The Experts below are selected from a list of 198 Experts worldwide ranked by ideXlab platform
Chiranjib Pal - One of the best experts on this subject based on the ideXlab platform.
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synthesis and biological evaluation of polyhydroxylated oxindole derivatives as potential Antileishmanial Agent
Bioorganic & Medicinal Chemistry Letters, 2018Co-Authors: Debarati Mukherjee, Abhishek Pal, Somaditya Dey, Chiranjib Pal, Saurav Chatterjee, Biswajyoti Sarkar, Susanta AdhikariAbstract:The devastating appearance of numerous drug-unresponsive strains of Leishmania donovani and severe toxic side effects of conventional Antileishmanial therapy necessitates the search for novel leads, to treat visceral leishmaniasis efficiently. The current study deals with the synthesis and biological evaluation of a unique C-5 functionalized oxindole based polyphenol to ascertain its activities against L. donovani infection, in vitro. The polyhydroxylated oxindole derivative (1) was generated by coupling styrene derivatives with 5-bromo bis-arylidene oxindole using Heck coupling reaction. The synthesized molecule 1 was tested for its Antileishmanial activity using both promastigote and amastigote stages of L. donovani. Molecule 1 showed promising anti-promastigote and anti-amastigote activities with IC50 values 15 µM and 1 µM, respectively, with no cytotoxicity towards host splenocytes. The results revealed that this compound induced parasite death by promoting oxidative stress, thereby triggering apoptosis.
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synthesis and biological evaluation of ferrocenylquinoline as a potential Antileishmanial Agent
ChemMedChem, 2015Co-Authors: Debarati Mukherjee, Abhishek Pal, Somaditya Dey, Supratim Mandal, Chiranjib Pal, Susanta AdhikariAbstract:The emergence of resistance against Antileishmanial drugs in current use necessitates the search for new classes of Antileishmanial compounds. Herein we report the design, synthesis, and evaluation of a novel ferrocenylquinoline for activity against Leishmania donovani. 7-Chloro-N-[2-(1H-5-ferrocenyl-1,2,3-triazol-1-yl)ethyl]quinolin-4-amine (1) was generated by coupling an iron(II) ethynylferrocene species with 4-(2-ethylazido)amino-7-chloroquinoline using click chemistry. The synthesized compound 1 was tested for its Antileishmanial activity using both promastigote and amastigote stages of L. donovani. Compound 1 showed promising anti-promastigote activity, with an IC50 value of 15.26 μM and no cytotoxicity toward host splenocytes. From the battery of tests conducted in this study, it appears that this compound induces parasite death by promoting oxidative stress and depolarizing the mitochondrial membrane potential, thereby triggering apoptosis. These results suggest that ferrocenylquinoline 1 is a suitable lead for the development of new Antileishmanial drugs.
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a one pot rearrangement of 2 n alkyl n aryl aminochromone 3 carbaldehyde to n alkyl 3 salicyloyl 2 quinolone an Antileishmanial Agent
ChemInform, 2012Co-Authors: Sourav Maiti, Chiranjib Pal, Suvadip Mallick, Suman Kalyan Panja, Chandrakanta BandyopadhyayAbstract:Substrates of type (I) rearrange on heating in wet acetic acid to yield quinolones (II) (15 examples).
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synthesis of a novel quinoline derivative 2 2 methylquinolin 4 ylamino n phenylacetamide a potential Antileishmanial Agent
ChemInform, 2002Co-Authors: Niranjan P Sahu, Chiranjib Pal, Nirup B Mandal, Sukdeb Banerjee, Mausumi Raha, Ashis Kundu, Anirban Basu, Monidipa Ghosh, Keshab Chandra Roy, Santu BandyopadhyayAbstract:Some novel quinoline derivatives were prepared and tested for Antileishmanial activity. 2-(2-Methylquinolin-4-ylamino)-N-phenylacetamide (2) was found to be significantly more active than the standard Antileishmanial drug sodium antimony gluconate (SAG) in reducing the parasite load both in the spleen and liver at a much lower concentration in hamster models. The results suggest that the compound could be exploited as an Antileishmanial drug.
Yusuke Wataya - One of the best experts on this subject based on the ideXlab platform.
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3 deoxy 3 fluoroinosine as a potent Antileishmanial Agent the metabolism and selective cytotoxic effect of 3 deoxy 3 fluoroinosine against leishmania tropica and l donovani in vitro and in vivo
Parasitology Research, 1995Co-Authors: Il Shik Shin, Hisato Tanifuji, Yasuda Arata, Yoshitomi Morizawa, Toshiaki Nakayama, Yusuke WatayaAbstract:We studied the Antileishmanial activity of 3′-deoxy-3′-fluoroinosine (3′-FI) againstLeishmania tropica andL. donovani. In in vitro cultivation, the EC50 values (the concentration of drug necessary to inhibit the growth rate of cells to 50% of the control value) obtained for 3′-FI against the promastigotes ofL. tropica andL. donovani were 2.3×10−7 and 1.0×10−6M, respectively. It was less toxic toward mouse mammary-tumor FM3A cells, a model host; the EC50 value was 1.9×10−4M. Leishmania promastigote metabolized 3′-FI to 3′-deoxy-3′-fluoroadenosine 5′-triphosphate (3′-FATP) but FM3A cells did not. 3′-FI was effective againstL. donovani amastigotes in J774.1 cells in an in vitro cultivation system under conditions similar to those used in the in vivo assay. 3′-FI (50 mg/kg, given i.v.)showed a cytotoxic effect against the amastigotes ofL. donovani in mice.
