Vivek D. Bobade

Synthesis and biological evaluation of some novel thiazole substituted benzotriazole derivatives.

A series of novel hybrid molecules 4a-y containing thiazole and benzotriazole templates were designed and synthesized. The structures of the synthesized compounds were elucidated by IR, (1)H NMR, (13)C NMR and mass spectral data. All the synthesized compounds were tested for their antimicrobial activity (zone of inhibition) against Gram-positive, Gram-negative strains of bacteria as well as fungal strains. After that minimum inhibitory concentrations (MICs), minimum bactericidal concentrations (MBCs) and minimum fungicidal concentrations (MFCs) of all the synthesized compounds were determined. The investigation of antimicrobial screening data revealed that most of the tested compounds showed moderate to good microbial inhibitions.

Simple and Efficient One-Pot Synthesis of 2-Substituted Benzoxazole and Benzothiazole

2-Substituted benzoxazole and benzothiazole were synthesized from condensation of aldehyde and 2-aminophenol or 2-aminothiophenol via a one-pot process using diethyl bromo phoshonate and tert-butyl hypochlorite.

Synthesis and pharmacological evaluation of a novel series of 3-aryl-2-(2-substituted-4-methylthiazole-5-yl)thiazolidin-4-one as possible anti-inflammatory and antimicrobial agents

A new series of 3-aryl-2-(2-aryl/benzyl-4-methylthiazole-5-yl)thiazolidin-4-one was synthesized by condensation of 2-aryl/benzyl-4-methylthiazole-5-carbaldehyde, aromatic amines and thioglycolic acid in toluene. All the synthesized compounds are characterized by IR, NMR and elemental or mass analysis. Sixteen out of the newly synthesized compounds were screened for in vivo anti-inflammatory activity using carrageenan-induced rat paw edema method. Some of the synthesized compounds exhibited good anti-inflammatory activity compared with indomethacin. The synthesized compounds were also evaluated for their in vitro antimicrobial activity. Some of the compounds showed mild antibacterial activity while most of the compounds showed good antifungal activity.

Hybrids of ravuconazole: Synthesis and biological evaluation

In continuation of our work on antimicrobial agents, a number of hybrid molecules 4a-y containing thiazole and triazole pharmacophores were designed and synthesized. The structure of the compounds was established by IR, NMR, MS and CHN analysis. All the synthesized compounds were tested for qualitative (Zone of inhibition) and quantitative (MIC) antimicrobial activities against four pathogenic bacteria Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa and two pathogenic fungi Candida albicans and Aspergillus niger. Of all the synthesized compounds screened, most of them show potent antimicrobial activity against Gram positive and Gram negative bacteria as well as the fungi species.

Synthesis and Antimicrobial Activities of Novel Series of 1-((4-Methyl-2-Substituted Thiazol-5-yl)Methyleneam INO)-2-Substituted Isothiourea Derivatives

A novel series of 1-((4-methyl-2-substituted thiazol-5-yl)methyleneamino)-2-substituted isothiourea derivatives was synthesized by alkylation of (Z/E)-1-((4-methyl-2-substituted thiazol-5-yl)methylene)thiosemicarbazide with alkylhalide in acetone. All the newly synthesized compounds were characterized by spectral (IR, 1H NMR, 13C NMR, and mass spectrometry) methods. The newly synthesized compounds were screened for in vitro antimicrobial activity. Most of the compounds show moderate to excellent antimicrobial activity. [Supplementary materials are available for this article. Go to the publishers online edition of Phosphorus, Sulfer, and Silicon and the Related Elements for the following free supplemental files: Additional figures and tables.] GRAPHICAL ABSTRACT

N-Chlorosuccinimide/1,8-Diazabicyclo[5.4.0]undec-7-ene (DBU)–Mediated Synthesis of 2,5-Disubstituted 1,3,4-Oxadiazoles

A mixture of N-chlorosuccinimide and 1,8-diazabicyclo[5.4.0]undec-7-ene oxidatively cyclizes structurally diverse acyl hydrazone, thereby providing an efficient and convenient method for the synthesis of various 2,5-disubstituted 1,3,4-oxadiazoles. The salient features of this method are mild reaction conditions, short reaction time, excellent yields, and simple workup procedure.

An Efficient Synthesis of Zolpidem

Imidazo[1,2-a]pyridines (IPs) have received considerable attention because of their interesting therapeutic properties,1 including antibacterial,2 antifungal,3,4 antiviral,5,6 antiulcer,7 and anti-inflammatory behavior.8 They have also been identified as selective cyclin-dependent kinase inhibitors,9 calcium channel blockers,10 β-amyloidal formation inhibitors,11 and benzodiazepine receptor agonists,12 and constitute a novel class of orally active nonpeptidic bradykinin B2 receptor antagonists.13 Drug formulations containing imidazo[1,2a]pyridines such as alpidem (anxolytic), zolpidem (hypnotic), and zolimidine (antiulcer) are currently marketed.

A ring-closing metathesis approach for the synthesis of (±)-pregabalin

Efficient utilization of a Mannich-type reaction and the ring-closing metathesis (RCM) approach that leads to a convenient synthesis of 3-(aminomethyl)-5-methylhexanoic acid (pregabalin) is described.Graphical abstract

Synthesis and biological evaluation of new thiosubstituted oxadiazole derivatives of coumarin under solvent-free conditionss

A series of new thiosubstituted 1,3,4-oxadiazole derivatives of coumarin were synthesised by reaction of 7-((5-mercapto-1,3,4-oxadiazol-2-yl)methoxy)-4-methyl-2H-chromen-2-one and α-haloketones by grinding, in solvent-free conditions at room temperature. The reaction was also carried out in ethanol in reflux conditions. Shorter reaction time and better yields were observed in solvent-free conditions. The structures of the compounds were characterised by IR, NMR, elemental analysis and mass spectral data. The synthesised compounds were evaluated for their in vitro antimicrobial screening on different strains of bacteria and fungi. Most of the compounds showed good to moderate activities.

A facile route for the synthesis of vinyl-substituted 1,3,4-oxadiazoles

An efficient synthesis of vinyl-substituted 1,3,4-oxadiazoles using o-nitrophenyl sulfoxide precursor via syn-elimination reaction using sodium acetate in THF is described. This method is cost effective as it uses cheap o-nitrothiophenol and can be used in the synthesis of vinyl intermediates during synthesis of bioactive compounds, which avoids the use of any toxic metals.