Nageswara Rao Golakoti

• Professor
• Sri Sathya Sai Institute of Higher Learning

3,19‐Furfurylidene‐12(S)‐thiophenyl‐14‐deoxy‐andrographolide (12‐Ph‐S‐Fur‐ADG) was synthesized and characterized using the FT‐IR, ¹H NMR, and ¹³C NMR, DEPT‐45, DEPT‐90, DEPT‐135, and 2D‐NMR (HOMO‐COSY and HSQC) and HRMS spectroscopy. A single product was obtained when sodium bicarbonate was used as a base in the reaction. The configuration at the C...

In our efforts to design mono‐carbonyl analogues of curcumin with potential antiplasmodial activity, diarylidenecyclopentanone (DACP) derivatives, Ia–Iu and II–V, have been synthesized and characterized using ¹H NMR, ¹³C NMR, IR, UV–Vis, and mass spectrometry. Structure of one of these DACPs has been verified by single crystal XRD. At the outset, a...

Arjunolic acid (AA) is a pentacyclic triterpene acid with various potent biological activities. In this work, arjunolic acid was isolated from the heartwood of Terminalia arjuna, and a series of novel arjunolic acid acetals were synthesized and characterized. The anti-cancer activity of the synthesized acetals was investigated against sixty cell li...

Arjunolic acid (AA) is a pentacyclic triterpene acid with various potent biological activities. In this work, arjunolic acid was isolated from the heartwood of Terminalia arjuna, and a series of...

Globally, cancer is the most prevalent chronic disease-related cause of death. Although there are many anticancer drugs, some of them have adverse effects. Due to their limited side effects, natural products are preferred over synthetic drugs. Andrographolide and its derivatives are known to be potent anticancer agents. In this context, sixteen nov...

A total of 10 benzopyrylium salts, 7 being novel, were synthesized by Claisen‐Schmidt condensation reaction and characterized by ¹H and ¹³C NMR, High‐Resolution Mass Spectrometry, FT‐IR, and UV‐Vis spectroscopy. The purity of these synthesized compounds was determined by HPLC. The in‐vitro anti‐cancer evaluation of these synthesized benzopyrylium s...

Eighteen isoandrographolide analogues were synthesized, characterized and tested for their anticancer activity against 60 cancer cell lines at NCI. Three of the synthesized acetals ((3,19)‐3‐Nitro‐benzylidene‐isoandrographolide (3 p), (3,19)‐4‐Nitrobenzylidene‐isoandrographolide (3 q) and (3,19)‐4‐Isopropyl‐benzylidene‐isoandrographolide (3 r)) are...

Curcumin has anti‐oxidant properties resulting from its radical scavenging ability and inhibition of inflammation‐associated factors. However, its lack of solubility, instability, and poor bioavailability are impediments to its therapeutic use. As potential alternatives, we synthesized and performed chemical analysis of thirty diarylidene‐N‐methyl‐...

With the objective of establishing the effect of cycloalkanone ring size on the NLO properties of bischalcones para-substituted diarylideneacetone and substituted diarylidenecycloalkanone derivatives were synthesized by the Claisen–Schmidt condensation reaction and characterized by using UV–Vis, FT-IR, 1 H NMR, 13C NMR and mass spectrometry. The...

Natural product, Andrographolide.is diterpene lactone extracted from Andrographis paniculata. In traditional form of medicine, it is being used in India, China and Malaysia for treating various diseases. While in the last two decades there are many reports on andrographolides and its derivatives with various biological activities such as anti-cance...

There is a significant need for new small molecule anti-inflammatory compounds. Curcumin, a small molecule natural product from the Turmeric (Curcuma longa) plant, has well-known anti-oxidant properties, resulting from its radical scavenging ability and inhibition of inflammation-associated factors. However, its lack of solubility, instability, and...

A series of 22 different 3,5‐diarylidenetetrahydro‐2H‐pyran‐4(3H)‐ones (DATPs) were synthesized, characterized, and screened for their in vitro antiplasmodial activities against chloroquine (CQ)‐sensitive Pf3D7, CQ‐resistant PfINDO, and artemisinin‐resistant PfMRA‐1240 strains of Plasmodium falciparum. DATP 19 (3,5‐bis(4‐hydroxy‐3,5‐dimethoxybenzyl...

