酸的存在下。结构相关的呋咱，没有NO释放能力，也被合成用于控制目的。研究了所有产物抑制重组曼氏血吸虫硫氧还蛋白谷胱甘肽还原酶（TGR）的能力。与PZQ相比，评价了在存在产品的情况下培养的曼氏血吸虫蠕虫的移动性和死亡。结果分析表明，一些产品同时具有PZQ和NO依赖性抗寄生虫特性。化合物6、7、18和24作为最有趣的平衡杂交体出现，值得对PZQ抗性寄生虫进行额外的研究。
A series of NO-donor praziquantel hybrid compounds was obtained by combining praziquantel (PZQ) and furoxan moieties in a single entity. NO-donor properties of the furoxan derivatives were evaluated by detecting nitrite after incubation of the products in 7.4 pH buffered solution in the presence of L-cysteine. Structurally-related furazans, devoid of NO release capacity, were also synthesized for control purposes. All products were studied for their ability to inhibit recombinant Schistosoma mansoni thioredoxin glutathione reductase (TGR). Mobility and death of adult Schistosoma mansoni worms cultured in the presence of the products were evaluated versus PZQ. Analysis of the results showed that some products were endowed with both PZQ and NO-dependent antiparasitic properties. Compounds 6, 7, 18, and 24 emerged as the most interesting balanced hybrids, worthy of additional study on PZQ-resistant parasites.
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DOI：
10.1007/bf00389899
发表时间：
1977-01-01
期刊：
ZEITSCHRIFT FUR PARASITENKUNDE-PARASITOLOGY RESEARCH
影响因子：
--
作者：
GONNERT, R;ANDREWS, P
通讯作者：
ANDREWS, P
影响因子：
7.3
作者：
Buonsanti, M. Federica;Bertinaria, Massimo;Gasco, Alberto
通讯作者：
Gasco, Alberto
影响因子：
5.8
作者：
FEELISCH, M;SCHONAFINGER, K;NOACK, E
通讯作者：
NOACK, E
影响因子：
7.3
作者：
Di Stilo, A;Visentin, S;Gasco, A
通讯作者：
Gasco, A
DOI：
10.1002/3527603751.ch6
发表时间：
2005-01-01
期刊：
NITRIC OXIDE DONORS: FOR PHARMACEUTICAL AND BIOLOGICAL APPLICATIONS
影响因子：
--
作者：
Gasco, Alberto;Schoenafinger, Karl
通讯作者：
Schoenafinger, Karl