S N Murthy Boddapati - Academia.edu (original) (raw)

Papers by S N Murthy Boddapati

Eurasian Journal of Chemistry, Dec 29, 2023

American Journal of Health-System Pharmacy, 1982

The compatibility and stability of aminophylline-dextrose injection admixtures were investigated.... more The compatibility and stability of aminophylline-dextrose injection admixtures were investigated. Aliquots of 5% dextrose injection, 0.9% sodium chloride injection, and 5% dextrose and 0.9% sodium chloride injection were studied for these physiochemical properties: pH, color, clarity, absorbance in a spectrophotometer at 400 nm, and hydroxymethylfurfural (HMF) content. Aminophylline injection was added to the solutions, and aliquots were withdrawn after 0, 6, 24, and 48 hours of storage at 5, 25, 35, and 55 degrees C for testing of the physiochemical properties and aminophylline content. An aminophylline admixture in 5% dextrose injection was passed through an in-line filter (IVEX-2), and eluents were collected for aminophylline assay and for testing the above physiochemical properties. HMF and theophylline were assayed to high-pressure liquid chromatography (HPLC). The aminophylline concentration remained constant in all admixtures studied. A yellow color developed in dextrose-containing aminophylline admixtures stored at 25, 35, and 55 degrees C for 48, 24, and 6 hours, respectively. HMF concentration, pH, and clarity remained within compendial limits. The in-line filter did not retain active ingredients or alter the physiochemical properties of the admixture. Solutions that were yellow showed additional peaks on HPLC. HMF seemed to be a precursor for this yellow color, inasmuch as HMF concentration increased with increasing color intensity. It is concluded that aminophylline-dextrose admixtures are visually and chemically stable for 48 hours when stored under refrigeration or at room temperature.

Journal of Organometallic Chemistry, Jul 1, 2018

One pot highly efficient and simple protocol for the construction of aryl tetrazole amines via de... more One pot highly efficient and simple protocol for the construction of aryl tetrazole amines via desulphurization/substitution/electro cyclization/C-N cross coupling reactions from thiourea with the use of cheap, readily available and air stable copper source as catalyst has been described. The reaction proceeds through the in situ formation of amino tetrazole followed by successive C-N cross-coupling reaction with aryl iodide. Further the temperature dependent regioselectivity in N-arylation of tetrazole amines has been described.

Egyptian Journal of Chemistry, 2020

A SERIES of 16 new (±)-1-(4-(3-fluorobenzyloxy) pyrrolidin-3-yl)-4-phenyl-1H-1,2,3triazole deriva... more A SERIES of 16 new (±)-1-(4-(3-fluorobenzyloxy) pyrrolidin-3-yl)-4-phenyl-1H-1,2,3triazole derivatives were synthesized from 2,5-dihydro-1H-pyrrole. Sixteen compounds are well characterized by their 1 H NMR, 13 C NMR and mass spectral data. Anticancer activities of these compounds were tested against HCT 116, MDA-MB231, Mia-PaCa2 cancer cell lines. Among these series of compounds, 8b exhibited highest activity with IC 50 of 42.5 µg/ mL against MDA-MB231 cell line. The compound 8o and 8n showed moderate activity with IC 50 of 64.3 µg/ mL and 68.4 µg/ mL against HCT-116 and Mia-PaCa2 cancer cell lines respectively.

Journal of Heterocyclic Chemistry

Current Pharmaceutical Analysis

Background: Lenvatinib is a potent drug utilized in the medication of thyroid cancer and it acts ... more Background: Lenvatinib is a potent drug utilized in the medication of thyroid cancer and it acts as a tyrosine kinase inhibitor. Thus, the development and validation of Lenvatinib and allied impurities in rat plasma, and its pharmacokinetic study, are one of the most significant areas of modern pharmaceutical analysis. Objective: The current study conducts bioanalytical system validation and pharmacokinetic analysis of Lenvatinib and associated impurities in rat plasma with LC-MS/MS. Methods: The current study involves bioanalytical system validation and pharmacokinetic analysis of Lenvatinib and associated impurities in rat plasma using LC-MS/MS. Gradient elution of Lenvatinib with a flow rate of 1 mL/min and an X-Bridge phenyl column (150x4.6 mm, 3.5μ) was used in the optimized process. In this method, buffer (1 mL formic acid in 1 liter of water) and acetonitrile mixture was used as the mobile phase. Results: By using Carfilzomib as the internal norm and impurity-4 as the active ...