A total of eight novel spirobibenzopyrans were synthesized by Claisen-Schmidt condensation reaction and have been characterized by 1H NMR, 13C NMR, FT-IR, UV-Vis spectroscopy, and High-Resolution Mass Spectrometry. The purity of these synthesized compounds was determined by HPLC. The in vitro anti-cancer screening of these synthesized spirobibenzop...

Acetals (2a-d, 3a-d, and 6a-d) of andrographolide (1), 14-deoxy-12-hydroxyandrographolide (4), and isoandrographolide (5) were synthesized using benzaldehyde and heteroaromatic aldehydes. All the synthesized derivatives were characterized using 1H-NMR, 13C-NMR, mass spectrometry, UV, and IR. The compound 6d was characterized via a single-crystal X-...

Unexpected spiro cyclic products were obtained from the popular alkali catalyzed Claisen-Schmidt reaction of ketones with salicylaldehyde apart from the bis-chalcones. However, in the acid catalyzed reaction, we observe their transformation to a benzopyrylium salt. In the present study, we demonstrate this phenomenon for three ketones namely cyclop...

Development of tunable photonic devices having molecular dimensions is an active research area in nonlinear optics which continues to evolve and impact many technologies. Here, we demonstrate the tailoring of nonlinear optical properties of nitrochalcone derivatives by engineering the donor-acceptor configurations on either end of the molecules, to...

Benzopyrylium salts are an unexplored class of compounds and as a first, this study reports them as potential therapeutic agents. In this effort we pursue the synthesis and in vitro anticancer, antibacterial and antioxidant properties of some novel benzopyrylium salts. The benzopyrylium salts were synthesized and further characterized via UV-vis, I...

Fifteen chalcone derivatives having D–A–D, D–A–A and A–A–D architectures have been synthesized by Claisen–Schmidt condensation reaction and characterized by UV–Vis, IR, 1H-NMR, 13C-NMR and Mass spectrometry. In order to unambiguously establish the structure–activity relationship for the non-linear optical activity of these compounds, for the first...

Twenty-five ( Ia-Iu , IIa-IIb , IIIa , and IVa ) diarylidene-N-methyl-4-piperidones (DANMPs) were synthesized and characterized via UV, FT-IR, NMR and MS while Id was characterized also by single-crystal XRD. Twenty-one compounds were shortlisted...

Cancer is often associated with chronic inflammation. In order to develop potential anticancer and anti-inflammatory agents a series of 26 diarylidenecyclopentanones (DACPs) Ia–Iv, II, III, and IV were synthesized. Five of the synthesized DACPs are novel (Ih, Ij, Ik, Is, and Iv), derivative Iv was characterized using single-crystal X-ray diffractio...

From times immemorial, natural products have played an important role in the management of human health. Andrographis paniculata, belonging to the family Acanthaceae and its constituents are reported to possess a wide range of biological properties such as anti-cancer, anti-diabetic, anti-inflammatory, anti-bacterial, anti-malarial, anti-hepatitis,...

Inflammation is a pathophysiological condition which progresses through the prostaglandin (PG) and leukotriene (LT) pathways channelized by the enzymes, COX/mPGES1 and 5-LOX respectively. Diarylidenecyclohexanone (DAC) derivatives (Ia-j, IIa-c, IIIa and IVa) were synthesized, characterized and screened for their in vitro anti-inflammatory activity...

Andrographolide (1), the major labdane diterpenoidal constituent of Andrographis paniculata Wall, has been found to be majorly responsible for the medicinal uses of the plant particularly anti-cancer properties. In our previous work, we have found 3,19-diacetyl-12-phenylthio-14-deoxy-andrographolide (3g), a semi-synthetic derivative of Andrographol...

This study is the first report on the anticancer activity of spirobibenzopyrans, an unexplored class of therapeutic agents. The synthesized spirobibenzopyrans were tested for anticancer activity across the NCI-60 cell-line panel. The in vitro and in silico results of the spirobibenzopyrans showed tremendous drug likeness score as potential anticanc...

The present invention relates to novel spirobibenzopyran conjugate derivatives with potent anti- cancer activity as pharmaceutical agents, their stereoisomers, their polymorphs and their pharmaceutically acceptable salts and their pharmaceutically acceptable solvates or mixtures thereof. The novel derivatives of spirobebenzopyrans have the general...