Mukul K Basu - One of the best experts on this subject based on the ideXlab platform.
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delivery in vivo of 14 deoxy 11 oxoandrographolide an Antileishmanial Agent by different drug carriers
Indian Journal of Biochemistry & Biophysics, 2003Co-Authors: Sanchaita Lala, A K Nandy, S B Mahato, Mukul K BasuAbstract:An Antileishmanial compound, 14-deoxy-11-oxo-andrographolide, a derivative of andrographlide, isolated from the Indian medicinal plant Andrographis paniculata was evaluated for efficacy in free form and in different vesicular delivery modes on hamster model of Leishmaniasis. The subcutaneous injection of free drug reduced the spleen parasite load by 39%, whereas for drug incorporated in liposomes, niosomes and microspheres, reductions in the parasite load were 78%, 91% and 59%, respectively. Moreover, the drug in various delivery modes, particularly in liposomal and niosomal forms, showed no apparent immediate toxicity. Although an inverse linear relationship between the size of carriers and per cent efficacy in reduction of spleen parasite load was established, involvement of other factors such as drug release profiles or rates remains an open question. Because of greater efficacy and lesser toxicity, liposomal, niosomal and possibly microsphere-incorporated 14-deoxy-11-oxo-andrographolide might have clinical application to combat visceral Leishmaniasis.
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phospholipid microspheres a novel delivery mode for targeting Antileishmanial Agent in experimental leishmaniasis
Journal of Drug Targeting, 2003Co-Authors: S Medda, Parasuraman Jaisankar, R K Manna, Bikash Pal, V S Giri, Mukul K BasuAbstract:Novel phospholipid microspheres were prepared from polylactic-co-glycolic acid (PLGA) and phosphatidyl ethanol amine in the molar ratio 1:71, to deliver drugs to macrophages in experimental leishmaniasis. Liposomes, well known as drug carrier systems, made from phosphatidylethanolamine, cholesterol and dicetyl phosphate in the molar ratio 7:2:1, were used as control, in order to compare the efficacies of the two carriers. As such, the membrane fluidity of the two carriers was kept at comparable levels by adjusting chemical composition. Moreover, because of the presence of mannosyl fucosyl receptors on macrophages, attempts were made to target an optically active synthetic compound dihydroindolo [2,3-a] indolizine, an Antileishmanial Agent, intercalated in both mannose-grafted liposomes and mannose-grafted microspheres. When tested for efficacy in lowering parasite load in the spleen, as well as in reducing the hepatic and renal changes associated with infection, the drug intercalated mannose-grafted microspheres were found to be the most active in comparison to drug intercalated liposomes or to the free drug. Thus, mannose-grafted microspheres may have possible application in the clinics not only in visceral leishmaniasis, but also in other macrophage-associated disorders.
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quercetin critical evaluation as an Antileishmanial Agent in vivo in hamsters using different vesicular delivery modes
Journal of Drug Targeting, 2002Co-Authors: Somenath Sarkar, Suparna Mandal, J Sinha, Sibabrata Mukhopadhyay, Nirmalendu Das, Mukul K BasuAbstract:Chemotherapy is still a major challenge for in vivo drug targeting to macrophages. Toxicity remains the major obstacle for the most potent drugs already known in the therapy of leishmaniasis. Thus, new drugs and new delivery systems are sought. By using different vesicular delivery modes e.g. liposomes, niosomes, microspheres and nanoparticles, attempts have been made to deliver an indigenous Antileishmanial compound, quercetin, to treat experimental leishmaniasis in the hamster model so as to increase its efficacy as well as to reduce the toxicity. At equivalent quercetin concentration, the nanocapsulated quercetin was found to be the most potent in reducing the parasite burden in the spleen as well as in reducing hepatotoxcity and renaltoxicity compared to free drug or drug in other vesicular forms. An inverse relationship between the efficacy and the size of the vesicles was established. Such a drug vehicle formulation especially in the nanocapsulated form may be considered for clinical trials.
