Synthesis and biological evaluation of bergenin derivatives as new immunosuppressants

2021 ◽  
Author(s):  
Lihua Deng ◽  
Cheng-Cheng Song ◽  
Youhong Niu ◽  
Qin Li ◽  
Meng Wang ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Pharmacological Properties ◽  
New Type ◽  
Bergenin Derivatives ◽  
Synthesis And Biological Evaluation

Bergenin, which is isolated from Bergenia species, exhibits various pharmacological properties. In the search for new type of immunosuppressants, a series of bergenin derivatives were designed and synthesized, and their...

scholarly journals Design, synthesis and biological evaluation of novel Schiff base-bridged tetrahydroprotoberberine triazoles as a new type of potential antimicrobial agents

MedChemComm ◽  
2017 ◽  
Vol 8 (5) ◽  
pp. 907-916 ◽  
Author(s):  
Jun-Rong Duan ◽  
Han-Bo Liu ◽  
Ponmani Jeyakkumar ◽  
Lavanya Gopala ◽  
Shuo Li ◽  
...  
Keyword(s):  
Schiff Base ◽  
Antimicrobial Agents ◽  
Interaction Mechanism ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
New Type ◽  
Synthesis And Biological Evaluation

Synthesis of a series of Schiff base-bridged tetrahydroprotoberberine triazoles as a new type of potential antimicrobial agents, and preliminary interactions with DNA indicated the possible interaction mechanism.

Design, synthesis, and biological evaluation of novel carbazole aminothiazoles as potential DNA-targeting antimicrobial agents

MedChemComm ◽  
2016 ◽  
Vol 7 (10) ◽  
pp. 1988-1994 ◽  
Author(s):  
Dinesh Addla ◽  
Si-Qi Wen ◽  
Wei-Wei Gao ◽  
Swetha Kameswari Maddili ◽  
Ling Zhang ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Dna Targeting ◽  
New Type ◽  
Synthesis And Biological Evaluation

Synthesis of a series of carbazole aminothiazoles as a new type of potential antimicrobial agents, and preliminary interactions with DNA indicated a possible intercalation mechanism.

Design, synthesis and biological evaluation of amino organophosphorus imidazoles as a new type of potential antimicrobial agents

2017 ◽  
Vol 60 (6) ◽  
pp. 769-785 ◽  
Author(s):  
Wei-Wei Gao ◽  
Syed Rasheed ◽  
VijaiKumarReddy Tangadanchu ◽  
Yi Sun ◽  
Xin-Mei Peng ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
New Type ◽  
Synthesis And Biological Evaluation

scholarly journals Phthalazines and phthalazine hybrids as antimicrobial agents: Synthesis and biological evaluation

2019 ◽  
Vol 44 (1-2) ◽  
pp. 31-41
Author(s):  
Asmaa Kamal Mourad ◽  
Abdelmoneim Abdelsalam Makhlouf ◽  
Ahmed Yousef Soliman ◽  
Samar Ahmed Mohamed
Keyword(s):  
Antimicrobial Agents ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Pharmacological Properties ◽  
Standard Drug ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Benzoic Acid Derivative ◽  
Microbial Strains ◽  
Synthesis And Biological Evaluation

Phthalazine and phthalazinone derivatives are important owing to their significant biological activities and pharmacological properties. Herein, a benzoic acid derivative (2), a benzoxazin-1-one derivative (3), and an oxophthalazin-2(1 H)-yl)acetohydrazide (13) are utilized as precursors to construct a novel series of phthalazinones bearing various valuable functional groups in excellent yields via several simple and promising approaches. Finally, the antimicrobial activity of the newly synthesized phthalazines is screened against different microbial strains; namely, Gram-negative and Gram-positive bacteria utilizing Amoxicillin as a standard drug.

scholarly journals Synthesis and Biological Activity of a Cytostatic Inhibitor of MLLr Leukemia Targeting the DOT1L Protein

Molecules ◽  
2021 ◽  
Vol 26 (17) ◽  
pp. 5300
Author(s):  
Corentin Bon ◽  
Yang Si ◽  
Melanie Pernak ◽  
Magdalena Barbachowska ◽  
Eva Levi-Acobas ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Mixed Lineage Leukemia ◽  
Pharmacological Properties ◽  
Cytostatic Effect ◽  
Acute Leukemias ◽  
Design Synthesis ◽  
Phase Ib ◽  
Histone 3 ◽  
Synthesis And Biological Evaluation ◽  
H3k79 Methylation

Histone methyltransferase DOT1L catalyzes mono-, di- and trimethylation of histone 3 at lysine residue 79 (H3K79) and hypermethylation of H3K79 has been linked to the development of acute leukemias characterized by the MLL (mixed-lineage leukemia) rearrangements (MLLr cells). The inhibition of H3K79 methylation inhibits MLLr cells proliferation, and an inhibitor specific for DOT1L, pinometostat, was in clinical trials (Phase Ib/II). However, the compound showed poor pharmacological properties. Thus, there is a need to find new potent inhibitors of DOT1L for the treatment of rearranged leukemias. Here we present the design, synthesis, and biological evaluation of a small molecule that inhibits in the nM level the enzymatic activity of hDOT1L, H3K79 methylation in MLLr cells with comparable potency to pinometostat, associated with improved metabolic stability and a characteristic cytostatic effect.

Synthesis and Biological Evaluation of a New Type of99mTechnetium-Labeled Fatty Acid for Myocardial Metabolism Imaging

2007 ◽  
Vol 18 (1) ◽  
pp. 216-230 ◽  
Author(s):  
Martin Walther ◽  
Christian M. Jung ◽  
Ralf Bergmann ◽  
Jens Pietzsch ◽  
Katrin Rode ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Myocardial Metabolism ◽  
Biological Evaluation ◽  
New Type ◽  
Synthesis And Biological Evaluation
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