Turkish Journal of Chemistry

Introduction Heterocyclic compounds are a vital part of most of the bioactive molecules used as d... more Introduction Heterocyclic compounds are a vital part of most of the bioactive molecules used as drugs and are the key motifs for the novel drug discovery. The heterocyclic compounds enhance their activity when fused with other ring systems [1-2]. Oxadiazoles with plethora of biological applications are identified as important construction motifs for the advance of innovative drug design [3-5], thus grabbing the attention of medicinal chemists around the world. With its capability to bind with a ligand, the oxadiazole ring can be used as a significant part of the pharmacophore. In certain instances, it behaves like a flat aromatic linker that affords the proper orientation of the molecule [6]. In the oxadiazole family, 1,3,4-oxadiazoles occupied a unique position in medicinal chemistry due to their multipurpose utility in designing many bioactive compounds. In medicinal chemistry 1,3,4-oxadiazole and its derivatives are playing a vital role with broad range of biological applications. Oxadiazoles are the bioisostere of compounds with carbonyl function, like carboxylic acids, amides, and esters capable to form superior hydrogen bonding interactions with various receptors thereby augmenting the biological responses to a notable extent [7-8]. Recently, A.M. Rabie reported [9] two antioxidant polyphenolic 1,3,4-oxadiazole motifs, 2,3-tris[5-(3,4,5trihydroxyphenyl)-1,3,4-oxadiazol-2-yl]propan-2-ol (CoViTris2020) and 5-[5-(7-chloro-4-hydroxyquinolin-3-yl)-1,3,4oxadiazol-2-yl]benzene-1,2,3-triol (ChloViD2020) as the first multi-target SARS-CoV-2 inhibitors (Figure 1), with greater potency than the currently used medicine ivermectin, remdesivir, and favipiravir. The computational docking investigation of these two compounds displayed incredible high inhibitory binding affinities with most of the docked SARS-CoV-2/ human proteins. Interestingly, the results of the biological assay showed that CoViTris2020 and ChloViD2020 exhibited very high and extremely significant anti-COVID-19 activities (anti-SARS-CoV-2 EC 50 = 0.31 and 1.01 μM, respectively), representing that they can be very promising parent lead compounds for the design and construction of novel anti-COVID-19 agents. Moreover, 1,3,4-oxadiazoles have engrossed the attention of medicinal chemists as serotonin receptor (5-HT 3) antagonists [10], Human Neurokinin-1 (NK 1) antagonists [11], benzodiazepine receptor agonists [12], muscarinic agonists[13], 5-hydroxytryptamine (5-HT 1D) receptor agonists [14], antirhinoviral [15], tyrosinase inhibitory compounds[16]. Among the 1,3,4-oxadiazole family 1,3,4-oxadiazoles with substitutions at 2 nd and 5 th positions are an Abstract: Ten novel 2-aryl-5-(arylsulfonyl)-1,3,4-oxadiazoles were produced and assessed for their in vitro antibacterial and antioxidant activities. Diverse spectroscopic methods like 1 H NMR, 13 C NMR, IR, and LCMS were used for the characterization of the prepared samples and all the data was in good agreement with the anticipated structures. The prepared compounds 6a-j were screened for their in vitro antibacterial activity against bacterial strains Pseudomonas aeruginosa, Enterobacter aerogenes, Escherichia coli (grampositive), and Bacillus cerus, Staphylococcus aureus, Bacillus subtilis (gram-negative). The antimicrobial screening outcome revealed that the prepared 2-(3,4-dimethylphenyl)-5-tosyl-1,3,4-oxadiazole (6j), 2-(3-isopropylphenyl)-5-tosyl-1,3,4-oxadiazole (6c), and 2-(2-ethylphenyl)-5-tosyl-1,3,4-oxadiazole (6i) are most potent among all the examined compounds. Furthermore, the antioxidant activity of the prepared compounds was also investigated by DPPH radical scavenging method and the results showed that some of the compounds were moderately active.

