Papers by Anireddy Jayashree
Journal of chemical and pharmaceutical research, 2013
Synthesis of new compounds possessing 7-membered rings with two heteroatom a 1,4-diazepines havin... more Synthesis of new compounds possessing 7-membered rings with two heteroatom a 1,4-diazepines having fused heterocyclic ring of coumarin and thiophene and cyclic secondary amine as a side chain. Substituted 8-amino-10methyl chromeno [3, 4-b] thieno [2, 3-e] [1, 4] diazepin-6(12H)-one hydrochlorides treated with cyclic secondary amine (N-methyl, N-ethyl, N-phenyl and N-benzylpiperazine) in potassium carbonate and toluene at reflux condition.
[BMIM][OH]-Mediated One-Pot Synthesis of 2-Amino-5-oxo-4-(1H-pyrazol-5-yl)-5H-chromeno[4,3-b]pyridine-3-carbonitriles as Potential Anticancer Agents
Russian Journal of General Chemistry, 2023
Synthesis and Characterization of Substituted-(1H-benzo[d]imidazol-2-yl) amino-pyrimidine Derivatives
International research journal of pharmacy, Mar 28, 2014
Novel molecules containing structural features of NSAIDs and 1,2,3-triazole ring: Design, synthesis and evaluation as potential cytotoxic agents
Journal of Molecular Structure, Dec 1, 2021
Abstract For the first time the template containing structural features of more than one NSAIDs a... more Abstract For the first time the template containing structural features of more than one NSAIDs and the 1,2,3-triazole ring was explored for the identification of potential cytotoxic agents. These new and complex molecules were predicted to be effective inhibitors of PDE4B by molecular modelling studies in silico. The multi-step synthesis of these compounds were carried out starting from the well-known drug nimesulide and involved the use of copper-catalyzed azide-alkyne cycloaddition (CuAAC) approach as the key step. Mainly two types of compounds e.g. 1-aryl-1H-1,2,3-triazoles and N-aryl-2-(1H-1,2,3-triazol-1-yl)acetamide derivatives were synthesized by using this method in good yields. The in vitro screening of these compounds against two cancer cell lines e.g. HCT-15 (human colon cancer cell line) and NCI-H226 (human lung cancer cell line) using a colorimetric MTT assay allowed identification of two preliminary hit molecules i.e. 8a and 8f. The SAR (Structure Activity Relationship) analysis indicated that the presence of an amide linker between the aryl ring and the 1,2,3-triazole moiety was favorable for the activities. The compound 8a and 8f showed significant inhibition of PDE4B in vitro and good interactions with this protein in silico suggesting PDE4B as their potential target. The usefulness and concerns of these molecules in the light of computational ADME prediction were analyzed. Overall, novel molecules were identified as potential cytotoxic agents for further study.
Oriental journal of chemistry, Jun 25, 2017
A stability indicating QbD based gradient method was developed and validated with the concept of ... more A stability indicating QbD based gradient method was developed and validated with the concept of quality by design (QbD) and with help of design of experiments (DoE) tool for the simultaneous determination of related organic impurities of Ibuprofen and Paracetamol in a combination solid oral dosage form by reverse phase high performance liquid chromatography (RP-HPLC). The most important critical quality attributes (CQA) of the developed test method were chosen and were evaluated by using "Design-Expert® 8" software tool with a quadratic mode of central composite design (CCD). The separation between all known impurities was achieved using "X-Terra RP18, 250-mm × 4.6-mm, 5-µm column with a 1.0 mL/min flow rate of gradient elution. The UV detection wavelength was used as 220 nm. The method validation is carried out as per ICH guidance, and the parameters include precision, accuracy, specificity, linearity, detection limit (DL), quantitation limit (QL), and robustness.
Heterocyclic Communications, Nov 26, 2016
A series of novel chroman-4-one fused benzofurans were synthesized by cyclization of the correspo... more A series of novel chroman-4-one fused benzofurans were synthesized by cyclization of the corresponding chalcones under microwave irradiation. All new compounds were characterized by IR, 1 H NMR, 13 C NMR and mass spectral data and were evaluated for their in vitro antimicrobial and antioxidant activities.
