Synthesis of novel β-lactam and thiazolidinone compounds derived from 4-methyl-1H-isochromen-1-one and their antibacterial activity

urn:nbn:sciencein.cbl.2019v6.107

Synthesis of novel β-lactam and thiazolidinone compounds derived from 4-methyl-1H-isochromen-1-one and their antibacterial activity

Published in: Chemical Biology Letters

  • Ashish Bhatt Mewar University
  • Krishna Srivastava Shri Ramswaroop Memorial University
  • Ravi Kant Shri Ramswaroop Memorial University
  • Deepa Lakhmani Shri Ramswaroop Memorial University

Keywords: 4-methyl-1H-isochromen-1-one, 1,1-biphenyl-4,4-diamine, Antibacterial activity, anti-microbial activity

Abstract

Selected novel β-lactam and thiazolidinone derivatives have been synthesized by the reaction of 4-methyl-1H-isochromen-1-one with 1,1-biphenyl-4,4-diamine, followed by the reaction with substituted benzaldehyde and further by the reaction with chloroacetyl chloride (for β-lactam type) and with thioglycolic acid (for thiazolidinone type) respectively . All the compounds were characterised by 1H NMR, IR and mass spectroscopy. These compounds were screened for in-vitro antimicrobial activity against Staphylococus aureus, E. coli, Pseudomonas aeruginosa strain. Some compounds have shown very good efficacy against antibacterial strain.

Cite as: Bhatt, A., Srivastava, K., Kant, R., & Lakhmani, D. (2019). Synthesis of novel β-lactam and thiazolidinone compounds derived from 4-methyl-1H-isochromen-1-one and their antibacterial activity. Chemical Biology Letters, 6(2), 46-54.

Retrieved full text from http://pubs.thesciencein.org/journal/index.php/cbl/article/view/107

Chemical libraries targeting Liver Stage Malarial infection

urn:nbn:sciencein.cbl.2019v6.96

Chemical Scaffolds Targeting liver-stage malaria parasite lifecycle

Published in: Chemical Biology Letters

  • Neha Sharma
  • Poonam FNU
  • Prakasha Kempaiah
  • Brijesh Rathi University of Delhi

Keywords: Malaria, Liver stage, Primaquine, Atovaquone, Clinical trials

Abstract

Despite the noteworthy advances in the use of chemotherapy for malaria, it continues to constantly affect large number of individuals. New molecules capable of blocking life-cycle of the parasite, preferably through targeting novel pathways and various modes of action, are increasingly becoming area of interest. Phenotypic screening of large chemical libraries is certainly one of the important criteria for the discovery of new and effective drugs. In recent years, diverse research groups including pharmaceutical industries have performed this large-scale phenotypic screening to identify the potential drug molecules. Most of the antimalarial drugs target blood-stage malarial infection and remain either less potent or ineffective against other life stages i.e. liver-stage, and the gametocyte stages of the parasite. Although, liver stage is considered as a crucial drug target, limited clinical options have significantly hampered the discovery of effective treatments. This short review presents the collection of selective molecules targeting specifically liver stage malaria parasites.

Cite as: Sharma, N., FNU, P., Kempaiah, P., & Rathi, B. (2019). Chemical libraries targeting Liver Stage Malarial infection. Chemical Biology Letters, 6(1), 14-22.

Retrieved full text from http://pubs.thesciencein.org/journal/index.php/cbl/article/view/96

Synthesis, DNA photocleavage, molecular docking and anticancer studies of 2-methyl-1,2,3,4-tetrahydroquinolines

urn:nbn:sciencein.cbl.2019v6.97

Published in: Chemical Biology Letters

  • P.J. Bindu Kuvempu University
  • T. R. Ravikumar Naik Indian Institute of Science
  • K.M. Mahadevan Kuvempu University
  • G. Krishnamurthy Sahyadri Science College

Keywords: Anti-oxidant, photodynamic therapy, DNA-Drug, tetrahydroquinolin

Abstract

2-Methyl-1,2,3,4-tetrahydroquinolin-4-yl)pyrrolidin-2-ones (3a−g) were synthesized by one pot multicomponent aza Diels-alder reaction between N-arylimines with two molecules of N-vinyl-2-pyrrolidinone in presence of Sm(III)nitrate as catalyst in acetonitrile solvent at room temperature stirring. The photocleavage studies with 2-methyl-1,2,3,4-tetrahydroquinolin-4-yl)pyrrolidin-2-ones (3a−g) revealed that almost all derivatives exhibited effective photocleavage of pUC−19 DNA at 365 nm, The The anticancer activities of newly synthesized compounds (3a−g) were more potent than doxorubicin on MCF−7 cells. The docking of PBR receptor (1EQ1) protein with newly synthesized THQ’s (3a-g) exhibited well established bonds with one or more amino acids in the receptor active pocket.

