
Varadaraj Bhat GiliyaruManipal Academy of Higher Education | MAHE · Manipal College of Pharmaceutical Sciences (MCOPS)
Varadaraj Bhat Giliyaru
M. Pharm., Ph.D.
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41
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Publications (41)
The enzyme chorismate mutase (or CM that is vital for the survival of bacteria) is an interesting pharmacological target for the identification of new anti-tubercular agents. The 5,5-disibstituted pyrazolo[4,3-d]pyrimidinone derivatives containing the fragment based on 4-amino-1-methyl-3-propyl-1H-pyrazole-5-carboxamide were designed and explored a...
In view of the reported chorismate mutase (CM or MtbCM) inhibitory activities of 3-indolylmethyl substituted (pyrazolo/benzo)triazinone derivatives the structurally similar 3-(benzofuran-2-ylmethyl) substituted (pyrazolo/benzo)triazinones were designed and evaluated in silico against CM. The docking of target molecules was performed at the interfac...
The Pd/Cu-catalyzed tandem coupling-cyclization-N-deprotection in a single pot (Method a) vs sequential coupling-cyclization under similar conditions (Method b) has been studied using propargylamine as a terminal alkyne under environmentally friendly conditions. The first sequence (Method a) was followed to afford the N-unsubstituted indoles when 2...
A series of novel isatin–indole derivatives has been designed as potential inhibitors of chorismate mutase (CM) that is known to be present in bacteria, fungi and higher plants but not in human. The design was supported by in silico docking studies that predicted strong interactions of these molecules with CM. The target compounds were synthesized...
The chorismate mutase (CM) is considered as an attractive target for the identification of potential antitubercular agents due to its absence in animals but not in bacteria. A series of 3-indolylmethyl substituted pyrazolotriazinone derivatives were designed and docked into CM in silico as potential inhibitors. These compounds were efficiently synt...
Propargylamine (secondary) has been explored as a building block in synthesizing indoles via an ultrasound assisted Pd/Cu-catalyzed coupling-cyclization method. Indoles containing a pyrazole moiety at C-2 attached via the –CH2NH– linker (designed as potential anti-tubercular agents) were synthesized first and then generality/scope of the methodolog...
Background: Streblusol E, a phenolic phytoconstituents of Streblus asper is a potential antihepatitis B viral agent. Objective: Current study is to mechanistically analyze the probable site of action for streblusol E. Material and methods: Streblusol E has been docked with EF3-CaM adenylyl cyclase(1PK0), deoxycytidine kinase(2NOA), human nucleoside...
The aligned manuscript reports synthesis, screening and QSAR analysis of twenty six 1, 2, 4-triazole analogues from their respective aromatic carboxylic acids. The structures of synthesized analogues were characterized using physical and spectral analysis. 1,2,4-Triazole analogs antioxidant capacity was determined using DPPH radical scavenging assa...
Phytochemistry accords with phytochemicals which are obtained from a plant source. In recent years, there is a great insistence to phytochemical constituents as they are devoid of adverse reactions. On ac-count of lack of modern scientific evidence for their basis of action on diseases, a crude extract is not well accepted. But due to the adverse s...
Phytochemistry accords with phytochemicals which are obtained from a plant source. In recent years, there is a great insistence to phytochemical constituents as they are devoid of adverse reactions. On account of lack of modern scientific evidence for their basis of action on diseases, a crude extract is not well accepted. But due to the adverse si...
The three dimensional quantitative structure activity relationships(3D-QSAR) of a series of previously synthesized 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted-2-propanol analogs(TDFPP) as antifungal against candida albicans, were studied using kNN(K nearest neighbour) protocol. This was in order to explore the selectivity requir...
1,5-Benzodiazepines were synthesized using chalcone & o-phenylene diamine. Their structures were characterized using physical & spectral data. These molecules are analogous to anthracin, henceforth evaluated for their anti-breast cancer activity, using in vitro model MTT assay against MCF-7 cell line. Results revealed that these molecules are havin...
1,5- Benzodiazepines and its derivatives constitute an important class of heterocyclic compounds which have proven its medicinal identity as anticancer, antioxidant, cardiovascular agents, viral infection, anticonvulsant, analgesic, sedative, antidepressive, and hypnotic agents. Keeping this in mind, the current research work is to synthesize 2,3-D...
Biginelli dihydropyrimidinone derivatives as structural analogs of Monastrol, a known Human kinesin Eg5 inhibitor, were synthesized and the IC50 values of synthesized compounds against the proliferation of HepG2 (Human hepatocellular carcinoma) and HeLa (Human epithelial carcinoma) cell lines were determined through MTT assay. Molecular docking stu...