Chemistry Africa

A series of novel N-(1-(3-fluoro-4-morpholinophenyl)-1H-tetrazol-5-yl) amides (8a–8l) were synthe... more A series of novel N-(1-(3-fluoro-4-morpholinophenyl)-1H-tetrazol-5-yl) amides (8a–8l) were synthesized and screened for their in vitro antibacterial properties against the medicinally relevant gram negative bacterial strains Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and gram positive bacterial strains Enterobacter aerogenes, Pseudomonas aeruginosa, Bacillus cerus. The compounds 8d, 8i, 8j, and 8l exhibited significant antibacterial activity. The compound 8d exhibited superior activity against Enterobacter aerogenes with an MIC value of 114 ± 0.48 µg/mL and compound 8l is most potent against Bacillus subtilis with an MIC of 75 ± 0.81 µg/mL. Moreover, in the present study, we have successfully screened the designed molecules as a DNA Gyrase enzyme inhibitors using in silico studies. The molecular docking simulation studies were performed using Molegro Virtual Docker (MVD) to identify the ligands responsible for antibacterial activity. The prepared compounds 8k, 8l, 8i and 8h gained good moldock scores of −156.622, −152.025, −148.189 and 146.362 respectively. The synthesized morpholine tetrazole hybrids offer a promising, friendly substitute and should be considered as a future goal for medicinal chemists working in the area of antibacterial research.

Journal of advanced scientific research, Apr 30, 2022

A series of 3-aryl indazoles 4a-4j were obtained by Pd catalyzed Suzuki coupling reaction. All th... more A series of 3-aryl indazoles 4a-4j were obtained by Pd catalyzed Suzuki coupling reaction. All the substrates were obtained in good yields under moderate reaction conditions. Next, the prepared compounds 4a-4j were screened for their antibacterial activity. The anti-bacterial activities of the prepared compounds were investigated against three bacterial strains i.e. Xanthomonas campestris, Escherichia coli, Bacillus megaterium. The anti-bacterial evaluation studies of these 3-aryl indazoles revealed that some of these test compounds possess moderate in vitro antibacterial activity.

Chirality

The direct separation of dipeptidyl peptidase IV (DPP‐4) inhibitors such as Sitagliptin (STG), Li... more The direct separation of dipeptidyl peptidase IV (DPP‐4) inhibitors such as Sitagliptin (STG), Linagliptin (LIG), and Saxagliptin (SAG) enantiomers in normal phase conditions have been achieved on immobilized polysaccharide‐based chiral stationary phases (CSPs), as well as on the macrocyclic glycopeptide vancomycin chiral stationary phase (Chirobiotic V2) under polar ionic mode. The enantiomers of these targets could be separated completely (resolution factor Rs > 2) using the Chirobiotic V2 column in polar ionic mode with the mobile phase (MeOH/AcOH/TEA 100/0.3/0.1 v/v/v) in an isocratic elution at 1.0 ml min−1. The effect of the mobile phase composition on separation, including buffer salts, acid–base modifiers, and analyte structures, was evaluated. The developed technique was validated in the polar ionic mode according to the International Conference on Harmonization (ICH) Q2R1 guidelines in terms of accuracy, precision, selectivity, linearity, limit of detection (LOD), and l...

Current Advances in Chemistry and Biochemistry Vol. 3, 2021

Caribbean Journal of Science and Technology, 2021

Studies on heterocyclic compounds are an evergreen branch of organic chemistry and attract the at... more Studies on heterocyclic compounds are an evergreen branch of organic chemistry and attract the attention of chemists working not only in the field of natural products but also in synthetic chemistry. Indazole and its derivatives are one of the most vital heterocycles in drug molecules. Diversely substituted indazole derivatives have gained considerable attention in the field of medicinal chemistry due to their versatile biological activities. This mini review aims to abridge the recent (2011-2021 till date) advances in various methods for the synthesis of indazole derivatives. Moreover, the current developments in the biological activities of indazole-based compounds are also presented.

