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

Design, synthesis and evaluation of Coumarin-Phenylthiazole conjugates as cholinesterase inhibitors

Design, synthesis and evaluation of Coumarin-Phenylthiazole conjugates as cholinesterase inhibitors

urn:nbn:sciencein.cbl.2019v6.111

Published in Chemical Biology Letters

  • Deepak Mishra Delhi Technological University
  • Atiya Fatima Delhi Technological University
  • Ram Singh Delhi Technological University
  • Nupur S Munjal Jaypee University of Information Technology
  • Vineet Mehta Jaypee University of Information Technology
  • Udayabanu Malairaman Jaypee University of Information Technology

Keywords: Alzheimer’s Disease, Brain disease, medicinal chemistry, coumarin derivative, AChE, BuChE, Nervous system, Neurological

Abstract

In this paper, we report the design, synthesis, in-silico, and in-vitro evaluations of a series of coumarin-phenylthiazole conjugates to inhibit cholinesterase enzymes. The coumarin and phenylthiazole derivatives have been synthesized separately, and further combined through covalent amine bond linkage. The synthesized compounds showed more inhibition towards BuChE than AChE, where 4-(3-bromophenyl)-1,3-thiazol-2-amine (7i) exhibited the strongest inhibition against BuChE with an IC50 value of 3.54 μM. For the conjugates, 3-{2-[4-(3-nitrophenyl)thiazol-2-ylamino]acetyl}chromen-2-one (8j) exhibited strongest inhibition with an IC50 value of 46.47 μM.  The better inhibition activities towards BuChE are also shown by 3-bromo and 2-fluoro derivatives. It was also observed that the substitution at 3-position, on phenylthiazole moiety produced better results against BuChE than 4-substituted counterparts.

Cite as: Mishra, D., Fatima, A., Singh, R., Munjal, N., Mehta, V., & Malairaman, U. (2019). Design, synthesis and evaluation of Coumarin-Phenylthiazole conjugates as cholinesterase inhibitors. Chemical Biology Letters6(2), 23-30.

Retrieved full text from http://pubs.thesciencein.org/journal/index.php/cbl/article/view/111

Clinical and Pre-Clinical advances in Medicinal Chemistry – Special Issue Chemical Biology Letters

The medicinal Chemistry, the science concerned with development of new drug molecules, has produced many new drug entities recently which has reach in the clinical trial stages of evaluation. This special issue is meant to cover the research advances in development of new drug molecules and science behind it (including molecular modeling and pharmaceutical science) along with the research advances with new molecules that has shown promising potential to move to clinical applications.

Medicinal Chemistry fraternity is invited to submit their manuscript (Research Articles, Review Articles, and Short Communications) for publication in this special issue.

Issue Editors:

Dr. Brijesh Rathi,
Department of Chemistry, Hansraj College,
University of Delhi, Delhi-110007. India
Visiting Assistant Professor, Department of Chemistry
Massachusetts Institute of Technology (M.I.T.)
77 Massachusetts Ave. Cambridge, MA 02139, USA EB,
Dr. Prakasha Kempaiah,
Department of Medicine, Loyola University Medical Center
Health Sciences Division 2160 South 1st Avenue
Maywood, Chicago, IL 60153, USA


Submission

Article (Research articles and Review Articles) should be submitted online on the journal site http://www.pubs.thesciencein.org/journal/index.php/cbl as per author guidelines. Authors need to indicate submission to special issue in cover letter to editor.

Submission Deadline October 16, 2019

There is no publication charges for publishing in special issue or in Chemical Biology Letters.



Critical evaluation of pharmaceutical rational design of Nano-Delivery systems for Doxorubicin in Cancer therapy

Critical evaluation of pharmaceutical rational design of Nano-Delivery systems for Doxorubicin in Cancer therapy

Published in: Journal of Materials NanoScience

urn:nbn:sciencein.jmns.2019v6.95

Running title: Rationale of designing of nanoparticular delivery systems and impact of chemistry used with doxorubicin for anti-cancer therapy

  • Bhupender S. Chhikara University of Delhi
  • Brijesh Rathi University of Delhi
  • Keykavous Parang Chapman University

Keywords: Adriamycin, Cancer Drug, CPP, Drug Delivery System, Lipophilic Dox, TAT peptide

Abstract

Doxorubicin (Dox), an antineoplastic drug, has been extensively used for the treatment of different cancers. Dox is hydrophilic and therefore distributes to normal organs at a faster rate. Due to its required high doses, it poses severe toxicity, such as cardiotoxicity and nephrotoxicity. Diverse approaches, including nanoparticulate delivery systems, have been designed and evaluated to improve its delivery to the target site and reduce toxicity to normal organs; however, this has met little success. Here in this review, we have discussed various systems (metal nanoparticles, carbon nanotubes, fullerenes, liposomes, dendrimers, cyclic peptides, and other covalent/non-covalent systems) that have been used for Dox. We have critically evaluated their designing and outcome (in vitro and in vivo) with potential applications in the clinical setting.

Cite as: Chhikara, B., Rathi, B., & Parang, K. (2019). Critical evaluation of pharmaceutical rational design of Nano-Delivery systems for Doxorubicin in Cancer therapy. Journal of Materials NanoScience, 6(2), 47-66.

Retrieved full text from http://pubs.thesciencein.org/journal/index.php/jmns/article/view/95

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.

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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.

Ethical Uses Declaration:

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.

Helsinki Declaration (contents from NIH-NLM): When reporting experiments on human subjects, authors should indicate whether the procedures followed were in accordance with the ethical standards of the responsible committee on human experimentation (institutional and national) and with the Helsinki Declaration of 1975, as revised in 2000 (5). If doubt exists whether the research was conducted in accordance with the Helsinki Declaration, the authors must explain the rationale for their approach, and demonstrate that the institutional review body explicitly approved the doubtful aspects of the study. When reporting experiments on animals, authors should be asked to indicate whether the institutional and national guide for the care and use of laboratory animals was followed.

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