Mahesh AR | M S Ramaiah University of Applied Sciences (original) (raw)

Papers by Mahesh AR

Aurones [2-benzylidine-1-benzofuran-3(2H)-ones] and its derivatives constitute a class of heteroc... more Aurones [2-benzylidine-1-benzofuran-3(2H)-ones] and its derivatives constitute a class of heterocyclic compounds have an extensive applications in drug development containing benzofuranone molecule. Aurones have been isolated from various natural sources and have been reported for their potent Anticancer, antidiabetic, anti-inflammatory activities. Alkylating neoplastic agents such as nitrogen mustards interfere with cellular proliferation. Based on the above consideration we have synthesized around eight benzofuran derivatives containing nitrogen mustard and screened for their In-Vitro Cytotoxic activity. Synthesis of N-N {Bis(2'-chloroethylamino)-Nitroso}-2-benzylidene-1-benzofuran was carried out by reacting O-hydroxy acetophenones with substituted benzaldehyde in presence of aqueous NaOH and was neutralized with 1N HCl to get chalcones, which was further refluxed with a mixture of CuBr 2 in DMSO and the reaction mixture was cooled, poured on ice-cold water to get aurones. Aurones was refluxed with hydroxylamine hydrochloride, sodium acetate trihydrate for 48 hours to get oxime, further treating with chloroacetyl chloride gave N-chloroacetyl-nitroso-2-benzylidene-1-benzofuran-3(2H)-one. This was further treated with Bis (2-chloroethyl) amine in pyridine to yield N-N {Bis(2'-chloroethylamino)-Nitroso}-2-benzylidene-1-benzofuran. The newly synthesized benzofuran derivatives were screened for their In-Vitro Cytotoxic activity against Breast cancer cell line. All the synthesized eight compounds showed mild to low cytotoxic activity.

Aurone is a heterocyclic benzofuranone molecule which is isolated from a natural source, aurone a... more Aurone is a heterocyclic benzofuranone molecule which is isolated from a natural source, aurone and its derivatives add a new dimension to drug discovery and development due to its anticancer, antidiabetic, antiviral, anti-malarial, anti-hepatitis, antihormonal, anti-diabetic, anti-obesity, anti-cholinesterase inhibitor and anti-inflammatory activity, which inspired chemist due to its incomparable properties. In this review we have compiled various pharmacological activity of aurone molecule in an effort to pave a way for development in this area of research.

Method 2: Few milligram of Copper (II) Bromide in Dimethyl sulfoxide and 2-hydroxychalcones is re... more Method 2: Few milligram of Copper (II) Bromide in Dimethyl sulfoxide and 2-hydroxychalcones is reflexed SJIF Impact Factor 2.062 ABSTRACT Aurones and its derivatives constitute a class of heterocyclic compounds which add a new dimension in drug development containing benzofuranone molecule. Aurones have been isolated from various natural sources and have been reported for their potent Anticancer, antidiabetic, anti-inflammatory activities Chemists were inspired by the unique properties of Aurones to develop various derivatives of aurone and assess their potential biological pertinence. In this review we have compiled and discussed several methods by which aurones and its derivatives can be chemically synthesized, in an effort to pave the way for a medicinal chemist for a comprehensive and target oriented information for development in this promising area of research.

Ficus is a genus of about 850 species of woody trees, shrubs, vines, epiphytes and hemiepiphytes ... more Ficus is a genus of about 850 species of woody trees, shrubs, vines, epiphytes and hemiepiphytes in the family Moraceae. which is also referred to as fig family which are an integral parts of common Indian diet and are freely available in Indian and adjoining continents. Its medicinal importance has also been mentioned in Ayurveda. Collectively known as fig trees or figs, Fig trees have profoundly influenced culture through several religious traditions. figs are important in Buddhism, Hinduism and Jainism. Among the more famous species are Ficus Benghalensis(Indian banyan or the wish fulfilling tree), ficus religiosa (Bodhi tree or sacred tree), ficus racemosa (goolar fig), ficus carica (common fig). The plants are reported to possess antidiabetic, antidiarrhea, antiepilepsy, anti-inflammatory, ear drop properties. The above metioned plants are an important source of compounds like phenols,

