Identification of Pyrazolo[3,4-e][1,4]thiazepin based CYP51 inhibitors as potential Chagas disease therapeutic alternative: In vitro and in vivo evaluation, binding mode prediction and SAR exploration.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.02.020
Abstract: American trypanosomiasis or Chagas disease (CD) is a vector borne pathology caused by the parasite Trypanosoma cruzi (T. cruzi), which remains a serious global health problem. The current available treatment for CD is limited to… read more here.
Keywords: cyp51 inhibitors; chagas disease; pyrazolo thiazepin; vitro vivo ... See more keywords
A convergent, scalable and stereoselective synthesis of azole CYP51 inhibitors.
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DOI: 10.1016/j.tetlet.2017.09.070
Abstract: The study and development of azole-based CYP51 inhibitors is an active area of research across disciplines of biochemistry, pharmacology and infectious disease. Support of in vitro and in vivo studies require the development of robust… read more here.
Keywords: convergent scalable; scalable stereoselective; cyp51 inhibitors; azole ... See more keywords
Design, Synthesis, and Biological Evaluation of Dual-Target COX-2/CYP51 Inhibitors for the Treatment of Fungal Infectious Diseases.
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DOI: 10.1021/acs.jmedchem.2c00878
Abstract: The design of novel dual-target (COX-2/CYP51) inhibitors was proposed in the study, and three series of compounds were constructed though the pathway of skeleton screening and combination; their molecular structures were synthesized and evaluated. Most… read more here.
Keywords: target cox; cyp51 inhibitors; cox cyp51; dual target ... See more keywords
Structure Based Design of CYP51 Inhibitors.
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DOI: 10.2174/1568026616666160719164933
Abstract: Structure based design has been widely used in many drug development programs. In parallel with the evolution of high performance computing systems and versatile molecular modeling programs, structure based drug design has become indispensible in… read more here.
Keywords: drug; structure based; cyp51 inhibitors; structure ... See more keywords