Cyclopentanone analogues specifically have been noted as potential leadsfor anti-inflammatory activity with promising nonlinear optical properties. Six novelcyclopentanoneanalogs were synthesized and extensively characterized using Fourier Transform-Infrared spectroscopy (FT-IR), UV-Vis spectroscopy, NMR and Mass spectrometry, and their NonLinear O...

Diarylidenecyclohexanone (DAC) derivatives (Ia-i, IIa-c and IIIa-b) were synthesized, characterized and screened for their invitro antiplasmodial activities against erythrocytic stages of chloroquine (CQ) sensitive and resistant strains of P. falciparum by using SYBR green I fluorescence assay. SAR studies of DAC derivatives showed antiplasmodial a...

Fungi have a prominent status in fermentation for the production of different bio-products. Endophytic fungi isolated from medicinal plants are particularly formidable in their adaptability to solid state fermentation as an extension of its natural habitat and are also a potent source of broad-spectrum cellulolytic enzymes. We report for the first...

The indigenous people of South East Asian countries have been using plants for treating various ailments for thousands of years. Since knowledge on medicinal importance of plants has been passed on orally from generation to generation there have been no written documents to store this information for posterit y. In addition, colonial forces have di...

Where, χ(3)is third order nonlinear susceptibility, I PC is PC signal input I probe is Probe intensity N is Refractive Index of media λ is wavelength of the laser used (532nm) L is the cuvette length I 1 and I 2 are the pump intensities To synthesize, characterize and study second and third order non-linear optical properties of para-(methylthio)cy...

Carbon nanotubes (CNTs) are effective supports for nano metals and together they represent hybrids that combine unique properties of both. A microwave induced reaction was used to deposit nano palladium on carboxylated and octadecylamine functionalized multiwall CNTs, which were used to carry out C-C coupling reactions in DMF and toluene. These hyb...

The requirement for materials which exhibit good second and third order non-linear optical properties and also for materials which could sense metals in trace quantities has kindled renewed investigations. Organometallics and coordination compounds show a lot of promise as new NLO materials combining the variety of organic moieties with the strengt...

In the recent times, the common diseases like food poisoning, pneumonia, diarrhea etc. have been observed to be drug resistant. The present study deals with the synthesis of known chalcone derivatives using the Claisen-Schmidt condensation and further characterization using UV-vis, IR, 1H-NMR, 13C-NMR and mass spectrometry. These derivatives were f...

Nine chalcones were prepared via Claisen-Schmidt condensation, and characterized by UV–vis, IR, ¹H NMR, ¹³C NMR and mass spectrometry. One of the representative member 4-NDM-TC has been studied via single crystal XRD and the TGA/DTA technique. SHG efficiency and NLO susceptibilities of the chalcones have been evaluated by the Kurtz and Perry method...

Plants have been used by people to fulfil their spiritual, cultural, emotional and materialistic needs. In quest of using plants, man has forgotten the implications of overexploitation of these resources. Hence the question of restoring the balance has long been intriguing the conservation biologists. In this review we focus on the struggle of medi...

Many reports have shown that Andrographolide and its derivatives possess notable anticancer activity. In this study, we present the molecular docking studies of some newly synthesized C-12 substituted-14-deoxy-andrographolide derivatives. This helped to evaluate the probable targets of action responsible for the observed in vitro anti-cancer activi...

Andrographolide, the major diterpenoidal constituent of Andrographis paniculata (Acanthaceae) and its derivatives have been reported to possess plethora of biological properties including potent anti-cancer activity. In this work, synthesis and in-vitro anti-cancer evaluation of new C-12-substituted aryl amino 14-deoxy-andrographolide derivatives (...

The major challenge faced during the synthesis of spiro molecules is the stability due to the excessive strain on the spiro atom. Hence in order to stabilize the spiro atom we introduce ring fragments. We study the effect of ring size on the stability of the system.

The present study brings out the interaction between vasicine, an alkaloid and Adhatoda vasica Nees with double stranded DNA. The physico-chemical interaction between small molecules and nucleic acids is a major area of focus in screening drugs against various cancers. Molecular probing in our study using Molecular Operating Environment (MOE) has r...

