scholarly journals Design, microwave-assisted synthesis, bioactivity and SAR of novel substituted 2-phenyl-2-cyclohexanedione enol ester derivatives

RSC Advances ◽  
2018 ◽  
Vol 8 (35) ◽  
pp. 19883-19893 ◽  
Author(s):  
Fei Ye ◽  
Peng Ma ◽  
Yue Zhai ◽  
Fei Yang ◽  
Shuang Gao ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Microwave Assisted Synthesis ◽  
Microwave Assisted ◽  
Structure Activity ◽  
Herbicide Safeners ◽  
Enol Ester

Based on the structure–activity relationship and active substructure combination, a novel class of substituted 2-phenyl-2-cyclohexanedione enol ester derivatives was designed for use as potential herbicide safeners.

Microwave-assisted synthesis of new sulfonyl hydrazones, screening of biological activities and investigation of structure–activity relationship

2016 ◽  
Vol 25 (8) ◽  
pp. 1590-1607 ◽  
Author(s):  
Nurcan Karaman ◽  
Emine Elçin Oruç-Emre ◽  
Yusuf Sıcak ◽  
Berna Çatıkkaş ◽  
Ayşegül Karaküçük-İyidoğan ◽  
...  
Keyword(s):  
Biological Activities ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Microwave Assisted Synthesis ◽  
Microwave Assisted ◽  
Structure Activity

Recursive Partitioning Analysis and Anti-Tubercular Screening of 3- Aminopyrazine-2-Carbohydrazide Derivatives

2019 ◽  
Vol 16 (11) ◽  
pp. 1264-1275
Author(s):  
Pankaj Miniyar ◽  
Anand Mahajan ◽  
Dattatray Anuse ◽  
Ashish Kumar ◽  
Mahesh Barmade ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Recursive Partitioning ◽  
Research Work ◽  
Structure Activity Relationship ◽  
Classification Model ◽  
Activity Relationship ◽  
Microwave Assisted Synthesis ◽  
Significant Activity ◽  
Standard Drug ◽  
Structure Activity

Background: Treating tuberculosis is a challenge due to the development of drug resistance. Hence, it is imperative to develop novel leads having high potency and efficacy to curb drug resistance. Methods: The present research work is focused on microwave-assisted synthesis of novel twenty-six 3-amino-N’-benzylidenepyrazine-2-carbohydrazide derivatives (3a-z), where, lyophilization technique was used for isolation of the major intermediate, 3-aminopyrazin-2-carbohydrazide. All synthesized compounds were subjected for anti-tubercular screening against Mycobacterium tuberculosis H37Ra by using XTT Reduction Menadione Assay (XRMA) protocol. Results: Out of 26 synthesized compounds, four N’-substitutedbenzaldehyde-3-amino-pyrazine-2- carbohydrazide derivatives viz. 3i, 3j 3v and 3z showed significant activity against M. tuberculosis H37Ra. The compounds 3i, 3j, 3v and 3z showed 99, 98, 92 and 87 % inhibition respectively as compared to 94% inhibition shown by the standard drug rifampicin. The MIC and IC50 values were in the range of 24.3-110 and 5.9-20.8 µg/ml respectively. Conclusion: A classification model called Recursive Partitioning (RP) based on binary Quantitative Structure-Activity Relationship (QSAR) was derived for the establishment of structure-activity relationship (SAR). The predictions derived on the basis of RP model were found to be in agreement with anti-tubercular screening data.

scholarly journals A review on microwave assisted synthesis, mechanism of action and structure activity relationship of 1, 3, 4-oxadiazoleA review on microwave assisted synthesis, mechanism of action and structure activity relationship of 1, 3, 4-oxadiazole derivatives as anticancer agent derivatives as anticancer agent

2021 ◽  
Vol 9 (1) ◽  
pp. 086-096
Author(s):  
Deeksha Tiwari ◽  
Rakesh Narang ◽  
Sukhbir Lal khokra
Keyword(s):  
Mechanism Of Action ◽  
Anticancer Agent ◽  
Activity Relationship ◽  
Microwave Assisted Synthesis ◽  
Research Groups ◽  
Synthesis Mechanism ◽  
Microwave Assisted ◽  
Structure Activity ◽  
Oxadiazole Derivatives ◽  
Relationship Of

1, 3, 4-oxadiazole derivatives received considerable attention of different research groups, as they have wide variety of biological activities. 1, 3, 4-oxadiazole derivatives exhibited noteworthy anticancer activities. In recent years, microwave-induced organic reactions attained significant attention due to several benefits, such as short reaction time, cost-effectiveness, excellent yield, and ease of work. In view of above in present work, SAR and mechanism of action of 1, 3, 4-oxadiazole derivatives as anticancer agents, reported by different research groups in recent years are summarized. Present review also highlighted the various synthetic approaches for efficient microwave-assisted green synthesis of 1, 3, 4-oxadiazole derivatives.

Structure-activity relationship of (-) mammea A/BB derivatives against Leishmania amazonensis

Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
MA Brenzan ◽  
CV Nakamura ◽  
BPD Filho ◽  
T Ueda-Nakamura ◽  
MCM Young ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Leishmania Amazonensis ◽  
Activity Relationship ◽  
Structure Activity ◽  
Relationship Of
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