
Kiran GangarapuAnurag University (Former Anurag Group of Institutions Lalitha College of Pharmacy) · Pharmacy
Kiran Gangarapu
M.Pharmacy, Ph.D
About
91
Publications
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Introduction
Design and synthesis of novel antidiabetic agents
Additional affiliations
July 2016 - present
Anurag University
Position
- Professor (Associate)
September 2009 - September 2012

S. R. College of Pharmacy
Position
- Professor (Assistant)
Publications
Publications (91)
Background: Avaram Amrit, derived from a traditional medicinal plant, has shown potential in diabetes management. This study aimed to evaluate its clinical efficacy in glycemic control. Methods: A 12-week, open-label clinical trial was conducted with 9 type 2 diabetes patients. Participants received Avaram Amrit extract daily. Fasting and postprand...
Cancer is a disease characterized by uncontrolled growth of abnormal cells in the body. Natural substances with potential anticancer properties, including guava and mango seeds, have been researched. Guava seeds contain tannins, phenolic acids, essential oils, and fatty acids that suppress cancer and induce apoptosis. Similarly, Mango seeds contain...
A novel series of oxazolyl‐pyrimidine derivatives (11 a–j) have been synthesized and structures were confirmed by spectral data. The synthesized compounds were assessed for cytotoxic profile towards human cervix cancer (SiHa), lung cancer (A549), breast cancer (MCF‐7), and colon cancer (Colo‐205) cell lines by employing MTT assay and using etoposid...
Vascular dementia (VaD) accounts to 30% of cases and is predicted as second most common form of dementia after Alzheimer’s disease by WHO. Earlier studies reported that plant-derived pentacyclic triterpenoids possess a wide range of pharmacological activities but these compounds are not extensively studied for their neuroprotective potential agains...
In an attempt to develop therapeutic agents to treat Alzheimer's disease, a series of flavonoid analogues were collected, which already had established acetylcholinesterase (AChE) enzyme inhibition activity. For each molecule we also collected biological activity data (Ki). Then, 3D-QSAR (quantitative structure-activity relationship model) was deve...
The present work aimed to develop a Field-based 3D-QSAR model with existing JAK-2 inhibitors. The JAK-STAT pathway is known to play a role in the development of autoimmune diseases, including rheumatoid arthritis, ulcerative colitis, and Crohn's disease. Dysregulation of JAK-STAT is also linked to the development of myelofibrosis and other myelopro...
A sensitive validated method has been developed for the quantification of Nadolol in rat plasma by high performance liquid chromatography coupled with tandem mass spectrometry (HPLC-MS/MS) using deuterated Nadolol (Nadolol D9) as internal standard (IS). The liquid-liquid extraction method using ethyl acetate was employed for the sample pretreatment...
Though there is no perfect way to define the term “nanotechnology,” we can sure put the term as “technology at the nanoscale.” Aquaculture, or in other words, aquaculture, can be defined as a method for the proliferation of aquatic organisms under controlled aquatic environmental conditions. Aquaculture has been identified as one of the quickest-de...
Nanotechnology is the control of materials on a nuclear or subatomic scale, particularly to assemble infinitesimal products. Placing particles like they were blocks, nanotechnology will give us unlimited oversight over the design of an issue, permitting us to construct any substance or construction allowed by the laws of nature. Nanotechnology has...
Background
The development of digital technologies and the evolution of open innovation approaches have enabled the creation of diverse virtual organizations and enterprises coordinating their activities primarily online. The open innovation platform titled “International Natural Product Sciences Taskforce” (INPST) was established in 2018, to bring...
Background: The development of digital technologies and the evolution of open innovation approaches have enabled the creation of diverse virtual organizations and enterprises coordinating their activities primarily online. The open innovation platform titled "International Natural Product Sciences Taskforce" (INPST) was established in 2018, to brin...
Background: The development of digital technologies and the evolution of open innovation approaches have enabled the creation of diverse virtual organizations and enterprises coordinating their activities primarily online. The open innovation platform titled “International Natural Product Sciences Taskforce” (INPST) was established in 2018, to brin...
The development of digital technologies and the evolution of open innovation approaches have enabled the creation of diverse virtual organizations and enterprises coordinating their activities primarily online. The open innovation platform titled “International Natural Product Sciences Taskforce” (INPST) was established in 2018, to bring together i...
Isatins are the important class of heterocyclic scaffolds which occupied a great role in the drug discovery. In the present study we synthesized Bis isatin derivatives(IIIa-f) and confirmed by physical and spectral data.compounds are evaluated for CNS activties (viz: gross behavioural study, locomotor activity, anticonvulsant activity) and antioxid...
