Hardik BhattNirma University | NU · Institute of Pharmacy
Hardik Bhatt
Doctor of Philosophy
About
45
Publications
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Introduction
Hardik Bhatt currently works at the Institute of Pharmacy, Nirma University. Hardik does research in Structural Biology, Cancer Research and Medicinal Chemistry.
Publications
Publications (45)
There is a need to develop innovative, safe, and more effective treatment methods for lung cancer due to obstacles including resistance, side effects, and low bioavailability, among others related to present medicines. Our previous research findings gave some promising results of tetrahydroquinoline (THQ) derivatives as mTOR inhibitors for the trea...
Type 2 diabetes mellitus (T2DM) is a potentially fatal metabolic disorder worldwide, in this COVID-19 era. Long-term allopathic treatment has a variety of side effects, prompting the search for alternative therapies. Oleuropein, the primary bioactive ingredient of Olive Leaf Extract (OLE), has shown noteworthy actions to control T2DM. The present s...
Telomerase is a ribonucleoprotein (RNP) responsible for the maintenance of chromosomal integrity by stabilizing
telomere length. Telomerase is a widely expressed hallmark responsible for replicative immortality in 80–90% of
malignant tumors. Cancer cells produce telomerase which prevents telomere shortening by adding telomeres
sequences beyond H...
Tankyrase (TNKS) enzymes remained central biotargets to treat Wnt-driven colorectal cancers. The success of Olaparib posited the druggability of PARP family enzymes depending on their role in tumor proliferation. In this work, an MD-simulation-based comparative assessment of the protein–ligand interactions using the best-docked poses of three selec...
ABSTRACT: Lenvatinib mesylate (LNB) is a potent anticancer
drug used in the treatment of thyroid cancer. No green technique
incorporating the use of green analytical chemistry (GAC) in
HPTLC for LNB has been reported. The current study focuses on
how GAC was used in the development and validation of a green
HPTLC technique using LNB. The mobile pha...
Efforts have been made to find an efficient scaffold (and its substitution) that can be used for the treatment of lung cancer via mTOR inhibition. A detailed literature search was carried out for previously reported mTOR inhibitors. The present review is focused on lung cancer; therefore, descriptions of some mTOR inhibitors that are currently in c...
Vaccines are used as one of the major weapons for the eradication of pandemic. However, the rise of different variants of the SARS-CoV-2 virus is creating doubts regarding the end of the pandemic. Hence, there is an urgent need to develop more drug candidates which can be useful for the treatment of COVID-19. In the present research for the scienti...
Structurally diversified coumarin analogs were found to display a remarkable array of affinity with the different molecular targets. 4-hydroxy-7-methylcoumarin was synthesized from m-cresol and malonic acid. In basic media, the 4-hydroxy group of coumarin is replaced further by the bromopropoxy group. Several potent piperazine-containing scaffolds...
Background
Alzheimer’s disease (AD) impairs memory and cognitive functions in the geriatric population and is characterized by intracellular deposition of neurofibrillary tangles, extracellular deposition of amyloid plaques, and neuronal degeneration. Literature suggests that latent viral infections in the brain act as prions and promote neurodegen...
A chronic, life threatening and immuno-suppressing malady caused by Human immunodeficiency virus (HIV) is formally known as Acquired Immune Deficiency Syndrome (AIDS). Currently, combinations of several anti-retroviral drugs are being used for the management of HIV infection. These drugs possess certain limitations and hence researchers across the...
In the present research, efforts were made to develop the novel, selective, and nontoxic CDK2 inhibitors. Previously reported potent CDK2 inhibitors were utilized for the pharmacophore creation through the GASP module of Sybyl X. Furthermore, pharmacophore-based virtual screening was carried out through the NCI database giving 20,542 molecules. Top...
Cancer is considered the second most prevailed cause of death worldwide. Newer strategies are developed to treat cancer over prevalent traditional chemotherapeutic agents, and targeting kinases is one of them. Kinases are crucial to understanding as well as a potent target for the discovery of anticancer agents. Protein kinases, which include serin...
