161798-25-0Relevant articles and documents
Click Chemistry Approach for Bis-Chromenyl Triazole Hybrids and Their Antitubercular Activity
Naik, Reshma J.,Kulkarni, Manohar V.,Sreedhara Ranganath Pai,Nayak, Pawan G.
, p. 516 - 523 (2012)
1,4-Disubstituted bis-chromenyl triazole hybrids 5a-m have been synthesized in a three-step reaction sequence from 4-(bromomethyl)-2H-chromen-2-ones 3a-m. The intermediate azides 4a-m underwent a regioselective 1,3-dipolar cycloaddition with a 2H-chromen-2-one linked acetylenic dipolarophile in the presence of Cu (II)/ascorbate/water/n-butanol reaction medium. Three compounds 5h-j exhibited 6.25μg/mL MIC against M. tuberculosis. Among the compounds screened for antifungal activity, lowest MIC of 6.25μg/mL was observed for 5c against A. niger that also exhibited DNA cleavage observed by agarose gel electrophoresis. All the compounds were moderately active against both Gram-positive and Gram-negative bacterial strains. The cytotoxic effect of potent compounds on normal cells (V79 and HBL100) was assessed by MTT assay.
Synthesis of coumarin-theophylline hybrids as a new class of anti-tubercular and anti-microbial agents
Mangasuli, Sumitra N.,Hosamani, Kallappa M.,Devarajegowda, Hirihalli C.,Kurjogi, Mahantesh M.,Joshi, Shrinivas D.
, p. 747 - 756 (2018)
A series of novel coumarin-theophylline hybrids were synthesized and examined for their anti-tubercular activity in vitro against Mycobacterium tuberculosis H37Rv, anti-microbial activity in vitro against gram-positive bacteria (Staphylococcus aureus) and gram-negative bacterias (Escherichia coli, Salmonella typhi) as well as fungi (Candida albicans). The compound (3a) has shown excellent anti-tubercular activity with MIC of 0.12 μg/mL. Electron donating compounds (3a, 3f) have displayed significant anti-microbial activity. The compounds have also been precisely elucidated using single crystal X-ray diffraction techniques. Molecular docking study has been performed against 4DQU enzyme of Mycobacterium tuberculosis showed good binding interactions and is in agreement with the in vitro results.
Synthesis of a PEGylated polymeric pH sensor and its pH sensitivity by fluorescence resonance energy transfer
Hong, Sung Woo,Ahn, Cheol-Hee,Huh, June,Jo, Won Ho
, p. 7694 - 7700 (2006)
A new pH-sensitive polymeric sensor with dispersion stability and biocompatibility is synthesized, and its pH sensitivity is examined on the basis of the fluorescence resonance energy transfer (FRET) efficiency. The polymeric pH sensor has a FRET donor an
Coumarin polycaprolactone polymeric nanoparticles: light and tumor microenvironment activated cocktail drug delivery
Karthik,Jana, Avijit,Selvakumar,Venkatesh, Yarra,Paul, Amrita,Shah, Sk. Sheriff,Singh, N. D. Pradeep
, p. 1734 - 1741 (2017)
Highly sensitive hypoxia (H2O2)-activated photoresponsive polymeric nanoparticles for cocktail delivery of anticancer drugs doxorubicin (Dox) and chlorambucil (Cbl) were developed. The photoresponsive polymer conjugate was constructe
Synthesis and biological evaluation of novel coumarin derivatives as antioxidant agents
Randive,Jaishree,Patil, K. Santosh,Patil, Kumar
, (2015)
Coumarins have been isolated from plants and reported for antioxidant properties. In the present study, we report synthesis of new coumarin derivatives as prospective therapeutic agents and investigate their antioxidant properties.
Synthesis, characterization, biological evaluation and docking of coumarin coupled thiazolidinedione derivatives and its bioisosteres as PPARγ agonists
Shukla, Shubhanjali,Das, Nirupam,Shrivastava, Sushant Kumar,Srivastava, Radhey Shyam,Kumar, Pankaj,Moorthy, N. S. Hari Narayana,Trivedi, Piyush
, p. 834 - 845,12 (2012)
Thiazolidinedione (TZD) derivatives are the novel class of oral antidiabetic drugs which are selective agonist for the nuclear PPAR γ that enhances the transcription of several insulin responsive genes but TZDs are known to cause weight gain, hepatotoxicity and fluid retention. So a new series of coumarin coupled thiazolidinedione derivatives and its bioisosters (oxazolidinedione and imidazolidinedione) were synthesized by Knoevenagel condensation of 4-((7-hydroxy-2-oxo-2H-chromen-4-yl) methoxy) benzaldehyde with 2,4 thiazolidinedione and its bioisosteres. The structures of these compounds were established by means of FT IR, 1H-NMR, elemental analysis and mass spectroscopy. All the compounds were screened for antidiabetic activity in streptozotocin induced diabetic wistar male rats. Most of the compounds revealed significant antidiabetic activity when compared with the standard drug rosiglitazone. Compounds 5 & 6 containing oxazolidinedione ring system were found to be more active than compounds having thiazolidinedione and imidazolidinedione nucleus. Molecular docking was performed on 2 PRG protein by using the software Glide (Schroedinger, LLC, USA). The QikProp program was used to obtain the pharmacokinetic properties of analogues.
Synthesis and preliminary evaluation of benzofuran-oxadiazole conjugates as potential antitubercular agents
Negalurmath, Veerabhadrayya S.,Kotresh, Obelannavar,Basanagouda, Mahantesha
, p. 965 - 970 (2019/03/07)
In the present study, a series of benzofuran-oxadiazole conjugates 7(a-o) was designed, synthesized and characterized through IR,1H NMR,13C NMR and mass spectral data. All the compounds were screened for preliminary antitubercular activity against Mycobacterium phlei and Mycobacterium tuberculosis H37RV. Among all the target compounds, the compound possessing chlorine (7k, MIC 1.56 μg/mL) and bromine (7m, MIC 1.56 μg/mL) on 6th position of benzofuran showed highest activity against Mycobacterium phlei. Whereas, bromine on either 5th position (7l, MIC 3.125 μg/mL) or 6th position (7m MIC 3.125 μg/mL) on benzofuran exhibited highest activity for Mycobacterium tuberculosis (H37 RV).
