Jai Narain Vishwakarma - Academia.edu (original) (raw)
Papers by Jai Narain Vishwakarma
Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry, Apr 1, 2006
A facile one-pot synthetic route to substituted fused tetrahydropyrimidines.
Current Chemistry Letters, 2018
A clean and efficient, mediated in water and assisted by ultrasound method for the synthesis of a... more A clean and efficient, mediated in water and assisted by ultrasound method for the synthesis of a series of N-substituted 1-amino-3-ferrocenyl-3-oxoprop-1-enes starting from acetyl ferrocene was developed. Our approach offers shortening of the reaction time under the mild reaction conditions and easy work up procedure.
Chemischer Informationsdienst, Aug 23, 1983
ChemInform, Aug 20, 2010
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Chemischer Informationsdienst, Nov 19, 1985
Chemischer Informationsdienst, Nov 19, 1985
Synthesis, 1984
© Georg Thieme Verlag, Rüdigerstr. 14, 70469 Stuttgart, Germany. All rights reserved. This journa... more © Georg Thieme Verlag, Rüdigerstr. 14, 70469 Stuttgart, Germany. All rights reserved. This journal, including all individual contributions and illustrations published therein, is legally protected by copyright for the duration of the copyright period. Any use, exploitation or ...
Anti-cancer drug design
ABSTRACT
Current Chemistry Letters, 2016
1H-indol-3-yl)-1-(4-methylphenyl)propenone has been prepared, and its crystal structure (C19H17NO... more 1H-indol-3-yl)-1-(4-methylphenyl)propenone has been prepared, and its crystal structure (C19H17NO, Mr = 275.34) has been determined by single-crystal X-ray diffraction analysis. The title compound crystallized in the triclinic system with space group P1 and unit cell parameters: a = 9.4014 (5) Å, b = 9.8347 (4) Å, c = 10.0318 (5) Å, α = 62.821 (3)°, β = 85.539 (3)°, γ = 65.262 (3)° and Z = 2. The final reliability index is 0.053 for the 2807 observed reflections. The title compound is linked through N-H•••O hydrogen bonds.
Monatshefte für Chemie - Chemical Monthly
In the present study, a novel series of side chain-modified quinoline β-enaminones were synthesiz... more In the present study, a novel series of side chain-modified quinoline β-enaminones were synthesized in good-to-excellent yields. The structures of all the synthesized compounds have been established with the help of spectral and analytical data and also by X-ray crystallography. All the compounds were screened for their potential in vitro anti-malarial activity against chloroquine resistant strain K1 and chloroquine sensitive strain 3D7. The compounds were also evaluated for their in vitro microfilaricidal and adulticidal effect against B. malayi microfilariae and adult worms using ivermectin as positive control. The cytotoxicity of the compounds was checked against Vero cell line and all the compounds were found to be non-toxic. The compounds showed low antimalarial activities against both the plasmodial strains compared to the standard drug chloroquine. However, four of the evaluated compounds have shown significant in vitro adulticidal activity and their percentage inhibition were found to be 68, 55, 64, and 66, respectively. Two of these were selected for further preliminary in vivo activity studies.
![Research paper thumbnail of Efficient, environment friendly and regioselective synthetic strategy for 2/3-substituted-8,8-dimethyl-8,9-dihydropyrazolo[1,5-a]quinazolin-6(7H)-ones and their structure elucidation](https://attachments.academia-assets.com/92890223/thumbnails/1.jpg)
](European Journal of Chemistry, Mar 31, 2022
An efficient and regioselective synthetic reaction friendly to the environment has been described... more An efficient and regioselective synthetic reaction friendly to the environment has been described to synthesize various derivatives of pyrazolo[1,5-a]quinozolinone. Condensation of aminopyrazole (4a-m) with formylated dimedone (3) in the presence of KHSO4, under ultrasonic irradiation furnished 2/3-substituted 8,8-dimethyl-8,9-dihydropyrazolo[1,5a]quinazolin-6(7H)-one (6a-m). This is a clean reaction, giving excellent yields with short reaction time. The structures were elucidated with the help of spectral and analytical data. X-ray crystallographic studies of a model compound 6a ascertained its structural configuration, crystal data for C12H12BrN3O (M =294.152 g/mol): Triclinic, space group P-1 (no. 2), a = 5.872(4) Å, b = 10.870(8) Å, c = 19.523(15) Å, α = 90.013(10)°, β = 90.009(11)°, γ = 93.838(11)°, V = 1243.3(16) Å 3 , Z = 4, T = 296.15 K, μ(Mo Kα) = 3.293 mm-1 , Dcalc = 1.571 g/cm 3 , 37271 reflections measured (4.18° ≤ 2Θ ≤ 52.7°), 5073 unique (Rint = 0.2404, Rsigma = 0.2366) which were used in all calculations. The final R1 was 0.0596 (I≥2σ(I)) and wR2 was 0.1759 (all data).