Type 2 diabetes mellitus is a serious metabolic disorder affecting global health and results in number of serious life-threatening complications leading to increased mortality rate. Complications can be prevented with early diagnosis and appropriate care. International Diabetes Federation and World Health Organization suggested an urgent need of na...
Tankyrase is an emerging target of 17 membered poly(ADP-ribose)polymerase enzyme family for the treatment of Wnt driven cancers. TNKS are associated with many cellular functions; Wnt–β-catenin signaling, telomere homeostasis, mitotic spindle formation etc. The inhibition of cell growth could be achieved by the inhibition of TNKS through Wnt-signali...
Insulin signaling pathways in muscle tissue play a major role in maintaining glucose homeostasis. Dysregulation in these pathways results in the onset of serious metabolic disorders like type 2 diabetes. Robustness is an essential characteristic of insulin signaling pathways that ensures reliable signal transduction in the presence of perturbations...
Introduction:
Tankyrase (TNKS) inhibitors gained significant attention as therapeutic targets in oncology as a result of their potency. Their primary role in inhibiting the Wnt-signaling pathway makes them a very important class of compounds with the potential to be used as a combination therapy in future treatments of colorectal cancer.
Areas co...
Rising mortality due to cancer has led to the development and identification of newer targets and molecules to cure the disease. Telomerase is one of the attractive targets for design of many chemotherapeutic drugs. This research highlights the designing of novel telomerase inhibitors using ligand-based (3D-QSAR) and structure-based (molecular dock...
Genetic mutations in APC or CNTBB1 gene with aberrant canonical Wnt/β-catenin pathway are responsible for more than 90% of colorectal carcinogenesis. Tankyrases (TNKS) are known to downregulate Wnt signaling by stabilizing AXIN protein through poly(ADP ribose)polymerization or PARSylation process and subsequently, promoting degradation of intracell...
Lung cancer is one of the most prevailed cancer worldwide. Many genes get mutated in lung cancer but the involvement of EGFR, KRAS, PTEN and PIK3CA are more common. Unavailability of potent drugs and resistance to the available drugs are major concern in the treatment of lung cancer. In the present research, mTOR was selected as an important altern...
Background
Inhibition of HIV-I protease enzyme is a strategic step for providing better treatment in retrovirus infections which avoids resistance and has less toxicities.
Objectives
In the course of our research to discover new and potent protease inhibitors, 3D-QSAR (CoMFA and CoMSIA) models were generated using 3 different alignment techniques...
Cancer is one of the major public catastrophes worldwide and as per WHO, cancer is the leading cause of death universally after CVS disorders accounting for 9.6 million deaths in 2018. WHO statistics revealed five dangerous types of cancer viz. lung, breast, colorectal, prostate and skin. In male, lung cancer causes highest death, while in female,...
Human Tankyrases (TNKS) are the potential and emerging targets for the treatment of many cancers like colon, breast, bladder, lung, gastric, pancreatic adenocarcinoma etc. Inhibition of Tankyrase results in inhibition of Wnt Signaling and indirect inhibition of telomerase actions which ultimately leads to cell growth inhibition and cell death respe...
A Novel series 2 & 3-(4-aminobenzamido) benzoic acid derivatives were designed virtually considering the basic pharmacophore N-(3,5-bis (trifluoromethyl) phenyl)- 5-chloro-2-hydroxybenzamide.The energy minimized conformers of each molecule was generated and docked with M. tuberculosis DHFR enzyme with PDB id: 1DF7 using Autodock 4.2.5.1. Most of th...
As per the World Health Organization (WHO), cancer is the second most leading cause of death after cardiovascular diseases in worldwide with around 9.88 million total new cases and 1.08 million were observed due to skin cancer in 2018. Amongst two types of skin cancer, progression of melanoma cancer is increasing day by day due to the environmental...
mTOR has become a promising target for many types of cancer like breast, lung and renal cell carcinoma. CoMFA, CoMSIA, Topomer CoMFA and HQSAR were performed on the series of 39 triazine morpholino derivatives. CoMFA analysis showed q ² value of 0.735, r ²cv value of 0.722 and r ²pred value of 0.769. CoMSIA analysis (SEHD) showed q ² value of 0.761...
