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Microwave assisted synthesis and SAR studies of novel hybrid phenothiazine analogs as potential antitubercular agents

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Title Microwave assisted synthesis and SAR studies of novel hybrid phenothiazine analogs as potential antitubercular agents
 
Creator Pemmadi, Raghuveer Varma
Kurre, Purna Nagasree
Guruvelli, Padma Vijaya Sangeetha
Jamullamudi, Risy Namratha
Muthyala, Murali Krishna Kumar
 
Subject Tuberculosis
Phenothiazine
Anti-psychotic
Anti-tubercular
Hybrid pharmacophores
Microwave assisted synthesis
 
Description 556-566
The present work has been initiated based on the interest driven by phenothiazine based neuroleptics with a special focus on thioridazine. Their clinically useful spectrum of anti-TB profile is the motivating factor. A hybrid pharmacophore has been designed containing phenothiazine nucleus and the synthetic reaction conditions have been optimized successfully with the help of a microwave synthesizer. Among the 60 synthesized compounds <strong>4b</strong>, <strong>4e</strong>, <strong>4i</strong> and <strong>4n</strong> show potent <em>in vitro</em> anti TB activity with an MIC 6.25 µg/mL and selectivity index >10.
 
Date 2018-04-12T05:50:12Z
2018-04-12T05:50:12Z
2018-04
 
Type Article
 
Identifier 0975-0983(Online); 0376-4699(Print)
http://nopr.niscair.res.in/handle/123456789/44179
 
Language en_US
 
Rights <img src='http://nopr.niscair.res.in/image/cc-license-sml.png'> <a href='http://creativecommons.org/licenses/by-nc-nd/2.5/in' target='_blank'>CC Attribution-Noncommercial-No Derivative Works 2.5 India</a>
 
Publisher NISCAIR-CSIR, India
 
Source IJC-B Vol.57B(04) [April 2018]