Actinobacteria are a potent source of secondary metabolites. These metabolites have unique metabolic activities which make them an important component in the development of a drug. Sesquiterpene belongs to the class of terpenes and are large structurally diverse group of marine natural products with C-15 carbon skeleton. Whole genome sequence infor...
A series of novel benzoxazole-isatin conjugates were synthesized by treating 2-amino benzoxazole with 5 and 7 substituted isatin derivatives and were screened for in vitro antimicrobial and cytotoxic activities. The results showed that all the synthesized compounds shown mild to potent antibacterial activity. The MIC values were found between 10 an...
A simple, selective and rapid ultra performance liquid chromatography-tandem mass spectrometry method was developed and validated for the simultaneous estimation of dolutegravir, lamivudine and tenofovir in bulk and tablet dosage form. Chromatographic separation was attained on Acquity Ethylene Bridged Hybrid (BEH) C18 column (50 × 2.1 mm, 3.5 µm),...
Designed and synthesized a series of novel urea derivatives of pyrimidine-pyrazole, and screened for their anticancer activity. Compounds with (3,5-dinitro and 3,4,5-trimethoxy) substitution were exhibited more potent cytotoxicity than standard Etoposide. Molecular docking studies suggested that compounds were well occupied at the colchicine bindin...
BK channels, or voltage-gated Ca2+ channels, are essential regulators of neuronal excitability and muscular contractions, all of which are abnormal in epilepsy, a chronic neuronal disease. The form, frequency, and transmission of action potentials (APs), as well as neurotransmitter release from presynaptic terminals, are all influenced by BK channe...
A new library of structurally modified aryl quinazoline-isoxazole (12a–j) derivatives have been designed, synthesized and characterized by ¹HNMR, ¹³CNMR and mass spectral data. Further these compounds were evaluated for anticancer applications against four human cancer cell lines including PC3, DU-145 (prostate cancer), A549 (lung cancer) and MCF-7...
In India as well as globally diabetes is in a state of high risk and only next to cardiovascular disease. As per the WHO the risk of diabetes is expected to rise to about 511 million by 2030. In quest for novel targets for type-2 diabetes many targets were elucidated such as Glycogen Synthase Kinase-3 (GSK-3), Dipeptidyl Peptidase (DPP-IV), PPAR-,...
A new library of amide derivatives of imidazo[2,1-b][1,3,4]thiadiazoles (11a–j) have designed and synthesized and their structures determined by ¹H NMR, ¹³C NMR, mass and HRMS spectral data. Further, all these compounds were evaluated for their anticancer potentials on a panel of cancer cell lines like MCF-7, MDA MB-231 (breast carcinoma), A549 (lu...
Background
Siddha Medicine is a valuable therapeutic choice which is classically used for treating viral respiratory infections, this principle of medicine is proven to contain antiviral compounds.
Objective
The study is aimed to execute the In Silico computational studies of Phytoconstituents of Siddha Official Formulation Kabasura Kudineer and N...
Vascular dementia (VaD) is well recognized as the second most familiar form of dementia in the aged population. The present study is aimed to investigate the neuroprotective effects of ethanolic extract of leaves of Ocimum sanctum (EEOS) against hyperhomocysteinemia (HHcy)-induced vascular dementia (VaD) in Wistar rats. HHcy was induced by administ...
Parkinson's disease (PD) is a major cause of morbidity and mortality among older individuals. Several researchers have suggested that iron chelators which cross the blood-brain barrier (BBB) might have clinical efficacy in treating PD. Therefore, efforts are made not only in order to improve the effect of L-dopa but also to introduce drugs which pr...
Objective:
The present study focused to build pyridine and quinazoline rings in a single molecule and designed a new fused Pyrido[2,1-b] quinazoline to have a better pharmacological activity.
Material and methods:
A three component, one-pot synthesis of substituted-1H-Pyrido[2,1-b] quinazoline derivatives has been described by conventional and m...
Stroke is becoming a main cause of early death and disability in developing countries like India, and it is mostly enhanced by increased predominance of major risk factors. A detailed knowledge about the nature and magnitude of the stroke cases in this particular area is not only important for acute treatment but also it helps to prevent hospital a...
A series of amide derivatives of azaindole-oxazoles (11a–n) were designed and synthesized and their structures were confirmed by ¹HNMR, ¹³CNMR and mass spectral analysis. Further, these derivatives were screened for their anticancer activity against human cancer cell lines viz; MCF7 (breast), A549 (lung) and A375 (melanoma). In vitro anticancer act...