Alzheimer's disease (AD) is an enervating and chronic progressive neurodegenerative disorder, occurring frequently in the elderly and adversely affecting intellectual capabilities and the cognitive processes. Bergenin possesses efficacious antioxidant, antiulcerogenic, anti-HIV, hepatoprotective, neuroprotective, anti-inflammatory and immunomodulat...
Background
We report here an efficient synthesis of new Mannich products 4(a-m) in excellent yields via multi-component reaction for the condensation of 5-bromothiophene- 2-carboxaldehyde (5-BT-2C), 2,4-dihydroxybenzophenone (2,4-DHBP) and primary/secondary amine derivative using Ethyl Ammonium Nitrate (EAN) as ionic liquid, which is reusable and p...
Cancer is a second major disease after metabolic disorders where the number of cases of death is increasing gradually. Mammalian target of rapamycin (mTOR) is one of the most important targets for treatment of cancer, specifically for breast and lung cancer. In the present research work, Comparative Molecular Field Analysis (CoMFA) and Comparative...
In order to design novel anti-HIV agents, pharmacophore modelling, virtual screening, 3D-QSAR and molecular docking studies were performed. Pharmacophore model was generated using 17 structurally diverse molecules using DISCOtech followed by refinement with GASP module of Sybyl X. The best model containing four features; two donor sites, one accept...
Development of novel synthetic compounds for the treatment of skin cancer is much needed, as there are sudden rise in incidences of skin cancer throughout the world and available chemotherapy is facing problems of resistance. Hence, present research efforts were made to discover potent molecules against skin cancer. Pharmacophore models were develo...
According to WHO statistics, lung cancer is one of the leading causes of death among all other types of cancer. Many genes get mutated in lung cancer but involvement of EGFR and KRAS are more common. Unavailability of drugs or resistance to the available drugs is the major problem in the treatment of lung cancer. In the present research, mTOR was s...
Aurora-B kinase played crucial role in cell cycle events and is identified as an important factor in regulation of spindle check point assembly. Thus, it can be proved as an important target in the field of oncology. 3D-QSAR model was generated using 54 molecules reported in literature containing thienopyrimidine and thienopyridine as scaffolds. Al...
Famotidine (FAM), Diclofenac (DCF) and Paracetamol (PCM) are used in combination for musculoskeletal disorders. A simple, sensitive, rapid, precise, reproducible and accurate spectrophotometric method for simultaneous determination of FAM, DCF and PCM was developed. The method was based on UV spectrophotometric determination of three drugs using si...
HIV integrase enzyme is well established potential target for antiretroviral therapy since a decade. Resistance to drugs (Raltegravir and Elvitegravir) used as HIV integrase inhibitors is already been identified and there is an urgent need to discover newer molecules which can overcome this issue. With this aim, ligand based drug design technique,...
SGLT2 has become a target of therapeutic interest in diabetes research. CoMFA and CoMSIA studies were performed on C-aryl glucoside SGLT2 inhibitors (180 analogues) as potential anti-diabetic agents. Three different alignment strategies were used for the compounds. The best CoMFA and CoMSIA models were obtained by means of Distill rigid body alignm...
This paper describes Raman spectroscopy as a reagent - free tool for the direct simultaneous quantitative estimation of metformin (MET) and gliclazide (GLI) in combined dosage forms. The percentage of MET and GLI were determined in a few seconds directly without the dissolution of the tablets. No spectral interference from tablet excipients were se...
Cyclocondensation of benzofuran chalcones (2) with paracetamol hydrazide (5) resulted in the formation of benzofuran-2-pyrazolines (6a-n). Chalcones are synthesized by Claisen-Schmidt condensation involving treatment of 2-acetyl benzofuran (1a) with different aromatic aldehydes. The compounds were evaluated for antitubercular, antimicrobial and ant...