In vitro potency of 2-(((2-hydroxyphenyl)amino)methylene)-5,5-dimethylcyclohexane-1,3-dione against drug-resistant and non-replicating persisters of Mycobacterium tuberculosis.

Objectives: New antituberculosis agents active against drug-resistant and non-replicating tubercle bacilli are required. We evaluated a previously identified hit, 2-(((2-hydroxyphenyl)amino)methylene)-5,5-dimethylcyclohexane-1,3-dione (PAMCHD), against several clinical Mycobacterium tuberculosis isolates, including multidrug-resistant (MDR) strains and non-replicating drug-tolerant persisters of M. tuberculosis H37Rv.

The synthesis, biological evaluation and structure-activity relationship of 2-phenylaminomethylene-cyclohexane-1,3-diones as specific anti-tuberculosis agents.

The present study utilised whole cell based phenotypic screening of thousands of diverse small molecules against H37Rv () and identified the cyclohexane-1,3-dione-based structures and as hits. The selected hit molecules were used for further synthesis and a library of 37 compounds under four families was synthesized for lead generation. Evaluation of the library against lead to the identification of three lead antituberculosis agents (, and ).

Oscimum sanctum extract inhibits growth of Gram positive and Gram negative bacterial strains.

In the present study petroleum ether, chloroform and methanolic extracts of Oscimum sanctum were prepared using soxhlet extractor. The extracts were evaluated for antibacterial activity against one Gram positive (Staphylococcus aureus) and one Gram negative (Escherichia coli) strain. The activity of the extracts was compared with the known antibacterial drugs, Oflaxacin and Penicillin G.

In vitro antimycobacterial activity of 2-(((2-hydroxyphenyl)amino)methylene)-5,5-dimethylcyclohexane-1,3-dione: a new chemical entity against Mycobacterium tuberculosis.

This study reports on the in vitro antituberculosis potential of 2-(((2-hydroxyphenyl) amino)methylene)-5,5-dimethylcyclohexane-1,3-dione (PAMCHD) against Mycobacterium tuberculosis H37Rv. PAMCHD has been proven to be a tuberculostatic as well as a tuberculocidal agent by agar and broth dilution methods with minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values equivalent to some standard antituberculosis drugs (ATDs). The dynamics of M.

Preparation and evaluation of antibacterial potential of Pithecellobium dulce root extract against Gram positive and Gram negative bacteria.

In the present study hexane, benzene, ethyl acetate and ethanol extracts of Pithecellobium dulce root were prepared using soxhlet extractor. The extracts were evaluated for antibacterial activity against one Gram positive (Staphylococcus aureus) and three Gram negative (Acetobacter aceti, Acetobacter aceti, Klebsiella pneumoniae) strains. Disc diffusion method revealed promising antibacterial activity of the extracts prepared in polar solvents (ethyl acetate and ethanol) compared to non-polar solvents (hexane and benzene).

Synthesis and in vitro evaluation of 2-(((2-ether)amino)methylene)-dimedone derivatives as potential antimicrobial agents.

The study was designed with an aim to synthesize a series of 2-(((2-ether)amino)methylene)-dimedone derivatives and evaluate the synthesized compounds for antimicrobial activity. Compound library was synthesized by reaction with alkyl, alkenyl, alkynyl and alicyclic bromo-compounds. Characterization of the synthesized compounds was performed by H NMR, C NMR and mass spectral techniques.

Synthesis and screening of ursolic acid-benzylidine derivatives as potential anti-cancer agents.

Ursolic acid present abundantly in plant kingdom is a well-known compound with various promising biological activities including, anti-cancer, anti-inflammatory, hepatoprotective, antiallergic and anti-HIV properties. Herein, a library of ursolic acid-benzylidine derivatives have been designed and synthesized using Claisen Schmidt condensation of ursolic acid with various aromatic aldehydes in an attempt to develop potent antitumor agents. The compounds were evaluated against a panel of four human carcinoma cell lines including, A-549 (lung), MCF-7 (breast), HCT-116 (colon), THP-1 (leukemia) and a normal human epithelial cell line (FR-2).

Promise of Retinoic Acid-Triazolyl Derivatives in Promoting Differentiation of Neuroblastoma Cells.

Retinoic acid induces differentiation in various types of cells including skeletal myoblasts and neuroblasts and maintains differentiation of epithelial cells. The present study demonstrates synthesis and screening of a library of retinoic acid-triazolyl derivatives for their differentiation potential on neuroblastoma cells. Click chemistry approach using copper(I)-catalyzed azide-alkyne cycloaddition was adopted for the preparation of these derivatives.

Metal free stereoselective synthesis of functionalized enamides.

An efficient and expeditious DABCO-mediated synthesis of functionalized enamides from alkenes is delineated. The reaction proceeds through an unprecedented cascade involving an Aza-Michael addition/α-bromination/elimination and a Morita-Baylis-Hillman type reaction to generate functionalized enamides in a regio- & stereoselective fashion.