Suneel Dodamani

Design, synthesis and pharmacological analysis of 5-[4′-(substituted-methyl)[1,1′-biphenyl]-2-yl]-1H-tetrazoles

In the present paper 5-[4′-({4-[(4-aryloxy)methyl]-1H-1,2,3-triazol-1-yl}methyl)[1,1′-biphenyl]-2-yl]-1H-tetrazoles (5a–g) and [2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl-substituted-1-carbodithioates (11h–q) have been designed and synthesized. These compounds were subjected to docking (against AT1 receptor protein enzyme in complex with Lisinopril), in vitro angiotensin converting enzyme inhibition, anti-proliferative, anti-inflammatory screening (through egg albumin denaturation inhibition and red blood cell membrane stabilization assay) and finally anti-fungal activity analyses. Some of the compounds have shown significant pharmacological properties.

Formulation of thermoreversible gel of cranberry juice concentrate: Evaluation, biocompatibility studies and its antimicrobial activity against periodontal pathogens

The present work aims to investigate the efficacy of thermoreversible gel of cranberry juice concentrate (CJC) as local drug delivery for the treatment of periodontitis. CJC was initially tested for its antimicrobial activities like MIC, MBC, antiadhesion, antibiofilm and time kill assay against the panel of organisms (S. mutans (SM), E. faecalis (EF), A. actinomycetemcomitans (AA), P. gingivalis (PG), T. forsythia (TF)) responsible for periapical and periodontal infections. Antimicrobial activity of CJC showed MIC value of 50mg/ml and MBC value of 100mg/ml with desirable antiadhesion (83-90%) and antibiofilm activity (70-85%). CJC was evaluated for its biocompatibility using periodontal fibroblasts by cell based MTT assay and found to be nontoxic. Influence of CJC on periodontopathogen PG derived virulence factors (fimA and kgp) was studied using real time polymerase chain reaction (RT-PCR) technique wherein down regulation of selected genes demonstrated inhibitory effect against PG virulence factors. Thermoreversible gel of CJC was formulated by cold method using poloxamer 407 as thermosensitive polymer and carbopol 934 as mucoadhesive polymer and evaluated for its gelation temperature, viscosity, gel strength and mucoadhesive strength. Comparison of optimized thermoreversible gel of CJC (500mg/ml) with commercially available chlorhexidine gluconate gel (0.2%) using agar well diffusion demonstrated equal zone of inhibition against SM, EF, AA, PG & TF. Hence the formulated thermoreversible gel of CJC could serve as a novel herbal alternative to currently available periodontal treatment modalities.

Transition metal complexes of a hydrazone derived from hydralazine hydrochloride and 3,5-di-tert-butylsalicylaldehyde

Mononuclear Co(III), Ni(II) and Cu(II) coordination compounds of (E)-1-(3,5-di-tert-butyl-2-hydroxybenzylidene)-2-(phthalazin-1-yl)hydrazine (LH) were prepared and characterized by physicochemical and spectroscopic methods. The metal-to-ligand ratio was found to be 1:2 in [Co(L)2]Cl·2H2O (1) and [Ni(L)2]·2H2O (2), while it is 1:1 in [Cu(L)Cl]·2CH3OH (3). The X-ray crystal structures of LH and complex 1 is are reported. LH shows monobasic behavior, coordinating through NNO donor atoms. The complexes were investigated for their antimicrobial properties. Complexes 1 and 3 show excellent antibacterial and antifungal activities, respectively.

Design and synthesis of coumarin–imidazole hybrid and phenyl-imidazoloacrylates as potent antimicrobial and antiinflammatory agents

An improved one pot, multi-component synthesis of tri- and tetrasubstituted coumarin–imidazole hybrid has been synthesized at C4 position in good to excellent yield. The reaction was performed under various catalysts and optimization condition results obtained are satisfactory. Wherein, trisubstituted coumarin–imidazole hybrid compounds were converted into phenyl-imidazole acrylates. Further, all the newly synthesized compounds were screened for their antimicrobial activity against Gram-positive Bacillus flexus and Gram-negative Pseudomonas spp. bacterial strains and two strains of fungi studies having Scopulariopsis spp. and Aspergillus terreus organisms. Similarly, antiinflammatory activity of all the compounds was screened against MMP-2 and MMP-9. Both antimicrobial and antiinflammatory results are excellent, among all compounds, sodium acrylate compounds are quite promising against microbial strains and matrix metalloproteins (MMPs). All the isolated compounds were characterized by IR, NMR, and mass spectral analysis.Graphical abstract