How to Cite Bindu, P., Naik, T. R. R., Mahadevan, K., & Krishnamurthy, G. (2019). Synthesis, DNA photocleavage, molecular docking and anticancer studies of 2-methyl-1,2,3,4-tetrahydroquinolines. Chemical Biology Letters, 6(1), 8-13.

Retrieve Full text from http://pubs.thesciencein.org/journal/index.php/cbl/article/view/97

Medicinal Chemistry in Anti-Cancer and Anti-HIV advances – Special Issue of Chemical Biology Letters

The two prominent diseases i.e Cancer and HIV infections has been putting a challenge to researchers community to find a reliable treatment. There have been newer developments and research advances in finding the cure for these by using chemistry biology interface research. To collect the advances in the filed, a special issue on anti-cancer and anti-HIV therapeutics development would be published in Chemical Biology Letters. The issue will cover the themes (though not limited to as field and research is wide):

– Kinase Inhibitor advances
– new targets for anti-cancer molecules
– development in anti-HIV therapeutics
– Medicinal Chemistry of Anti-Cancer drugs
– Medicinal Chemistry of anti – HIV molecules
– Development in drug delivery systems for anti-cancer and anti-HIV drugs
– Peptides based drug delivery
– Peptide therapeutics
– targeted drug delivery
– Small molecules and Heterocyclic molecules for anti-cancer and anti-HIV therapy

The Medicinal Chemistry community is invited to contribute a ‘Review Article’ ‘Research Article’ or ‘Short Communication’ for processing in special issue.

Submission: The manuscript should be prepared as per details provided on Author Guidelines page: http://pubs.thesciencein.org/author-guidelines-chemical-biology-journal/

The article should be submitted online on the journal site at http://pubs.thesciencein.org/journal/index.php/cbl

Last date for submission of manuscript: ongoing.

Edited by

Dr Parang Prof. Keykavous Parang
Associate Dean of Research, Graduate Studies, and Global Affairs
Professor of Medicinal Chemistry and Pharmacology
Harry and Diane Rinker Health Science Campus
9401 Jeronimo Rd.
Irvine, CA 92618-1908. USA
Email: parang@chapman.edu

Author Guidelines Chemical Biology Journal

Information for Authors

The Authors need to submit a single file containing all the details as described below. The supplementary data files should be submitted as a separate file. A cover letter and graphical abstract should be submitted along with manuscript as details provided below.

Cover letter

Authors should supply a cover letter indicating rational of their work. Cover letter should also have details of at least three reviewers (with email). Cover letter should be provided on the first step of submission in “Comments for Editor’ box.

Graphical Abstract

Authors need to submit a graphical abstract highlighting the contents of manuscript. The guidelines for graphical abstract preparation and submission are available on this link.

Manuscript

Manuscript should include Title, Author (s), Affiliation (complete name of institutions), Abstract, 5 Keywords, (other sections like Introduction, Results and discussion, conclusion, experimental procedures in the main body text of manuscript could be used for full paper article), acknowledgment and references in the listed order. Short communications need not to be arranged in different sections. References should be formatted as shown for articles,1 theses,2 books,3,4 and patents,5

1. R. Ping, M. Laura, P.S. Mario. Title of the journal article should be included here. Int. Lett.Org. Chem. 1996, 61, 4439–4449.

2. B.K. Sharma. Ph.D. Dissertation, Thesis Title, Cornell University, 1995.

3. R. Hussain, D. Shinkoi. Title of book like Synthesis and application of ionic liquid, John Wiley & Sons: New York, 2010.

4. R.S. Buchanod, D.K. Reddy. In Selective Organic Transformations; T.R. Thyagarajan, Ed.; Integrated science: New York, 2002; Vol. 2, pp 1–95.

5. G.L. Loyale, U.S. Patent 5 934 456, 1998; Chem. Abstr. 1998, 65, 2870.

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Authors should mention any conflict of interest in the work submissted to Chemical Biology Letters. The statement about conflict of interest may be mentioned in the ‘Letter to editor’ or placed in the manuscript after acknowledgement section.

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If the manuscript report the experimentation on animals (including clinical trials on human beings), then declaration about ethical way handling of animals and about keeping the complete privacy of human identity (in case of clinical trials) must be mentioned in the manuscript.

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