Cross-dehydrogenative C(sp<sup>3</sup>)–C(sp<sup>3</sup>) coupling <i>via</i> C–H activation using magnetically retrievable ruthenium-based photoredox nanocatalyst under aerobic conditions
Chemical Communications, 2019
A robust, magnetically retrievable photoredox Ru-based heterogeneous nanocatalyst was fabricated ... more A robust, magnetically retrievable photoredox Ru-based heterogeneous nanocatalyst was fabricated for the highly regio-selective synthesis of N-aryl-tetrahydroisoquinoline derivatives.
American Journal of Analytical Chemistry, 2021
A simple, rapid, and highly sensitive LC-MS/MS method has been developed for the simultaneous and... more A simple, rapid, and highly sensitive LC-MS/MS method has been developed for the simultaneous and trace level quantification of underivatized boronic acids in lumacaftor active pharmaceutical ingredient. Chromatographic separation of boronic acids and lumacaftor achieved using Agilent Poroshell HPH C18 150 × 4.6 mm 2.7 µ column with 0.1% ammonia in water as mobile phase A and 100% acetonitrile as mobile phase B at a flow rate of 0.25 ml/min. Gradient elution was used with a total method run time of 14 minutes. Boronic acids were successfully ionized and quantified without derivatization using electrospray ionization in negative mode using tandem quadrupole mass spectrometry in multiple reactions monitoring mode. Method validation was performed as per ICH guidelines with good linearity over the concentration range of 0.05 ppm to 5 ppm of Lumacaftor test concentration for both the boronic acids with a correlation coefficient of >0.99. Recoveries were found good at different concentration levels and within the range of 80%-120%. The developed method can be successfully used for the routine quantification of boronic acids at a concentration level of 20 ng/ml (1 ppm with respect to 20 mg/ml lumacaftor).
ONE-POT SYNTHESIS PF NOVEL 10-ARYL[1,2,4]TRIAZOLO[3′,4′:2,3][1,3,4]-THIADIAZEPINO[6,7-c]QUINOLIN-6(5H)-ONES
Organic preparations and procedures international, Dec 1, 1993
Synthesis of 5<i>H</i>-Quinolin[3,4-<i>b</i>][1,4]benzothiazin-6(12H)-ones
Synthetic Communications, Apr 1, 1990
ABSTRACT
Optimization of process parameters for conventional pyrolysis of algal biomass into bio–oil and bio–char production
Chemical Engineering and Processing, Mar 1, 2023
Russian Journal of General Chemistry, Apr 1, 2019
In a SAR study, we have synthesized a few 1H-pyrazole carboxylate related microbicides using Vils... more In a SAR study, we have synthesized a few 1H-pyrazole carboxylate related microbicides using Vilsmeier reagent. The anti-microbial screening results of 1H-pyrazole-3-carboxylate are reported here for the first time. The effect of 1H-pyrazole carboxylates on the mycelial growth of plant pathogenic fungi is revealed. The first X-ray structure in the family of microbicidal 1H-pyrazole-4-carboxylates is presented.
Journal of Chemical Sciences, Feb 12, 2016
An efficient method for the preparation of 8-substituted odoratine [(3-(3 ′ ,4 ′-methylenedioxyph... more An efficient method for the preparation of 8-substituted odoratine [(3-(3 ′ ,4 ′-methylenedioxyphenyl)-5,6,7-trimethoxyisoflavone] derivatives, structurally similar to glaziovianin A, a known cytotoxic substance, has been described. The key steps in the synthesis are site selective bromination reaction followed by Suzuki coupling reaction in very good yield. The structural assignment of the bromo derivative was determined utilizing 2D-HMBC and NOEs NMR techniques.
Design, Synthesis and Antibacterial Evaluation of Compounds Based on New Benzoxepine-oxime-1,2,3-triazole Hybrid
Mini-reviews in Medicinal Chemistry, Apr 30, 2018
A library of small molecules based on the new benzoxepine-oxime-1,2,3-triazole hybrid was initial... more A library of small molecules based on the new benzoxepine-oxime-1,2,3-triazole hybrid was initially designed as potential antibacterial agents. These compounds were synthesized using a Cu-catalyzed azide-alkyne cycloaddition (CuAAC) as a key step to construct the desired 1,2,3-triazole ring. Thus the click reaction between the appropriate alkyne containing the benzoxepine-oxime framework with aryl azides afforded the target compounds in good yields. To assess their antibacterial properties all the synthesized compounds were tested against four strains of bacterial microorganisms including one Gram-positive and three Gram-negative species. These compounds were generally found to be effective towards gram -ve species and one of them showed selective cytotoxicity against lung cancer cell line.
