Title |
Synthesis, solubility, plasma stability, and pharmacological evaluation of novel sulfonylhydrazones designed as anti-diabetic agents
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Published in |
Drug Design, Development and Therapy, September 2016
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DOI | 10.2147/dddt.s108327 |
Pubmed ID | |
Authors |
Gisele Zapata-Sudo, Isabelle Karine da Costa Nunes, Josenildo Segundo Chaves Araujo, Jaqueline Soares da Silva, Margarete Manhães Trachez, Tiago Fernandes da Silva, Filipe P da Costa, Roberto Takashi Sudo, Eliezer J Barreiro, Lídia Moreira Lima |
Abstract |
Neuropathy is a serious complication of diabetes that has a significant socioeconomic impact, since it frequently demands high levels of health care consumption and compromises labor productivity. Recently, LASSBio-1471 (3) was demonstrated to improve oral glucose tolerance, reduce blood glucose levels, and display an anti-neuropathy effect in a murine streptozotocin-induced diabetes model. In the present work, we describe the design, synthesis, solubility, plasma stability, and pharmacological evaluation of novel sulfonylhydrazone derivatives (referred to herein as compounds 4-9), which were designed by molecular modification based on the structure of the prototype LASSBio-1471 (3). Among the compounds tested, better plasma stability was observed with 4, 5, and 9 in comparison to compounds 6, 7, and 8. LASSBio-1773 (7), promoted not only hypoglycemic activity but also the reduction of thermal hyperalgesia and mechanical allodynia in a murine model of streptozotocin-induced diabetic neuropathic pain. |
X Demographics
Geographical breakdown
Country | Count | As % |
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Unknown | 1 | 100% |
Demographic breakdown
Type | Count | As % |
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Practitioners (doctors, other healthcare professionals) | 1 | 100% |
Mendeley readers
Geographical breakdown
Country | Count | As % |
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Brazil | 1 | 5% |
Unknown | 19 | 95% |
Demographic breakdown
Readers by professional status | Count | As % |
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Professor | 2 | 10% |
Other | 2 | 10% |
Student > Doctoral Student | 2 | 10% |
Student > Postgraduate | 2 | 10% |
Professor > Associate Professor | 2 | 10% |
Other | 5 | 25% |
Unknown | 5 | 25% |
Readers by discipline | Count | As % |
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Chemistry | 6 | 30% |
Pharmacology, Toxicology and Pharmaceutical Science | 4 | 20% |
Physics and Astronomy | 2 | 10% |
Biochemistry, Genetics and Molecular Biology | 1 | 5% |
Unspecified | 1 | 5% |
Other | 1 | 5% |
Unknown | 5 | 25% |