Twenty isolates of Ganoderma spp. indigenous to India were used in this study. A reverse-phase high-performance liquid chromatography (HPLC) method was used to quantify 2 of the most bioactive triterpenes, ganoderic acid A (GAA) and ganoderic acid B (GAB), among the cultivated Ganoderma spp. The HPLC analysis was performed on an Agilent 1260 Infini...

Biofuels are a sustainable and cost-effective alternative to existing transportation fuels. Currently a combination of chemical and enzymatic degradation of lignocellulosic biomass to fermentable sugars has been pursued despite economic challenges. In this study, we have critically investigated individual and synergistic combination of Asperigillus...

In this paper we have identified accessions of a traditional medicinal plant, Adhatoda vasica Nees, from eight ecogeographically distinct nodes of Western Ghats of Malabar area, India. Alkaloids have been extracted from the leaves and analysed qualitatively using spectroscopic techniques. A method has been developed to determine relative amounts of...

In this study the applicability of Zirconium ion impregnated coconut fiber carbon (ZICFC) as an adsorbent for fluoride removal from water was investigated. The dependence of fluoride adsorption on the physicochemical properties includes pH, agitation time, adsorbent dosage, temperature, and the initial concentration of the adsorbate. Maximum defluo...

Present exploration deals with the therapeutic perspective of methyl gallate isolated from the leaf extract of Acacia nilotica (L.) Delile in contrast to food-borne bacterial pathogen's viz., Escherichia coli, Klebsiella pneumoniae, Salmonella typhimurium, Pseudomonas aeruginosa and Staphylococcus aureus with their evolutionary succession. The extr...

Andrographolide, the major labdane diterpenoid from Andrographis paniculata has been reported to be cytotoxic against various cancer cells in vitro. Our research efforts led to the discovery of novel 12-phenyl thio and 12-aryl amino-14-deoxy-andrographolide derivatives (III q and III r) with potent cytotoxic activity, 12-benzyl amino-14-deoxy-andro...

The hazardous effects of current nanoparticle synthesis methods have steered researchers to focus on developing newer eco-friendly methods for synthesizing nanoparticles using non-toxic chemicals. Owing to the diverse applications of nanoparticles in various fields such as catalysis, medicine, diagnostics, and sensors, several novel green approache...

The chemical, sugars composition and nutritional value of two Pleutorus species (Pleurotus florida and Pleurotus oyesterus) along with their sporeless and low-sporing mutants, were determined. Chemical composition evaluation included determination of crude fat content, crude protein, ash, crude fibre, carbohydrates, and nutritional value. The macro...

Various conditions for successful cultivation of twenty indigenous strains of G.lucidumwere optimized by studying the mycelial growth at different temperatures, pH and media. The quality differences of these cultivated strains of G.lucidumfrom different origins were investigated by comparing total polysaccharide, total triterpenoid and Ganoderic ac...

We report here the nonlinear optical (NLO) properties of eight bis-chalcones of D-π-A-π-D type. These dibenzylideneacetone (DBA) derivatives are synthesized by Claisen–Schmidt reaction. The compounds are characterized by UV–vis, FTIR, 1H NMR, 13C NMR, mass spectroscopy and powder XRD. By substituting different groups (electron withdrawing and elect...

In the title compound, C6H6BrNO, the Br atom is displaced from the pyridine ring mean plane by 0.0948 (3) Å, while the hydroxyl O atom and the methyl C atom are displaced by 0.0173 (19) and 0.015 (3) Å, respectively. In the crystal, mol­ecules are linked via O—H⋯N hydrogen bonds, forming chains propagating along the a-axis direction. These chains a...

Two novel optical power limiters, 2-[ethyl-(4-phenylazo-phenyl)-amino]-ethanol (E4PA) and 2-[ethyl-(4-trifluoromethyl-phenylazo-phenyl)-amino]-ethanol (E4TPA) were synthesized using a diazotization reaction. The purified azo material was made into thin films in a poly(methyl methacrylate) matrix using a gravity settling technique. The electronic no...

Methanolic extracts of cap and stipe of commercially obtained mushrooms Agaricus bisporus, Hypsizygus ulmarius, and Calocybe indica were analyzed for their antioxidant activity in different chemical systems including reducing power, free radical scavenging, ferric reducing antioxidant power (FRAP), superoxide scavenging, peroxide scavenging, metal...

