A5036170497- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Tryptophan and brain disorders
- Click Chemistry and Applications
- Crystallography and molecular interactions
- Bipolar Disorder and Treatment
- Protein Kinase Regulation and GTPase Signaling
- Stress Responses and Cortisol
- Catalytic C–H Functionalization Methods
- Receptor Mechanisms and Signaling
- Synthesis and Characterization of Heterocyclic Compounds
- Molecular Sensors and Ion Detection
- Organoboron and organosilicon chemistry
- Boron Compounds in Chemistry
- Biochemical and Molecular Research
- HIV/AIDS drug development and treatment
- Chemical Synthesis and Analysis
- Plant biochemistry and biosynthesis
- Radioactive element chemistry and processing
- Axial and Atropisomeric Chirality Synthesis
- Biochemical Acid Research Studies
- Cyclopropane Reaction Mechanisms
- Monoclonal and Polyclonal Antibodies Research
- Luminescence and Fluorescent Materials
- Hydrogen Storage and Materials
University of Minnesota
2021-2025
Indian Institute of Technology Guwahati
2014-2019
Indian Institute of Technology Madras
2015
Assam University
2014
Uncontrolled metabolism of l-tryptophan (l-Trp) in the immune system has been recognized as a critical cellular process tolerance. Indoleamine 2,3-dioxygenase 1 (IDO1) enzyme plays an important role local l-Trp through kynurenine pathway systems. In this regard, IDO1 emerged therapeutic target for treatment diseases that are associated with suppression like chronic infections, cancer, and others. study, we synthesized series pyridopyrimidine, pyrazolopyranopyrimidine, dipyrazolopyran...
Synthetic anion transporters have been recognized as one of the potential therapeutic agents for treatment diseases including cystic fibrosis, myotonia, and epilepsy that originate due to malfunctioning natural Cl- ion transport systems. Recent studies showed synthetic can also disrupt cellular ion-homeostasis induce apoptosis in cancer cell lines, leading a revived attention transporters. Herein, we report development conformationally controlled 1,2-diphenylethylenediamine-based...
With N-tosylhydrazone as an ambiphilic reagent, unprecedented cyclization reaction of two identical or different tosylhydrazones has been developed to access various 4,5-disubstituted-2H-triazoles under transition metal, azide, and oxidant-free conditions. A mechanistic rationalization study led the identification several electronically diverse unsaturated systems for regioselective synthesis 1- 2-substituted 1,2,3-triazoles pyrazoles.
The antibacterial agent Bio-AMS is metabolized in vivo through hydrolysis of the central acyl-sulfamide linker leading to high clearance and release a moderately cytotoxic metabolite M1. Herein, we disclose analogues designed prevent metabolism moiety steric hindrance or attenuation electrophilicity. Bio-9 was identified as metabolically stable analogue with single-digit nanomolar dissociation constant for biotin protein ligase (BPL) minimum inhibitory concentrations (MICs) against...
The improvement of body's own immune system is considered one the safest approaches to fight against cancer and several other diseases. Excessive catabolism essential amino acid, L-tryptophan (L-Trp) assists cells escape normal obliteration. formation disproportionate kynurenine downstream metabolites suppress T cell functions. Blocking this immunosuppressive mechanism as a promising approach cancer, neurological disorders, autoimmunity, immune-mediated Overexpression indoleamine...
Abstract A high‐yielding synthetic route for the preparation of group 9 metallaboratrane complexes [Cp*MBH(L) 2 ], 1 and ( , M=Rh, M=Ir; L=C 7 H 4 NS ) has been developed using [{Cp*MCl } ] as precursor. This method also permitted synthesis an Rh–N,S‐heterocyclic carbene complex, [(Cp*Rh)(L )(1‐benzothiazol‐2‐ylidene)] 3 ; in good yield. The reaction compound with neutral borane reagents led to isolation a novel borataallyl complex [Cp*Rh(L) B{CH C(CO Me)}] ). Compound features rare η...
