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
Keyword(s):  
Antitubercular Agents

Concise and Facile Synthesis of Novel Pyrano[2,3-d]pyrimidine-7- one/thione Derivatives as In Vitro Antimicrobial and Antitubercular Agents

2011 ◽  
Vol 8 (8) ◽  
pp. 750-757 ◽  
Author(s):  
Prashant T. Mistry ◽  
Nimesh R. Kamdar ◽  
Dhaval D. Haveliwala ◽  
Saurabh K. Patel
Keyword(s):  
Antitubercular Agents ◽  
Facile Synthesis

Computational Approaches as Rational Decision Support Systems for Discovering Next-Generation Antitubercular Agents: Mini-Review

2019 ◽  
Vol 15 (5) ◽  
pp. 369-383
Author(s):  
Rahul Balasaheb Aher ◽  
Kunal Roy
Keyword(s):  
Recent Progress ◽  
Neglected Tropical Diseases ◽  
Acyl Carrier Protein ◽  
Thioredoxin Reductase ◽  
Protein Tyrosine Phosphatases ◽  
Antitubercular Agents ◽  
Computer Aided Drug Design ◽  
Modeling Studies ◽  
Catalase Peroxidase ◽  
Molecular Modeling Studies

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.

Recent Synthetic Approaches and Biological Evaluations of Amino Hexahydroquinolines and Their Spirocyclic Structures

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
Keyword(s):  
Double Bond ◽  
Calcium Channel ◽  
Michael Addition ◽  
Antitubercular Agents ◽  
Sar Studies ◽  
Two Component ◽  
Synthetic Routes ◽  
Synthetic Approaches ◽  
Three Components

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.

scholarly journals Correction to: Synthesis and biological evaluation of some 4-aminoquinoline derivatives as potential antitubercular agents

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Shankar Alegaon ◽  
Kamlesh Kashniyal ◽  
Sanket Kuncolienkar ◽  
Rohini Kavalapure ◽  
Preeti Salve ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Antitubercular Agents ◽  
Synthesis And Biological Evaluation

Structure-Activity Relationships on Purine and 2,3-Dihydropurine Derivatives as Antitubercular Agents: a Data Mining Approach

2011 ◽  
Vol 78 (4) ◽  
pp. 718-724
Author(s):  
Daniele Pietra ◽  
Marcello Imbriani ◽  
Alice Borghini ◽  
Irene Giorgi ◽  
Federico Da Settimo ◽  
...  
Keyword(s):  
Data Mining ◽  
Antitubercular Agents ◽  
Structure Activity Relationships ◽  
Data Mining Approach ◽  
Structure Activity

C-3 Alkyl/Arylalkyl-2,3-dideoxy Hex-2-enopyranosides as Antitubercular Agents:  Synthesis, Biological Evaluation, and QSAR Study

2007 ◽  
Vol 50 (13) ◽  
pp. 2942-2950 ◽  
Author(s):  
Mohammad Saquib ◽  
Manish K. Gupta ◽  
Ram Sagar ◽  
Yenamandra S. Prabhakar ◽  
Arun K. Shaw ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Antitubercular Agents ◽  
Qsar Study

Synthesis of Substituted -N-(5-((7-Methyl-2-Oxo-2H-Chromen-4-yl)-Methyl)-1,3,4-Thiadiazol-2-yl)-Benzamide Derivatives Using TBTU As Coupling Agent And Their Evaluation For Anti Tubercular Activity

2021 ◽  
Vol 18 ◽  
Author(s):  
Monika Kakadiya ◽  
Yunus Pasha ◽  
Malleshappa Noolvi ◽  
Ashish Patel
Keyword(s):  
Antitubercular Activity ◽  
Side Chain ◽  
Antitubercular Agents ◽  
Facile Synthesis ◽  
Aromatic Side Chain ◽  
Reaction Conditions ◽  
Coupling Reagent ◽  
H37rv Strain ◽  
Benzamide Derivatives

: 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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