Synthesis of 2-(2-oxo-2H-chromen-3-yl)-3-phenylquinazolin-4(3H)-ones as potent antimicrobial and antitubercular agents

2021 ◽  
pp. 100744
Author(s):  
B. Suresh Kuarm ◽  
Hanumaiah Marumamula ◽  
B. Rajitha
2011 ◽  
Vol 8 (8) ◽  
pp. 750-757 ◽  
Author(s):  
Prashant T. Mistry ◽  
Nimesh R. Kamdar ◽  
Dhaval D. Haveliwala ◽  
Saurabh K. Patel

2019 ◽  
Vol 15 (5) ◽  
pp. 369-383
Author(s):  
Rahul Balasaheb Aher ◽  
Kunal Roy

Tuberculosis, malaria, dengue, chikungunya, leishmaniasis etc. are a large group of neglected tropical diseases that prevail in tropical and subtropical countries, affecting one billion people every year. Minimal funding and grants for research on these scientific problems challenge many researchers to find a different way to reduce the extensive time and cost involved in the drug discovery cycle of these problems. Computer-aided drug design techniques have already been proved successful in the discovery of new molecules rationally by reducing the time and cost involved in the development of drugs. In the current minireview, we are highlighting on the molecular modeling studies published during 2010-2018 for target specific antitubercular agents. This review includes the studies of Structure-Based (SB) and Ligand-Based (LB) modeling and those involving Machine Learning (ML) techniques against different antitubercular targets such as dihydrofolate reductase (DHFR), enoyl Acyl Carrier Protein (ACP) reductase (InhA), catalase-peroxidase (KatG), enzyme antigen 85C, protein tyrosine phosphatases (PtpA and PtpB), dUTPase, thioredoxin reductase (MtTrxR), etc. The information presented in this review will help the researchers to get acquainted with the recent progress in the modeling studies of antitubercular agents.


2019 ◽  
Vol 19 (7) ◽  
pp. 875-915 ◽  
Author(s):  
Amr M. Abdelmoniem ◽  
Magda F. Mohamed ◽  
Doaa M. Abdelmoniem ◽  
Said A.S. Ghozlan ◽  
Ismail A. Abdelhamid

In this review, the recent synthetic approaches of amino hexahydroquinolines and their spirocyclic structures were highlighted. The synthetic routes include, two-components, three-components or fourcomponents reactions. The two-component [3+3] atom combination reaction represents the simplest method. It involves Michael addition of the electron rich β-carbon of β-enaminones to the activated double bond of cinnamonitriles followed by cyclization to yield hexahydroquinoline compounds. The bioactivity profiles and SAR studies of these compounds were also reviewed with emphasis to the utility of these substances as antimicrobial, anticancer and antitubercular agents, as well as calcium channel modulators.


2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Shankar Alegaon ◽  
Kamlesh Kashniyal ◽  
Sanket Kuncolienkar ◽  
Rohini Kavalapure ◽  
Preeti Salve ◽  
...  

2011 ◽  
Vol 78 (4) ◽  
pp. 718-724
Author(s):  
Daniele Pietra ◽  
Marcello Imbriani ◽  
Alice Borghini ◽  
Irene Giorgi ◽  
Federico Da Settimo ◽  
...  

2007 ◽  
Vol 50 (13) ◽  
pp. 2942-2950 ◽  
Author(s):  
Mohammad Saquib ◽  
Manish K. Gupta ◽  
Ram Sagar ◽  
Yenamandra S. Prabhakar ◽  
Arun K. Shaw ◽  
...  

2021 ◽  
Vol 18 ◽  
Author(s):  
Monika Kakadiya ◽  
Yunus Pasha ◽  
Malleshappa Noolvi ◽  
Ashish Patel

: Tuberculosis remains a highly infectious disease across the world. In the identification of new antitubercular agents, coumarin clubbed thiadiazole amides have been synthesized and evaluated for in vitro antitubercular activity. Due to the growing concern about chemicals and their impact on the environment, greener and faster reaction conditions needed to be incorporated. Therefore, we used TBTU as a coupling reagent for efficient and facile synthesis of substituted-N-(5-((7-methyl-2-oxo-2H-chromes-4-yl)-methyl)-1,3, 4 - thiadiazol-2-yl)-benzamide 4a-j with good yields up to 95% in mild reaction condition. All the synthesized compounds were evaluated in vitro for antitubercular activity against the H37Rv strain of M.Tuberculosis. Compounds 4c, 4f, and 4j were found active at 25 µg/mL against M. tb H37Rv. Electron withdrawing substituents present on aromatic side-chain showed promising anti-tubercular activity.


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