Rajesh R

Department of Communication Engineering

School of Electronics Engineering

Vellore Campus

Manikandan A

Ramasubbu C

Nagaraju N.

Vellore Institute of Technology (VIT) is a private university located in&nbsp;Tamil Nadu, India. Founded in 1984, as Vellore Engineering College, the institution offers 20 undergraduate, 34 postgraduate, four integrated and four research programs. It has campuses in Vellore, Amravati, Bhopal and Chennai.

VIT is one of the top ranked private universities in India according to NIRF, THE and QS Rankings.&nbsp;Govt. of India has recognized&nbsp;VIT, Vellore as an&nbsp;Institution of Eminence. This has allowed VIT to take independent quality initiatives and move up in world ranking.

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VIT University

European Journal of Medicinal Chemistry

Molecular adaptation of small molecules that are targeted as therapeutic agents is a most anticipated one in drug designing and development. In the present approach, a family of substituted 1H-benzo[d]imidazol-2-amine derivatives (5a-d and 6a-e) were effectively synthesised and testified for their molecular adaptations in order to develop them as novel medications against oxidation, inflammation and inflammation associated cancer types by means of in silico and in vitro assessments. Chronic inflammation, regardless of infectious agents, plays a vital role in various cancer development. Moreover, hypoxia-inflammation-cancer are highly associated together. Hydrogen peroxide free-radical scavenging, HRBC membrane stabilization assay and cell viability test by MTT assay (macrophage) were executed to establish antioxidant, anti-inflammatory and anticancer properties of these compounds. As the prostaglandin-endoperoxide synthase 2 is highly involved in inflammation and cancer development respectively, molecular docking was executed on the corresponding X-ray crystallographic models (PDB structures).

Fulltext

Asian Journal of Chemistry

Synthesis and Molecular Drug Validations of 1H-Benzo[d]imidazol-2-amineDerivatives: Molecular Docking and its Biological Activities

2-(4-phenylquinoline-2-yl)phenol derivatives (4a-l) with COX-2 enzyme inhibition, analgesic, anti-inflammatory and antipyretic potentials were executed and reported. From the in vitro COX-2 enzyme inhibition assay, compounds 4 h (IC 50 0.026 µM) and 4j (IC 50 0.102 µM) were found as most potent COX-2 inhibitors. Consequently, to get more insight into the binding mode with COX-2, compounds 4a-l were docked into the COX-2 (PDB ID: 1CX2) active site. In the Human Red Blood Cells (HRBC) membrane stabilization assay (in vitro anti-inflammatory), compounds 4f (IC 50 0.064 µM) substituted with –OH (R 1 ) and –3Cl (R 2 ), 4 h (IC 50 0.021 µM), 4i (IC 50 0.484 µg/ml) and 4j (IC 50 0.092 µM) with –CHO containing alkanol and ether group at R1 and –4F, –4Br and –OMe at R2 (C2) were showed most potent anti-inflammatory activity. Eventually, acute toxicity studies revealed that 2-(4-phenylquinoline-2-yl)phenol derivatives (4a-l) are safe up to a toleration dose limit of 100 µg/kg body weight. In the Backer’s yeast intraperitoneal injection test, compounds 4f, 4 h and 4j produced significant (p &lt; 0.05) antipyretic activity at 1, 1.5, 2 and 2.5 h, whereas test compound 4j and the reference drug indomethacin showed significant antipyretic activity throughout the observation period up to 2.5 h. Promising in vivo results obtained were correlated with the standard non-steroidal anti-inflammatory drugs and the compounds 4f, 4 h, 4i, 4j, and 4 l were efficiently identified as therapeutically potent/fortune moieties as non-steroidal anti-inflammatory agents/analgesics. At the end, ulcerogenic study result ensured that the tested 2-(4-phenylquinoline-2-yl)phenol derivatives created no side-effect. © 2017, Springer International Publishing.

Inflammopharmacology

Efficacy of phenyl quinoline phenol derivatives as COX-2 inhibitors; an approach to emergent the small molecules as the anti-inflammatory and analgesic therapeutics

Cancer Chemotherapy and Pharmacology

Molecular explorations of substituted 2-(4-phenylquinolin-2-yl) phenols as phosphoinositide 3-kinase inhibitors and anticancer agents

(E)-N′-(Substituted-benzylidene)-2-(7-fluoro-2-methoxyquinolin-8-yl)acetohydrazide-hydrazone derivatives9a–nrepresent a new series of antibacterial agents and DNA gyrase inhibitors.

RSC Advances

Synthesis of quinoline acetohydrazide-hydrazone derivatives evaluated as DNA gyrase inhibitors and potent antimicrobial agents

American Chemical Society (ACS)

Highly Viscous Binary Solvents: DMSO-d6/Glycerol and DMSO-d6/Glycerol-d8 for Polar and Apolar Mixture Analysis by NMR

Bioorganic & Medicinal Chemistry

Corrigendum to “Antiplasmodial phloroglucinol derivatives from Syncarpia glomulifera” [Bioorg. Med. Chem. 24 (2016) 2544–2548]

Substituted methoxybenzyl-sulfonyl- 1H -benzo[d]imidazoles evaluated as effective H + /K + -ATPase inhibitors and anti-ulcer therapeutics

Journal	Data powered by TypesetEuropean Journal of Medicinal Chemistry
Publisher	Data powered by TypesetElsevier BV
ISSN	0223-5234
Open Access	0