We describe a novel class of amphiphiles with squaramide moiety as phosphate bioisostere. Most synthesized squaramide-based have the favorable physicochemical properties lipids, such as: formation stable liposomes or giant unilamellar vesicles in aqueous solution, high phase-transition temperature, low vesicle leakage and phospholipase resistance properties.
An unusual transformation of indoles to pyrazoles via an aromatic ring-opening strategy has been developed. The salient feature this involves the C2–N1 bond opening and concomitant cyclization reaction C2═C3 indole moiety with tosylhydrazone, which proceeds under transition-metal ligand free conditions. This functionalization provides a wide scope differently substituted pyrazoles.
The first example of a homometallic neutral zirconaborane, [(Cp2Zr)2B5H11], 1, has been prepared through the thermolysis [Cp2Zr(BH4)2], generated from fast metathesis reaction [Cp2ZrCl2] and LiBH4·thf with BH3·thf. solid-state structure 1 shows an open geometry planar B3 ring. bonding between Zr center central ring was studied computationally by DFT methods, based on combined experimental computational results compound can be defined as metal-stabilized arachno-B3H9. Further, in attempt to...
Indoleamine 2,3-dioxygenase 1 (IDO1) is considered as an important therapeutic target for the treatment of cancer, chronic infections and other diseases that are associated with immune suppression. Recent developments in understanding catalytic mechanism IDO1 enzyme revealed conversion l-tryptophan (l-Trp) to N-formylkynurenine proceeded through epoxide intermediate state. Accordingly, we synthesized a series 3-substituted oxindoles from l-Trp, tryptamine isatin. Compounds C3-substituted...
Protein kinase C (PKC)-C1 domain targeted regulator development is considered as a potential therapeutic strategy for the treatment of cancer and immunological other diseases. Efforts are underway to synthesize small molecules achieve higher specificity C1-domain than natural activator, diacylglycerols (DAGs). In this regard, we conveniently synthesized 4-hydroxy-3-(hydroxymethyl) phenyl ester analogues measured in vitro binding properties. We also investigated different physicochemical...
Abstract Membrane forming synthetic lipids constitutes a new class of biomaterials with impressive applications in the field biological and pharmaceutical sciences. Interestingly, alteration(s) headgroup region offer wide chemical space to investigate their specific properties. In this regard, we have utilized β‐azidophosphonate chemistry gain access novel triazole‐phosphonate (TP) amphiphiles fascinating physicochemical properties lipids. TP form stable vesicles that exhibit negative...
Modified C-nucleosides have proven to be enormously successful as chemical probes understand fundamental biological processes and small-molecule drugs for cancer infectious diseases. Historically, the modification of glycosyl unit has focused on 2′-, 3′-, 4′-positions well ribofuranosyl ring oxygen. By contrast, 1′-position rarely been studied due labile nature anomeric position. However, improved stability allows with substituents not found in conventional N-nucleosides. Herein, we disclose...
Protein kinase C-C1 domain binding specificity of the anionic hybrid lipids.
While biochemical, structural, and computational studies have shown the importance of remdesivir's C1′-substituent in its perturbation SARS-CoV-2 RdRp action, we recognized paucity methods to stereoselectively install substituents at this position as an obstacle rigorous explorations SAR mechanism. We report utilization anomerically pure 1′-cyano intermediate entry point a chemically diverse set substitutions, allowing for 1′diversification while obviating need tedious separation anomeric mixtures.
The synthesis of 1′-azido C-nucleosides is described to expand the set azide-functionalized nucleosides for bioorthogonal applications and as potential antiviral drugs. Lewis acid-promoted azidation a nucleoside hemiketal resulted in formation tetrazole through Schmidt reaction manifold. Conformational control prevent ring–chain tautomerism enabled efficient 1′-azidation with complete β-diastereoselectivity. unique reactivity further derivation are also reported.
Investigation of γ-hydroxymethyl-γ-butyrolactone substituents as protein kinase C ligands, in an effort to develop small molecule-based regulators with higher specificity for C1 domain than the endogenous ligand, diacylglycerols.
Abstract An intermolecular reaction with the optimized conditions is also presented to yield corresponding hydrazone derivative (VII).