Methanolic extracts of four cultivated edible mushrooms of Pleurotus spp. namely Pleurotus florida, Pleurotus sajor-caju, Pleurotus cystidiosus and Pleurotus djamor along with the sporeless/low sporing mutants of Pleurotus florida, and Pleurotus sajor-caju were analyzed for their antioxidant activity using different chemical assays. The electrochem...

A donor-π-acceptor-π-donor (D-π-A-π-D) type Bis-Chalcone, (1E,4E)-1,5-di-2-thienylpenta-1,4-dien-3-one (D2TDO) was synthesized by Claisen–Schmidt reaction. Structural characterization was done with the help of UV, FT-IR, 1H NMR, 13C NMR and Mass Spectroscopic techniques. Through gravity settling method, a homogenous film of D2TDO with 65 μm thickne...

The title compound, C13H10OS2, exhibits twists between the central C3O and ethene residues [O—C—C—C torsion angles = −8.4 (3) and 11.8 (3)°], and between the ethene and adjacent thio­phenyl residues [C—C—C—C torsion angles = −4.2 (3) and 10.5 (3)°]. As a result, the mol­ecule is non-planar, the dihedral angle formed between the terminal thio­phenyl...

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In this study the applicability of Zirconium ion impregnated coconut fiber carbon (ZICFC) as an adsorbent for fluoride removal from water was investigated. The dependence of fluoride adsorption on the physicochemical properties includes pH, agitation time, adsorbent dosage, temperature, and the initial concentration of the adsorbate. Maximum defluo...

In the presence of Al(III) ions, 5-hydroxyflavone (5HF) through a complexation reaction in MeOH, shows dual fluorescence, characterized by a newly developed peak at 554nm upon excitation at 363nm. In this communication, the subsequent ligand exchange reaction of the complex with fluoride ion causing a fluorescence enhancement followed by a decrease...

The present study was designed to investigate and arrive at the quantitative chemical composition, inclusive of fluoride content, of 56 kidney stone (renal calculi) samples from 50 patients aged between 20 and 60 years, admitted to Sri Sathya Sai Institute of Higher Medical Sciences Hospital, Prasanthigram, Anantapur District, Andhra Pradesh. Analy...

Activated charcoals which are effective for fluoride removal, when impregnated with zirconium metal ions have an increase in their fluoride adsorption capacity by 3 to 5 times to that of plain activated charcoal. Continuous down flow adsorption mode at room temperature was adopted to defluoridate drinking water. Three columns were prepared by the i...

A new water-soluble fluorescent fluoride ion signaling system has been developed based on the ligand exchange mechanism in aqueous medium. This procedure is based on the exchange of two Alizarin Red S (ARS) molecules coordinated to Al(III) by fluoride ion without interference from other common anions. The binary complex of ARS with Al(III) provides...

The batch adsorptive fluoride removal from water by Zirconium ion impregnated coconut shell carbon (ZICSC) was investigated. ZICSC was found to have fluoride adsorption capacity, 25 to 30 times that of plain activated carbon. The effect of various parameters such as pH, agitation time, and adsorbent dosage on fluoride removal were studied. The fluo...

A simple fluorescent detection based on the ligand exchange mechanism is proposed for the fluoride ion in aqueous media. This procedure is based on the exchange of 8-hydroxyquinoline (oxine) coordinated to Zr(IV) by fluoride ion without interference from other common anions. The ternary complex of oxine with [Zr(H(2)O)(2)EDTA].2H(2)O formed by repl...

Photochemical cycloaddition reactions constitute a convenient route to compounds which are difficult to prepare by other methods. An experiment on a [2+2] cycloaddition is relatively easy to carry out using sunlight for photochemical mediation. The starting material, dibenzylideneacetone, is easily prepared from benzaldehyde and acetone. The Pyrex...

Defluoridation of drinking water was carried out by the continuous down flow adsorption mode at room temperature. Five columns were prepared by the impregnation of ZrOCl2, CaO, Alum, CaCl2 and Borax in activated coconut shell charcoal. Known fluoride influent water was run into the column at a constant rate of 4.0 L/h and a constant level of water...

The isolation and spectral data of di-(2-ethyl) hexyl phthalate (1) from Cassia auriculata leaves are reported.