Tribal community are using their traditional knowledge system to cure various diseases. They use ... more Tribal community are using their traditional knowledge system to cure various diseases. They use natural source of drugs through trial and error method and the process is experienced over hundreds of years, this says that the medicinal plant shave been in the focus as lifesaving drugs right from the beginning of the human civilization. Citrus sinensisis one such drug which has a strong research support of its use in biological activities such as antityphoid activity, antidiabetic activity, anticarcinogenic activity, antiproliferative activity, antioxidant activity, antibiotic activity, antifungal activity, antioxidant, anxiolytic effect, anti-lipidperoxidative effect, anti-inflammatory, lipoxygenase inhibitor, amylase inhibition, urease inhibition, Anti-hyperthyroidism, trypsin inhibition, inotropic effect, anti-arthritic, cardio-protective, anti-asthmatic, depression treatment, hepatotoxicity treatment, thrombosis treatment and rheumatic disease treatment. Citrus sinensisis a well-known herb which is found in the tropical and subtropical regions of India, China, Northern Australia and New Caledonia. Since Citrus sinensis has shown a wide variety of medicinal importance, we have here tested antitubercular activity by using Micro-plate Alamar Blue Assay (MABA) method.The dried peels of Citrus sinensiswereinitiallyde-fated and then were subjected to the methanolic extraction. The methanolic extract obtained was dissolved in various solvents such as water, methanol, ethanol, chloroform, diethyl ether separately and were subjected to evaluation of antitubercular activity against Mycobacterium tuberculosis by Microplate Alamar Blue Assay (MABA) method. The results concluded that the extract dissolved in water as solvent showed significant activity at 50μgm/ml.

We have chosen molecule having moieties possessing antimicrobial activity, one of which is hydraz... more We have chosen molecule having moieties possessing antimicrobial activity, one of which is hydrazide skeleton, which is reported to have antibacterial and antitubercular activity and other morpholine ring attached to 4 th position of the benzene ring which possess the antibacterial, antimycobacterial and antifungal activity. Present work deals with the preparation of morpholie and 4-chloro-benzonitrile on reflux gives 4-(morpholine-4-yl) benzonitrile. this upon treating with sodium hydroxide gives 4-(morpholin-4-yl)benzoic acid. Then this upon treating with thionyl chloride gives 4-(morpholin-4-yl) benzoyl chloride. This on further treatment with hydrazine-hydrate gives 4-(morpholin-4-yl) benzohydrazide then it is treated with various substituted to form morpholine derivatives.Hydrazides were synthesized so as to increase intracellular concentration and so as to try and decrease the resistant developed due to decrease intracellular concentration of the drug. These synthesized compounds were subjected to preliminary biological evaluation. The characterization of synthesized compounds was identified on the basis of IR, 1 HNMR, Mass spectroscopy. The compounds have been evaluated for antimicrobial activity.

Ethyl piperazine is treated with 4-chloro nitrobenzene in presence of anhydrous potassium carbona... more Ethyl piperazine is treated with 4-chloro nitrobenzene in presence of anhydrous potassium carbonate and methanol is used as a solvent forms 1 ethyl-4-[4-nitrophenyl] piperazine, then it is treated with iron dust in presence of hydrochloric acid and neutralized with sodium carbonate to form the 4-[4-ethyl piperazine-1-yl] anilline, it is reacted with n-chloro acetyl aryl amine in presence of anhydrous potassium carbonate forms the final product 1-[2-(aryl amino-2-oxoethyl)-amino-4-(n-ethyl piperazine)] benzene derivatives were synthesized, the synthesized compounds were screened for their antibacterial activates against s. aures and e.coli by cup plates method. From screening results of some compounds found highly active against both gram – positive and gram – negative bacteria while other compounds possess moderate activity.