Russian Journal of Organic Chemistry, 2022
Abstract A series of novel 3-(adamantan-1-yl)-1-(alkyl, aryl, aralkyl, hydroxyethyl)-7,7-dimethyl... more Abstract A series of novel 3-(adamantan-1-yl)-1-(alkyl, aryl, aralkyl, hydroxyethyl)-7,7-dimethyl-1,2,3,4,5,6,7,8-octahydroquinazolin-5-ones have been synthesised by the reaction of 3-(alkyl/aralkyl/aryl)amino-5,5-dimethylcyclohex-2-en-1-ones with adamantan-1-amine and formaldehyde in refluxing methanol. The initial enaminones were obtained by the condensation of dimedone with primary amines under microwave irradiation. The synthesized compounds were characterized by IR, 1 H and 13 C NMR, and mass spectra, and X-ray analysis of 3-(adamantan-1-yl)-1-(4-bromophenyl)-7,7-dimethyl-1,2,3,4,5,6,7,8-octahydroquinazolin5-one was performed for the final structure assignment. The synthesized compounds were tested for their antibacterial activity.
An entry from the Cambridge Structural Database, the world's repository for small molecule cr... more An entry from the Cambridge Structural Database, the world's repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.
An entry from the Cambridge Structural Database, the world's repository for small molecule cr... more An entry from the Cambridge Structural Database, the world's repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.
Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry, Apr 1, 2006
A facile one-pot synthetic route to substituted fused tetrahydropyrimidines.
Current Chemistry Letters, 2018
A clean and efficient, mediated in water and assisted by ultrasound method for the synthesis of a... more A clean and efficient, mediated in water and assisted by ultrasound method for the synthesis of a series of N-substituted 1-amino-3-ferrocenyl-3-oxoprop-1-enes starting from acetyl ferrocene was developed. Our approach offers shortening of the reaction time under the mild reaction conditions and easy work up procedure.
Chemischer Informationsdienst, Aug 23, 1983
ChemInform, Aug 20, 2010
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Chemischer Informationsdienst, Nov 19, 1985
Chemischer Informationsdienst, Nov 19, 1985
Synthesis, 1984
© Georg Thieme Verlag, Rüdigerstr. 14, 70469 Stuttgart, Germany. All rights reserved. This journa... more © Georg Thieme Verlag, Rüdigerstr. 14, 70469 Stuttgart, Germany. All rights reserved. This journal, including all individual contributions and illustrations published therein, is legally protected by copyright for the duration of the copyright period. Any use, exploitation or ...
Anti-cancer drug design
ABSTRACT
Current Chemistry Letters, 2016
1H-indol-3-yl)-1-(4-methylphenyl)propenone has been prepared, and its crystal structure (C19H17NO... more 1H-indol-3-yl)-1-(4-methylphenyl)propenone has been prepared, and its crystal structure (C19H17NO, Mr = 275.34) has been determined by single-crystal X-ray diffraction analysis. The title compound crystallized in the triclinic system with space group P1 and unit cell parameters: a = 9.4014 (5) Å, b = 9.8347 (4) Å, c = 10.0318 (5) Å, α = 62.821 (3)°, β = 85.539 (3)°, γ = 65.262 (3)° and Z = 2. The final reliability index is 0.053 for the 2807 observed reflections. The title compound is linked through N-H•••O hydrogen bonds.