Synthesis, Biological Evaluation, and Lipinski Analysis of New Hybrids Containning 1,2,3-Triazoles and Dihydropyrimidinone Scaffolds
Russian Journal of General Chemistry
Synthesis of novel 2,4,6-trisubstituted pyrimidine derivatives and their in vitro antimicrobial activity
Russian Journal of General Chemistry, 2016
A series of novel pyrimidines (6a–6i) has been synthesized from corresponding chalcones and isoni... more A series of novel pyrimidines (6a–6i) has been synthesized from corresponding chalcones and isonicotinimidamide.HCl in the presence of potassium carbonate involving Michael addition followed by cycloaddition. All newly synthesised chalcones and pyrimidines were screened for in vitro antimicrobial activity against various Gram positive, Gram negative bacterial and fungal strains. Most of compounds displayed high antimicrobial activity compared to standard drugs Penicillin, Streptomycin and Ampothericin-B.
Asian Journal of Chemistry, 2015
INTRODUCTION 2-Butyl-5-chloro-1H-imidazole-4-carbaldehyde (1) and its chemistry is considered to ... more INTRODUCTION 2-Butyl-5-chloro-1H-imidazole-4-carbaldehyde (1) and its chemistry is considered to be an important class of Nheterocyclic compounds with various active sites serving as synthons for the synthesis of several new compounds with useful biological properties. Weinstock et al. 1 reported the use of 1 and its derivatives to exhibit potent and selective angiotension II receptor antagonists, Kantevari et al. 2 reported that, N-alkyl chalcone derivatives can be used as angiotension converting enzyme (ACE) inhibitors, Salimbeni et al. 3 reported the N-alkyl derivatives can act as nonpeptide angiotension II receptor antagonists and several reports reveal the use of 1 with various biological activities 4-7. Although there are numerous reports on N-alkylations of various compounds using various solvents but most of them suffer due to hazardous use of solvents, harsh reaction conditions, use of external phase transfer catalysts and longer reaction times. Hence, there is a need for the development of new techniques which are environmentally benign in nature. Use of polyethylene glycol as solvent has attracted the attention of many researchers in the present context of green synthesis. PEG has been considered as green and efficient solvent for carrying various organic reactions. In present work, choose of PEG-600 as solvent provoked by being thermally labile, availability, inexpensive, easy workup and recyclability. PEG-600 has unique solvent property which has excellent cataionic coordination capability which render it a perfect proton abstracter facilitating N-alkylations. Conventional N-alkylations mostly requires base like K2CO3 which neutralize the acid liberated from the reaction PEG-600 Mediated Phase Transfer Catalyst Free N-Alkylations of 2-Butyl-5-chloro-1H-imidazole-4-carbaldehyde
An efficient and novel method for the preparation of N-aryl-quinolone via enaminone synthesis has... more An efficient and novel method for the preparation of N-aryl-quinolone via enaminone synthesis has been described. Subsequent derivatization at 3 position has been accomplished by the palladium catalyzed Suzuki cross coupling reaction. Using this method, various aryl boronic acids as well as hetero aryl boronic acids have been coupled with 3-bromoquinolone to generate the novel 1,3-di-aryl-quinolone derivatives. The key step quinolone ring formation has been achieved by intramolecular displacement reaction of enaminone 2 with suitably substituted ortho-fluoro group in the aromatic ring.
Journal of Amino Acids, Nov 19, 2014
A new series of isoxazole tethered quinone-amino acid hybrids has been designed and synthesized i... more A new series of isoxazole tethered quinone-amino acid hybrids has been designed and synthesized involving 1,3-dipolar cycloaddition reaction followed by an oxidation reaction using cerium ammonium nitrate (CAN). Using this method, for the first time various isoxazole tethered quinone-phenyl alanine and quinone-alanine hybrids were synthesized from simple commercially available 4-bromobenzyl bromide, propargyl bromide, and 2,5-dimethoxybenzaldehyde in good yield.
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Papers by Anireddy Jayashree