A novel series of triazole integrated phenyl heteroterpenoids have been synthesized and screened for their in vitro activity against intracellular amastigote form of Leishmania donovani. Among all tested compounds, compound 3a was found to be the most active with IC50 6.4μM and better selectivity index (SI) 18 as compared to reference drugs, miltefosine and miconazole. When evaluated in vivo in L. donovani/hamster model, 3a has exhibited 79±11% inhibition of parasite multiplication at 50mgkg(-1)×5days on day 7 post treatment.
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http://dx.doi.org/10.1016/j.bmcl.2013.03.055 | DOI Listing |
J Hazard Mater
December 2024
State Key Laboratory of Water Environment Simulation, School of Environment, Beijing Normal University, Beijing 100875, China.
Under the widespread use backgrounds of fungicides in paddy-dominated basin, the neglect of fungicide environmental fates may aggravate their pollution risks. By integrating field detection with model simulation, we quantified the loss loads and explored the environmental fates of one thiophosphate and five triazole fungicides. Based on the experimental results, we simulated fungicide loss loads with the coefficient of determination of the verification results greater than 0.
View Article and Find Full Text PDFZhongguo Zhong Yao Za Zhi
October 2024
School of Pharmacy, Shandong University of Traditional Chinese Medicine Ji'nan 250355, China State Key Laboratory of Integration and Innovation of Classic Formula and Modern Chinese Medicine, Lunan Pharmaceutical Group Co., Ltd. Linyi 273400, China.
This study aims to explore the therapeutic effect of Yuzhi Zhixue Granules on polycystic ovary syndrome(PCOS) in rats and explain the underlying mechanism by metabolomics. Rats were randomized into normal, model, low-, medium-, and high-dose(0.5, 1.
View Article and Find Full Text PDFMol Divers
December 2024
Department of Pharmaceutical Chemistry, ISF College of Pharmacy, Moga, Punjab, India.
Acquired immunodeficiency syndrome (AIDS) poses a significant threat to life. Antiretroviral therapy is employed to diminish the replication of the human immunodeficiency virus (HIV), extending life expectancy and improving the quality of patients' lives. These HIV-1 integrase inhibitors form robust covalent interactions with Mg ions, contributing to their tight binding, thereby inhibiting the integration of viral DNA into the CD4 cell DNA.
View Article and Find Full Text PDFBioorg Chem
November 2024
Integrated Drug Discovery Centre, Department of Pharmaceutical Chemistry, Acharya & BM Reddy College of Pharmacy, Bengaluru 560107, Karnataka, India.
Mater Horiz
December 2024
Natural Sciences and Science Education, National Institute of Education, Nanyang Technological University, Singapore 637616, Singapore.
Homojunction engineering holds promise for creating high-performance photocatalysts, yet significant challenges persist in establishing and modulating an effective junction interface. To tackle this, we designed and constructed a novel Janus homojunction photocatalyst by integrating two different forms of triazole-based carbon nitride (CN). In this design, super-sized, ultrathin nanosheets of carbon-rich CN grow epitaxially on a nitrogen-rich honeycomb network of CN, creating a tightly bound and extensive interfacial contact area.
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