Monatshefte für Chemie - Chemical Monthly
In the present study, a novel series of side chain-modified quinoline β-enaminones were synthesiz... more In the present study, a novel series of side chain-modified quinoline β-enaminones were synthesized in good-to-excellent yields. The structures of all the synthesized compounds have been established with the help of spectral and analytical data and also by X-ray crystallography. All the compounds were screened for their potential in vitro anti-malarial activity against chloroquine resistant strain K1 and chloroquine sensitive strain 3D7. The compounds were also evaluated for their in vitro microfilaricidal and adulticidal effect against B. malayi microfilariae and adult worms using ivermectin as positive control. The cytotoxicity of the compounds was checked against Vero cell line and all the compounds were found to be non-toxic. The compounds showed low antimalarial activities against both the plasmodial strains compared to the standard drug chloroquine. However, four of the evaluated compounds have shown significant in vitro adulticidal activity and their percentage inhibition were found to be 68, 55, 64, and 66, respectively. Two of these were selected for further preliminary in vivo activity studies.
European Journal of Chemistry, Mar 31, 2022
An efficient and regioselective synthetic reaction friendly to the environment has been described... more An efficient and regioselective synthetic reaction friendly to the environment has been described to synthesize various derivatives of pyrazolo[1,5-a]quinozolinone. Condensation of aminopyrazole (4a-m) with formylated dimedone (3) in the presence of KHSO4, under ultrasonic irradiation furnished 2/3-substituted 8,8-dimethyl-8,9-dihydropyrazolo[1,5a]quinazolin-6(7H)-one (6a-m). This is a clean reaction, giving excellent yields with short reaction time. The structures were elucidated with the help of spectral and analytical data. X-ray crystallographic studies of a model compound 6a ascertained its structural configuration, crystal data for C12H12BrN3O (M =294.152 g/mol): Triclinic, space group P-1 (no. 2), a = 5.872(4) Å, b = 10.870(8) Å, c = 19.523(15) Å, α = 90.013(10)°, β = 90.009(11)°, γ = 93.838(11)°, V = 1243.3(16) Å 3 , Z = 4, T = 296.15 K, μ(Mo Kα) = 3.293 mm-1 , Dcalc = 1.571 g/cm 3 , 37271 reflections measured (4.18° ≤ 2Θ ≤ 52.7°), 5073 unique (Rint = 0.2404, Rsigma = 0.2366) which were used in all calculations. The final R1 was 0.0596 (I≥2σ(I)) and wR2 was 0.1759 (all data).
Russian Journal of Organic Chemistry, 2022
Abstract A series of novel 3-(adamantan-1-yl)-1-(alkyl, aryl, aralkyl, hydroxyethyl)-7,7-dimethyl... more Abstract A series of novel 3-(adamantan-1-yl)-1-(alkyl, aryl, aralkyl, hydroxyethyl)-7,7-dimethyl-1,2,3,4,5,6,7,8-octahydroquinazolin-5-ones have been synthesised by the reaction of 3-(alkyl/aralkyl/aryl)amino-5,5-dimethylcyclohex-2-en-1-ones with adamantan-1-amine and formaldehyde in refluxing methanol. The initial enaminones were obtained by the condensation of dimedone with primary amines under microwave irradiation. The synthesized compounds were characterized by IR, 1 H and 13 C NMR, and mass spectra, and X-ray analysis of 3-(adamantan-1-yl)-1-(4-bromophenyl)-7,7-dimethyl-1,2,3,4,5,6,7,8-octahydroquinazolin5-one was performed for the final structure assignment. The synthesized compounds were tested for their antibacterial activity.
An entry from the Cambridge Structural Database, the world's repository for small molecule cr... more An entry from the Cambridge Structural Database, the world's repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.
An entry from the Cambridge Structural Database, the world's repository for small molecule cr... more An entry from the Cambridge Structural Database, the world's repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.