Flavonoids(Rotenoids) present in Boerhaavia diffusa is known for its different biological activit... more Flavonoids(Rotenoids) present in Boerhaavia diffusa is known for its different biological activities such as antioxidant, anti-diabetic, anti-stress, anticonvulsant, antibacterial, hypoglycemic, anti-nociceptive, hepato-protective, anti-proliferative and anti-estrogenic, anti-inflammatory. The following work constitutes the enrichment of iso-flavonoids present in the methanolic extract of Boerhaavia diffusa by partition technique using various solvents such as acetone, water, Butanol, ethyl acetate, hexane, chloroform and methanol. Enrichment was determined by Thin Layer Chromatography and HPLC and the presence of flavonoids was confirmed with Shinoda test, lead acetate test and sodium hydroxide test.

Lantana camara belongs to the family Verbenaceae, is an evergreen plant found throughout India. T... more Lantana camara belongs to the family Verbenaceae, is an evergreen plant found throughout India. Traditionally it has been used in treating various ailments and they were supported by scientific data's. Various literatures have reported the phytoconstituents present in t Lantana camara. In our present study we have selected to isolate compound from toluene extract of the aerial parts and analyze the major constituent present in these extract by developing a novel HPLC method. The dried aerial parts were subjected for extraction with n-hexane and toluene in soxhlet apparatus. The dried toluene extract were subjected for column chromatography for the isolation of phytoconstituent. The structural analysis of the isolated compound (LC carried out by IR, NMR, MS and qualitative estimation by HPLC method using C-18 column with SPD-M20A prominence diode array detector was used. From the retention time and percentage yield (1.02%w/w) of the isolated compound obtained from toluene extract, it was concluded compound LC-01(pentacyclic triterpenoid) were found as major chemical constituent which have structural similarities with the reference standard (Lupeol). belongs to the family Verbenaceae, is an evergreen plant found throughout India. Traditionally it has been used in treating various ailments and they were supported by scientific data's. Various literatures have reported the phytoconstituents present in the aerial parts of. In our present study we have selected to isolate compound from toluene extract of the aerial parts and analyze the major constituent present in these extract by developing a novel HPLC method. The dried aerial parts were hexane and toluene in soxhlet apparatus. The dried toluene extract were subjected for column chromatography for the isolation of phytoconstituent. The structural analysis of the isolated compound (LC-01) was R, NMR, MS and qualitative estimation by HPLC M20A prominence diode array detector was used. From the retention time and percentage yield (1.02%w/w) of the isolated compound it was concluded that 01(pentacyclic triterpenoid) were found as have structural similarities

Boerhaavia diffusa is one of the renowned medicinal plants used to treat large number of human ai... more Boerhaavia diffusa is one of the renowned medicinal plants used to treat large number of human ailments as mentioned in Ayurveda, Charaka Samhita, and Sushrita Samhita. The Plant in whole or its peculiar parts (Aerial parts and Roots) have a numerous medicinal properties and are used by endemic and tribal people in India and Unani medicine in Arab countries to show Anti-bacterial, Anti-nociceptive, hepato-protective, hypo-glycemic, anti-proliferative, anti-estrogenic, anti-inflammatory, anti-convulsant, anti-stress and anti-metastatic activities and also in treatment of stress, dyspepsia, abdominal pain, inflammation, jaundice. Various phytochemical, pharmacological, experimental and clinical investigations are done on Boerhaavia diffusa by many scientist, researchers etc., to clearly understand the ancient Ayurvedic, Endemic and tribal usage of Boerhaavia diffusa. This paper includes the evidence-based overview of pharmacological and phytochemical properties of the aerial parts and the roots of Boerhaavia diffusa, which may be helpful to establish a standard natural drug for further research.