Podcast – Editorial: Image Perception

Journal Name: Current Medical Imaging
Formerly: Current Medical Imaging Reviews

Podcast by Author(s): Euishin Edmund Kim.

Volume 15 , Issue 9 , 2019

Web: https://www.eurekaselect.com/174515/a…

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Podcast | In Silico Appraisal, Synthesis, Antibacterial Screening and DNA Cleavage for 1,2,5-thiadiazole Derivative

Author(s): Suraj N. Mali*, Sudhir Sawant, Hemchandra K. Chaudhari*, Mustapha C. Mandewale

 

Graphical Abstract:

 

Abstract:

Background: Thiadiazole not only acts as “hydrogen binding domain” and “two-electron donor system” but also as constrained pharmacophore.

Methods: The maleate salt of 2-((2-hydroxy-3-((4-morpholino-1, 2,5-thiadiazol-3-yl) oxy) propyl) amino)- 2-methylpropan-1-ol (TML-Hydroxy)(4) has been synthesized. This methodology involves preparation of 4-morpholino-1, 2,5-thiadiazol-3-ol by hydroxylation of 4-(4-chloro-1, 2,5-thiadiazol-3-yl) morpholine followed by condensation with 2-(chloromethyl) oxirane to afford 4-(4-(oxiran-2-ylmethoxy)-1,2,5-thiadiazol- 3-yl) morpholine. Oxirane ring of this compound was opened by treating with 2-amino-2-methyl propan-1- ol to afford the target compound TML-Hydroxy. Structures of the synthesized compounds have been elucidated by NMR, MASS, FTIR spectroscopy.

Results: The DSC study clearly showed that the compound 4-maleate salt is crystalline in nature. In vitro antibacterial inhibition and little potential for DNA cleavage of the compound 4 were explored. We extended our study to explore the inhibition mechanism by conducting molecular docking, ADMET and molecular dynamics analysis by using Schrödinger. The molecular docking for compound 4 showed better interactions with target 3IVX with docking score of -8.508 kcal/mol with respect to standard ciprofloxacin (docking score= -3.879 kcal/mol). TML-Hydroxy was obtained in silico as non-carcinogenic and non-AMES toxic with good percent human oral absorption profile (69.639%). TML-Hydroxy showed the moderate inhibition against Mycobacteria tuberculosis with MIC 25.00 μg/mL as well as moderate inhibition against S. aureus, Bacillus sps, K. Pneumoniae and E. coli species.

Conclusion: In view of the importance of the 1,2,5-thiadiazole moiety involved, this study would pave the way for future development of more effective analogs for applications in medicinal field. For article details, please visit: http://www.eurekaselect.com/169670/article

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Podcast | Simultaneous Determination of Substance P and CGRP in Rat Brainstem Tissue Using LC-ESI-MS/MS Method

Journal Name: Current Analytical Chemistry

Author(s): Neva Alasağ*, Erol Şener, Dilek Doğrukol-Ak.

For article details, please visit: http://www.eurekaselect.com/158976

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Podcast | Concise Review on the Applications of Magnetically Separable Brønsted Acidic Catalysts

Journal Name:Current Organic Chemistry 

Author(s): Jagatheeswaran Kothandapani, Subramaniapillai S. Ganesan*.

 

 

 

For article details, please visit: http://www.eurekaselect.com/170659

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Podcast | Simultaneous Determination of Substance P and CGRP in Rat Brainstem Tissue Using LC-ESI-MS/MS Method

Author(s): Neva Alasağ*

Journal Name: Current Analytical Chemistry

 

For article details, please visit: https://bit.ly/2HtsTS7

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PODCAST: Therapeutic Potential Of Small Activating RNAs (saRNAs) In Human Cancers

PODCAST BY: SORAH YOON

FOR ARTICLE DETAILS, PLEASE VISIT: http://www.eurekaselect.com/162489

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PODCAST: Journey of 2′-deoxy-2′-fluoro-5-methyl-1-β-D-arabinofuranosyluracil (FMAU)

 

 

PODCAST BY: MIAN M. ALAUDDIN

 

FOR ARTICLE DETAILS, PLEASE VISIT: http://www.eurekaselect.com/157824

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PODCAST: Curcumin as an Adjunct Therapy and microRNA Modulator in Breast Cancer

 

 

Podcast by Dr. Muhammed Majeed

Author(s): Saeed Norouzi, Muhammed Majeed, Matteo Pirro, Daniele Generali,Amirhossein Sahebkar*.

 

For article details, please visit: http://www.eurekaselect.com/157866

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PODCAST: Preparation and Characterization of Stable Nanosuspension for Dissolution Rate Enhancement of Furosemide: A Quality by Design (QbD) Approach

 

PODCAST BY: DR. MOHSIN KAZI

 

Author(s): Akbar L. Marzan, Rahnuma Tabassum, Basarat Jahan, Mehedi H. Asif, Hasan M. Reza, Mohsin Kazi*,Sultan M. Alshehri, Marcel de Matas, Mohammad H. Shariare*.

For article details, visit: http://www.eurekaselect.com/159279/article

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PODCAST: The Role of Carbonic Anhydrase in Hepatic Glucose Production

Author(s):  Ibrahim S. Ismail*

For article details, visit: http://www.eurekaselect.com/148340

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