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GPR55(G protein-coupled receptor 55)	1

Background: Antimicrobial resistance is growing quickly throughout the world due to extensive and indiscriminate use of antibiotics. Reduction of indole derivatives comprises a very important and interesting branch of synthetic organic chemistry as these reactions are utilized in the synthesis of several drugs, dyes, agrochemicals and higher alkaloids. Objective: The objective of the present study is to assess the antibacterial properties of six indole derivatives viz, 3-(Naphth-1-y - methyl) –indole (II), 3-(1-Naphthylcarbonyl – indole (III), 3,3' –diformyl-2,2' –bis indole (IV), 1,4- (3,3' –di indolyl) – 1,4-dioxobutane (V), 3-benzoyl indole (VI) and 1,1 – bis – (3-indolyl)- ethane (VII) synthesized by single electron transfer reduction of 3-formylindole (I) against two Gram +ve and two Gram –ve bacteria which usually cause human infections. Methods: Synthesis of 3-formyl indole from which the indole derivatives were prepared were further characterized by IR and NMR analysis. The six synthesized compounds were screened for their antibacterial activity by agar diffusion method and the activities were further confirmed by determining their MIC values by microdilution technique. Results: All of the compounds more or less showed activity against different bacterial species except compound IV which showed activity only against B. subtilis. Compound II exhibited the most potent activity with lower MIC values against two Gram –ve and one Gram +ve bacteria of which the Gram –ve ones are known to be responsible for nosocomial and community acquired infections. Conclusion: Compound II being the most potent active compound may serve as leads for further optimization most likely to contribute as a broad spectrum antibiotic.

01 Apr 2021·Journal of the Indian Chemical Society

An intramolecular oxa-Michael addition on prebuilt β-lactam tethered α, β-unsaturated ester: A remarkable synthesis of a unique scaffold of 2,3-fused β-lactam-1,4-dioxepane

Author: Bimal K. Banik ; Armando Paniagua ; Ram N. Yadav

An expeditious base assisted highly diastereoselective intramol. oxy-Michael addition reaction in the synthesis of enantiomerically pure 1,4-dioxepane fused β -lactam I (Ph, 4-methoxyphenyl; R¹ = Me, Et) has been described.This present study has been portrayed a rapid intramol. 7-exo-trig oxy-Michael reaction involving chemoselective nucleophilic addition of 20 alc. of the vic-diols II to an α β-unsaturated Ester, III.Furthermore, the developed methodol. elaborates an extremely atom-economical approach in constructing the C-O bond in stereoselective fashion under mild reaction conditions.

01 Mar 2021·Silicon

New Nano-Bioactive Glass/Magnesium Phosphate Composites by Sol-Gel Route for Bone Defect Treatment

Author: H. H. Liu ; M. M. Farag ; A.H. Makhlouf

Abstract: This work was mainly aimed to synthesize new ceramic composites based on nano-bioactive glass (nBG) and magnesium phosphate ceramic (MgP) with different ratios using the sol-gel approach in order to overcome the limitations of both materials.The glass was based on 85SiO₂-10CaO-5P₂O₅ (mole %), and MgP was based on the formula; Mg₃(PO₄)₂.The obtained composites were characterized by DTA, XRD, FTIR, SEM/EDX and Zeta potential techniques.The in vitro bioactivity test was carried out in SBF, and the cell viability test was conducted by culturing the composites with human normal fibroblast cell line (BJ1).The results of XRD analyses showed that there were often no strong diffraction peaks detected which indicated the amorphous nature of the ceramic composites.Moreover, soaking of the ceramic composites in SBF exhibited that addition of MgP to nBG was increased the degradation of the latter one, and nBG was improved the formation of apatite crystals on MgP ceramic.Moreover, the cell viability results showed that MgP was showed significant higher viability than nBG at high concentrations, and it improved the viability of nBG in the ceramic composites.

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Pipeline

Pipeline Snapshot as of 15 Nov 2024

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

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