A novel pharmacophore with theophylline and acetylene moieties was constructed by using a fragment-based drug
design and a series of twenty theophylline containing acetylene conjugates were designed and synthesized, and all
the compounds were evaluated by enzyme-based in vitro α-amylase inhibition activity. The in vitro evaluation revealed
that mos...
A new series of Pyrazolo[3,4‐d]pyrimidine containing amide derivatives (8 a‐l) were designed, synthesized, and evaluated for their in vitro α‐amylase inhibitory activity. The IC50 values of the target compounds ranged from 1.60±0.48 to 2.04±1.20 μM as compared to the standard acarbose 1.73±0.05 μM. All the Pyrazolo[3,4‐d]pyrimidine amide derivative...
Saquinavir mesylate (SQM) is subjected to forced degradation under conditions of hydrolysis, oxidation, dry heat, photolysis as recommended by International conference on Harmonization guideline Q1A (R2). In total, degradation products (I-V) were formed in acidic hydrolytic, alkaline hydrolytic and oxidative conditions. SQM and all degradation prod...
β-amino acids are the important building blocks for the production of medicines, a precursor for β lactams and building blocks for oligomers. The present study illustrates, novel and efficient asymmetric method for the synthesis of b amino acids has been described. So, the present work deals with the transformation of chiral aspartic acid to β, g-a...
α-Glucosidase of the synthetic Theophylline containing acetylene derivatives was rarely explored despite these agents have wide range of biological activities. The In vitro α-glucosidase inhibitory activity of the synthetic motifs Va-e were evaluated using acarbose as standard positive control. The IC50 values of these compounds were ranged from 22...
The aim of the present study was to develop a reverse phase high performance liquid chromatographic (RP-HPLC) method for the simultaneous estimation of Betamethasone Dipropionate (BDP) and Calcipotriene (CPT). By using phosphate buffer (pH 3.0) and mobile phase consists The retention times (Rt) were found to be 2.669 min. and 3.855 min. for BDP and...
Insert grafical abstract figure here Abstract. The aim of the present research work is to validate the apixaban content in bulk and pharmaceutical dosage formulation and validate it as per ICH guidelines. A simple, rapid, precise and highly selective spectrophotometric method was developed for estimation of apixaban in tablet dosage form by Area Un...
A simple, specific, validated reverse phase high performance liquid chromatographic method has been developed for the quantification of related impurities of Efavirenz in bulk drug substance. In this method impurities are quantified successfully at 0.2% quantification threshold. This method utilizes high purity silica based RP-C18 column i.e Inerts...
Cancer, which is considered to be the world’s most serious illness cause 8.2 million deaths and this rate may double by 2030. We herein report a new series of 3-(2-(p-substituted)-2-((5-phenyl-1,3,4-thiadiazol-2-yl)imino)-2-(p-substituted)ethylidene)indolin-2-one (15–19) and 5-substituted-5′-substituted phenyl-2′,4′-dihydrospiro[indoline-3,3′-pyraz...
The NF-κB is family of transcription factor has important role in innate immunity and inflamation which regulate expression of both pro-and anti-inflammatory mediators. Dysregulation of NF-κB pathways results in severe diseases such as arthritis, immunodeficiency, autoimmunity, and cancer. Hence, a method of inhibiting NF-κB signaling has potential...
A novel synthesis of 2-hydroxy-N′-(2-oxoindolin-3-ylidene) benzohydrazide derivatives was synthesized by the condensation of 2-hydroxybenzohydrazide with substituted isatins. The synthesized compounds were characterized by FT-IR,
1
H-NMR, and mass spectral data. Further, the compounds were screened for
in vivo
anti-inflammatory activity by carragee...
A series of novel 3-(substituted)-2-(substituted quinazolinylamino)quinazolin-4(3H)-ones were synthesized by the reaction of 3-(substituted)-2-hydrazino-quinazoline-4(3H)-ones with 2-phenyl-3,1-benzoxazin-4-one. The starting materials 3-(substituted)-2-hydrazino-quinazolin-4(3H)-ones were synthesized from various primary amines by a multistep synth...
The main objective of this study was to develop mebeverine hydrochloride colon targeted drug delivery system using compression coating technique for effective treatment of irritable bowel syndrome. This work was mainly focused on the formulation & in-vitro evaluation of compression coated tablets of mebeverine hydrochloride with different pH depend...
A series of novel 7-azaindole (1a–j) and 7-azaisatin (2a–j) derivatives were screened for their in vitro breast, lung and liver cytotoxic activities against MCF-7, A549 and HEPG2 cell lines, respectively, by MTT assay method. Among them, compounds 1h, 1i, 2h and 2i have shown good breast cytotoxic activity, and compounds 1h and 1i showed good lung...