Mass spectrum of compound 3 g.
Proton NMR spectrum of compound 3j.
Proton NMR spectrum of compound 3 g.
Mass spectrum of compound 1d.
Mass spectrum of compound 3j.
Proton NMR spectrum of compound 1d.
Carbon NMR spectrum of compound 3f.
Mass spectrum of compound 3f.
In the present work, we had synthesized some novel pyrimidine-2,4-diones by condensing various substituted amines with 3-substituted -6-chlorouracil. The structure of the synthesized compounds was characterized using physical & spectral data. Novel pyrimidine-2,4-(1H,3H)-diones were then screened for their antimicrobial profile using Kirby Bauer Di...
Crocin( Crocetin di-gentiobiose ester ) is the chemical constituent isolated from the Saffron, the dried trifid stigma of the plant Crocus sativus L. and also from the fruits of Gardenia(Gardenia jasminoides Ellis) It is found to be effective as antiproliferative, anti-oxidant, learning and memory enhancer, brain neurodegenerative disorder, sperm c...
1,5- Benzodiazepines and its derivatives constitute an important class of heterocyclic compounds which possess wide range of therapeutic and pharmacological properties as anticonvulsant, analgesic, sedative, antidepressive, and hypnotic agents. In the last decade, the area of biological interest of 1,5-Benzodiazepines has been extended to several d...
The aim of current research work was to synthesized some novel pyrimidine-2,4-diones by condensing various substituted amines with 3-substituted -6-chlorouracil. The structure of the synthesized compounds were characterized using physical & spectral data. Novel pyrimidine-2,4-(1H,3H)-diones were then screened for their antimicrobial profile using k...
Cocos nucifera (CN), commonly known as Coconut tree, is used for its several beneficial health effects as antitumor, anthelmintic, antidotal, antiseptic, aperients, aphrodisiac, astringent, bactericidal, depurative, diuretic, hemostat, pediculicide, refrigerant, stomachic,styptic, suppurative and vermifuge. Our objective was to determine the antiox...
The fruits of Cocos nucifera Linn. (Arecaceae) have long been used in traditional medicine for the treatment of cardio-metabolic disorders.
To evaluate the ethanolic extract of Cocos nucifera Linn. endocarp (CNE) for its vasorelaxant activity on isolated rat aortic rings and antihypertensive effects in deoxycorticosterone acetate (DOCA) salt-induce...
QSAR analysis of a series of previously synthesised 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted-2-propanols(TDFPP) as analogues of fluconazole were tested for growth inhibitory activity against Candida albicans using computer assisted multiple regression analysis. This was in order to explore the selectivity requirements for fun...
A series of 2-substituted phenoxymethyl benzimidazoles and 1-alkyl-2-substituted phenoxymethyl benzimidazoles (R1X 1-4 -R8X 1-4) were prepared. The structures of the benzimidazole derivatives were confirmed on the basis of spectral data. The compounds were screened for their in vitro antibacterial, antifungal, antituberculars activity using bacteri...
Tuberculosis (TB) is a major cause of illness and death worldwide, especially in Asia and Africa. Globally, 9.2 million new cases and 1.7 million deaths from TB occurred in 2006, of which 0.7 million cases and 0.2 million deaths were in HIV-positive people.Still powerful new anti-TB drugs with new mechanisms of action have not been developed in the...
Cyclocondensation of benzofuran chalcones (2) with Norfloxacin and Mefenamic acid hydrazides resulted in the formation of benzofuran 2-pyrazolines (3,4). Chalcones (2) were synthesized by Claisen-Schmidt condensation involving treatment of 2-acetyl benzofuran with different aromatic aldehydes. The compounds were evaluated for antitubercular, antimi...
We have described the synthesis of new 1,2,4-triazoles and have evaluated their antimicrobial profile. Antitubercular activity was determined in triplicate using the Lowenstein-Jensen medium. A loopful of Mycobacterium tuberculosis suspension was inoculated on the surface of each Lowenstein-Jensen media containing the test compounds (100, 10 or 1 m...
A series of new 1,3,5-trisubstituted 2-pyrazolines have been synthesized and evaluated for antitubercular, antibacterial and antifungal activity in-vitro. Some of the compounds exhibited antitubercular activity at 1μg/ml concentration level. However, none of the compounds exhibited antibacterial/antifungal activity.