Journal of Pharmaceutical Research International, 2021

Aims: The present application is a Newly Validated Reverse Phase-High Performance Liquid Chromato... more Aims: The present application is a Newly Validated Reverse Phase-High Performance Liquid Chromatography Method for the Assay of Dexmethylphenidate and Serdexmethylphenidate with PDA. Study design: Mentioned study is a quick, rapid, economical, precise, and accurate reverse phase- high performance liquid chromatographic method for estimating Dexmethylphenidate and Serdexmethylphenidate. Place and duration of study: The present assay was carried out at the Shree icon Pharma laboratories PVT.ltd, Vijayawada, AP, and India, from December 2020 to February 2021. Methodology: The stationary phase Agilent C18 column with dimensions of 150x4.6mm, 3.5 was used for chromatography and pH-2.5 ammonium acetate buffer with orthophosphoric acid: acetonitrile in a 50:50 ratio used as a buffer. The detection wavelength was 265nm, and the flow rate was 1mL/min. The strategy was justified according to ICH guidelines Results: Dexmethylphenidate and Serdexmethylphenidate had retention periods of 4.258 an...

New Ideas Concerning Science and Technology Vol. 11, 2021

Oriental journal of chemistry, 2021

The In vitro antimicrobial properties of a series of N-methyl-3-aryl indazoles (5a-5j) were scree... more The In vitro antimicrobial properties of a series of N-methyl-3-aryl indazoles (5a-5j) were screened. In this present work, we describe our efforts towards the development of potent antimicrobial activity of synthesized indazole derivatives. The antimicrobial activities of the prepared compounds were investigated against four bacterial strains: Xanthomonas campestris, Escherichia coli, Bacillus cereus, Bacillus megaterium, and a fungal strain Candida albicans. The biological evaluation studies of these indazole derivatives revealed that some of these tested compounds have shown moderate to good In vitro antimicrobial activities.

Future Journal of Pharmaceutical Sciences, 2021

Background Using a Symmetry C18 (4.6 × 150 mm, 3.5) column, a high-performance liquid chromatogra... more Background Using a Symmetry C18 (4.6 × 150 mm, 3.5) column, a high-performance liquid chromatographic method for quantification of Rilpivirine and Cabotegravir in active pharmaceutical ingredients was developed and validated. The mobile phase is made up of buffer, acetonitrile, and 0.1 percent formic acid in a 20:80v/v ratio. The flow rate was kept constant at 1.0 ml/min, and detection was accomplished through absorption at 231 nm with a photodiode array detector. Results The calibration curve was linear, with a regression coefficient (R2) value of 0.999 and concentrations ranging from 30 to 450 g/ml of Rilpivirine and 20–300 g/ml of Cabotegravir. The method's LOD and LOQ were 0.375 g/ml, 1.238 g/ml, and 0.25 g/ml, 0.825 g/ml for Rilpivirine and Cabotegravir, respectively. Conclusions In the forced degradation studies, the degradants were characterized by using LCMS and FTIR. The current application was found to be simple, economical, and suitable, and validated according to ICH...

New Journal of Chemistry, 2021

2-Halo arylcyanamides have been constructed from cyanamides via Pd(ii)-catalyzed selective ortho-... more 2-Halo arylcyanamides have been constructed from cyanamides via Pd(ii)-catalyzed selective ortho-halogenation under moderate reaction conditions.

Molecules, 2020

A facile, one-pot, and proficient method was developed for the production of various 2-arylaminob... more A facile, one-pot, and proficient method was developed for the production of various 2-arylaminobenzimidazoles. This methodology is based for the first time on a copper catalyst promoted domino C–N cross-coupling reaction for the generation of 2-arylaminobenzimidazoles. Mechanistic investigations revealed that the synthetic pathway involves a copper-based desulphurization/nucleophilic substitution and a subsequent domino intra and intermolecular C–N cross-coupling reactions. Some of the issues typically encountered during the synthesis of 2-arylaminobezimidazoles, including the use of expensive catalytic systems and the low reactivity of bromo precursors, were addressed using this newly developed copper-catalyzed method. The reaction procedure is simple, generally with excellent substrate tolerance, and provides good to high yields of the desired products.