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evaluation of the in vivo activity and toxicity of amarogentin an Antileishmanial Agent in both liposomal and niosomal forms
Journal of Antimicrobial Chemotherapy, 1999Co-Authors: S Medda, Sibabrata Mukhopadhyay, Mukul K BasuAbstract:The Antileishmanial property of amarogentin, a secoiridoid glycoside isolated from the Indian medicinal plant Swertia chirata, was examined in a hamster model of experimental leishmaniasis. The therapeutic efficacy of amarogentin was evaluated in free and two different vesicular forms, liposomes and niosomes. The amarogentin in both liposomal and niosomal forms was found to be a more active leishmanicidal Agent than the free amarogentin; and the niosomal form was found to be more efficacious than the liposomal form at the same membrane microviscosity level. Toxicity studies involving blood pathology, histological staining of tissues and specific enzyme levels related to normal liver function showed no toxicity. Hence, amarogentin incorporated in liposomes or niosomes may have clinical application in the treatment of leishmaniasis.
Il Shik Shin - One of the best experts on this subject based on the ideXlab platform.
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3 deoxy 3 fluoroinosine as a potent Antileishmanial Agent the metabolism and selective cytotoxic effect of 3 deoxy 3 fluoroinosine against leishmania tropica and l donovani in vitro and in vivo
Parasitology Research, 1995Co-Authors: Il Shik Shin, Hisato Tanifuji, Yasuda Arata, Yoshitomi Morizawa, Toshiaki Nakayama, Yusuke WatayaAbstract:We studied the Antileishmanial activity of 3′-deoxy-3′-fluoroinosine (3′-FI) againstLeishmania tropica andL. donovani. In in vitro cultivation, the EC50 values (the concentration of drug necessary to inhibit the growth rate of cells to 50% of the control value) obtained for 3′-FI against the promastigotes ofL. tropica andL. donovani were 2.3×10−7 and 1.0×10−6M, respectively. It was less toxic toward mouse mammary-tumor FM3A cells, a model host; the EC50 value was 1.9×10−4M. Leishmania promastigote metabolized 3′-FI to 3′-deoxy-3′-fluoroadenosine 5′-triphosphate (3′-FATP) but FM3A cells did not. 3′-FI was effective againstL. donovani amastigotes in J774.1 cells in an in vitro cultivation system under conditions similar to those used in the in vivo assay. 3′-FI (50 mg/kg, given i.v.)showed a cytotoxic effect against the amastigotes ofL. donovani in mice.
Susanta Adhikari - One of the best experts on this subject based on the ideXlab platform.
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synthesis and biological evaluation of polyhydroxylated oxindole derivatives as potential Antileishmanial Agent
Bioorganic & Medicinal Chemistry Letters, 2018Co-Authors: Debarati Mukherjee, Abhishek Pal, Somaditya Dey, Chiranjib Pal, Saurav Chatterjee, Biswajyoti Sarkar, Susanta AdhikariAbstract:The devastating appearance of numerous drug-unresponsive strains of Leishmania donovani and severe toxic side effects of conventional Antileishmanial therapy necessitates the search for novel leads, to treat visceral leishmaniasis efficiently. The current study deals with the synthesis and biological evaluation of a unique C-5 functionalized oxindole based polyphenol to ascertain its activities against L. donovani infection, in vitro. The polyhydroxylated oxindole derivative (1) was generated by coupling styrene derivatives with 5-bromo bis-arylidene oxindole using Heck coupling reaction. The synthesized molecule 1 was tested for its Antileishmanial activity using both promastigote and amastigote stages of L. donovani. Molecule 1 showed promising anti-promastigote and anti-amastigote activities with IC50 values 15 µM and 1 µM, respectively, with no cytotoxicity towards host splenocytes. The results revealed that this compound induced parasite death by promoting oxidative stress, thereby triggering apoptosis.
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synthesis and biological evaluation of ferrocenylquinoline as a potential Antileishmanial Agent
ChemMedChem, 2015Co-Authors: Debarati Mukherjee, Abhishek Pal, Somaditya Dey, Supratim Mandal, Chiranjib Pal, Susanta AdhikariAbstract:The emergence of resistance against Antileishmanial drugs in current use necessitates the search for new classes of Antileishmanial compounds. Herein we report the design, synthesis, and evaluation of a novel ferrocenylquinoline for activity against Leishmania donovani. 7-Chloro-N-[2-(1H-5-ferrocenyl-1,2,3-triazol-1-yl)ethyl]quinolin-4-amine (1) was generated by coupling an iron(II) ethynylferrocene species with 4-(2-ethylazido)amino-7-chloroquinoline using click chemistry. The synthesized compound 1 was tested for its Antileishmanial activity using both promastigote and amastigote stages of L. donovani. Compound 1 showed promising anti-promastigote activity, with an IC50 value of 15.26 μM and no cytotoxicity toward host splenocytes. From the battery of tests conducted in this study, it appears that this compound induces parasite death by promoting oxidative stress and depolarizing the mitochondrial membrane potential, thereby triggering apoptosis. These results suggest that ferrocenylquinoline 1 is a suitable lead for the development of new Antileishmanial drugs.