Background and Objective: A Simple, Green and efficient procedure for the synthesis of 4-aryl-3, 4-dihydropyrimidine-2(1H)-ones/thione (Biginelli reaction) from 1, 3-dicarbonyl compound, substituted aldehydes and urea/thiourea in the presence of Sodium Dodecyl Sulphate (SDS), a novel catalyst has been introduced in this study. Materials and Methods...
A series of new β-isatin aldehyde-N,N′-thiocarbohydrazone, bis-β-isatin thiocarbohydrazones, bis-β-isatin carbohydrazones was synthesized by condensation of 5-substituted isatin with thiocarbohydrazide or carbohydrazide. The chemical structures of the newly synthesized compounds were confirmed by FT-IR, 1H NMR, and mass spectral analysis. The synth...
The present study was aimed at evaluating the cardioprotective effect of novel synthetic 𝑁
,𝑁
-bis[5-methyl-2-oxo-1,2-dihydro-
3H-indol-3-ylidene]carbonohydrazide derivative, by estimating the various biomarkers like creatine kinase-myoglobin (CK-MB),
lactate dehydrogenase (LDH), aspartate aminotransferase (AST), and triglycerides (TG) in plas...
The present study was aimed at evaluating the cardioprotective effect of novel synthetic ,-bis[5-methyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene]carbonohydrazide derivative, by estimating the various biomarkers like creatine kinase-myoglobin (CK-MB), lactate dehydrogenase (LDH), aspartate aminotransferase (AST), and triglycerides (TG) in plasma and ant...
The aim of the present study was to evaluate the hepatoprotective activity of 1-(4-(dimethylamino)benzylidene)-5-(2-oxoindolin-3-ylidene) thiocarbohydrazone, a novel isatin derivative against carbon tetrachloride (CCl4)-induced hepatotoxicity in rats. Hepatic damage was induced by administration of CCl4 (1 ml/kg, b.w., p.o.) in combination with liq...
In the present study, the synthesis of new bis-isatin carbohydrazone derivatives and their antimicrobial and antioxidant activities were investigated. The structures of new compounds were elucidated by Fourier transform infrared, 1H nuclear magnetic resonance and mass spectra. The antimicrobial activity of the compounds was determined by using the...
A series of β-Isatin aldehyde-N,-thiocarbohydrazone derivatives were synthesized and assayed for their in vitro antimicrobial and antioxidant activity. The new compounds were characterized based on spectral (FT-IR, NMR, MS) analyses. All the test compounds possessed a broad spectrum of activity having MIC values rangeing from 12.5 to 400 μg/ml agai...
In obtaining some new cytotoxic and chemopreventive agents with potent antiproliferative activity against cancer cells, a series of new -isatin aldehyde-N,N'-thiocarbohydrazone, bis--isatin thiocarbohydrazones, bis--isatin carbohydrazones, N,2-bis(thiophen-2-ylmethylidene) thiocarbohydrazone and N,2-bis(thiophen-2-ylmethylidene) carbohydrazone deri...
. A novel series of 4-(substituted benzylamino)-5-substituted phenyl-3-amino-1, 2, 4-triazole deriva-tives were synthesized by reaction of 5-substituted phenyl-3,4-diamino-1,2,4-triazole with different aromatic aldehydes. The structures of the compounds were synthesized and characterised by elemental analysis, 1H NMR, Mass and IR Spectra. The title...
The methanolic extract of Trianthema portulacastrum (Aizoaceae) was evaluated for antihyperlipidemic and antioxidant activity in high-fat-diet–induced hyperlipidemic rats. It was found that the extract caused a significant reduction in the lipid levels in hyperlipidemic rats and was comparable with the standard anti-hyperlipidemic drug atorvastatin...
The whole plant of the methanolic extract from Leucas cephalotes was screened for in vitro antioxidant (using the DPPH method), in vivo analgesic (using hot plate test in mice) and anti-inflammatory (using rat paw edema test) activities. The methanolic extract of Leucas cephalotes (MELC) scavenged the DPPH radicals in a dose-dependent manner. The I...
A series of 2-substituted-((N, N-disubstituted)-1, 3-benzoxazole)-5-carboxamides derivatives were synthesized by the reaction of 2-substituted-5-carbomethoxy benzoxazole with different secondary amines. The newly synthesized compounds were characterized on the basis of spectral (FT-IR, 1H NMR, MS) & elemental analysis. All these compounds were scre...