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Papers by Diptendu Goswami
OBM Integrative and Complementary Medicine
Curcumin, the yellow principle of the Indian Turmeric, ‘Haldi’ has recently attracted renewed int... more Curcumin, the yellow principle of the Indian Turmeric, ‘Haldi’ has recently attracted renewed interest in the field of experimental medicine with pleiotropic activity. This review has emphasized three pharmaceutical studies of interest: the pharmacokinetics, pharmacology, and pharmacodynamics of curcumin. In this review, we attempted to review the general pharmacokinetics profile, pharmacokinetic interactions, and pharmacokinetic-pharmacodynamic interactions of curcumin and its formulations. Different species of turmeric in India, as well as their cultivars, different forms of curcumin, and harvesting methods have also been discussed. Furthermore, pharmacokinetic studies of the interaction of curcumin and its different formulations with efflux transporters such as P-glycoprotein, ABC-transporter protein, multidrug-resistant protein, and cytochrome p450 metabolism enzymes have been broadly explained following data from preclinical and clinical trials reported in the literature. A few...
120-123As a part of a composite programme of rational drug design (RDD)1, we had synthesized some... more 120-123As a part of a composite programme of rational drug design (RDD)1, we had synthesized some substituted benzene sulphonyl glutamines and evaluated their inhibitory activities against Ehrlich Ascites Carcinoma (EAC) cell line in Swiss albino mice. Quantitative structure activity relationship (QSAR) studies of these inhibitory activities using Fujita-Ban model as well as Modified Hansch-Fujita model gave excellent correlations (correlation coefficient r = 0.89 and 0.82 respectively). These results could be useful in designing 'lead' compound with potent inhibitory activity on DNA and RNA synthesis and tumour development
An attempt was made to develop a two Dimensional Quantitative Structure-Activity Relationship (2D... more An attempt was made to develop a two Dimensional Quantitative Structure-Activity Relationship (2D-QSAR) and molecular docking studies on a series of quinazolinone derivatives acting as glutamate receptor inhibitors for correlating the chemical composition of quinazolinone analogs and estimation of their anticonvulsant activity using Multiple Linear Regression (MLR) Analysis. New Chemical Entities (NCEs) were designed using results of pharmacophore profiling from known anticonvulsants. Binding affinities of designed NCEs were studied on Glutamate receptor using docking studies and their ADMET properties were also predicted. Finally, most promising compounds were selected from molecular modeling studies. 12 compounds showed significant Glutamate receptor inhibiting activity compared to standard ligand bound with glutamate receptor (PDB: 1GR2). These four basic strategies (pharmacophore mapping, QSAR, docking & ADMET screening) were implemented to evaluate the performance of derivative...
Current Bioactive Compounds, 2019
Background: Epilepsy is one of the most prevalent noncommunicable neurological conditions. More t... more Background: Epilepsy is one of the most prevalent noncommunicable neurological conditions. More than 10 million people in India are afflicted with epilepsy. Treatment available has many detrimental side effects. Up to one-third of epilepsy patients remain resistance to optimum drug treatment. These facts triggered the further scope and search for newer more effective and less toxic anticonvulsants. Methods: Quinazolinone semicarbazone derivatives showing protection in chemoconvulsant induced seizure models (as reported in our previous study) were further screened in MES and scPTZ induced seizure models. Neurotoxicity was determined; quantification of anticonvulsant activity and toxicity was also done. Finally compounds were screened by liver functional test to ascertain the possible hepatotoxicity in the active compounds. Results: Compounds N-1- (menthone) -N- [3-(4-(substituted)-phenyl) -4-oxo- 3,4-dihydroquinazolin- 2-yl] methyl semicarbazone (3A-d-4, 3B-d-4 and 3C-d-4) showed sig...
ChemInform, 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.
Few series of glutamic acid analogs and its cyclised variants were designed, synthesized and char... more Few series of glutamic acid analogs and its cyclised variants were designed, synthesized and characterized by FT-IR, 1 H NMR, Protondecoupled 13 C NMR, MS and elemental analysis. Compounds were tested in vivo for antineoplastic activity in female Swiss albino mice against EAC (Ehrlich Ascites Carcinoma) strain. Cytotoxicity study was carried out on HUVEC and Vero cell lines by MTT assay method. Some promising results are noticed which show that few molecules are having selective inhibitory effect on EAC cell growth and probable antiangiogenic activity but there is no significant toxic effect on normal cell.
Crystal Research and Technology, 2002
The crystal structure and molecular conformation of solvated 1-(4-methoxybenzenesulfonyl)-5-oxopy... more The crystal structure and molecular conformation of solvated 1-(4-methoxybenzenesulfonyl)-5-oxopyrrolidine-2-carboxamide (C 12 H 14 O 5 N 2 S.H 2 O), synthesized and biologically evaluated as a possible antineoplastic agent, have been studied by X-ray analysis and AM1 molecular orbital methods. The compound crystallizes in the monoclinic space group P2 1 , with a = 9.661(4), b = 7.246(3), c = 11.378(5)Å, β = 113.42(2)°, Z= 2. The structure has been solved by direct methods and refined to R = 0.0438 for 1721 observed reflections. The crystal structure consists of an essentially planar methoxyphenyl ring linked to a 2-carboxamide substituted oxo-pyrrolidine moiety via sulfonyl group and a lattice water molecule. The conformational analysis of the title compound investigated by semiempirical quantum mechanical AM1 calculations shows a good agreement with the X-ray structure except a rotation of the carboxamide moiety about the C (oxo-pyrrolidine)-C (carboxamide) bond. In the solid state, the molecules translated in the b-direction are linked by intermolecular N-H⋅⋅⋅O hydrogen bonds to form infinite one-dimensional chain.
OBM Integrative and Complementary Medicine
Curcumin, the yellow principle of the Indian Turmeric, ‘Haldi’ has recently attracted renewed int... more Curcumin, the yellow principle of the Indian Turmeric, ‘Haldi’ has recently attracted renewed interest in the field of experimental medicine with pleiotropic activity. This review has emphasized three pharmaceutical studies of interest: the pharmacokinetics, pharmacology, and pharmacodynamics of curcumin. In this review, we attempted to review the general pharmacokinetics profile, pharmacokinetic interactions, and pharmacokinetic-pharmacodynamic interactions of curcumin and its formulations. Different species of turmeric in India, as well as their cultivars, different forms of curcumin, and harvesting methods have also been discussed. Furthermore, pharmacokinetic studies of the interaction of curcumin and its different formulations with efflux transporters such as P-glycoprotein, ABC-transporter protein, multidrug-resistant protein, and cytochrome p450 metabolism enzymes have been broadly explained following data from preclinical and clinical trials reported in the literature. A few...
120-123As a part of a composite programme of rational drug design (RDD)1, we had synthesized some... more 120-123As a part of a composite programme of rational drug design (RDD)1, we had synthesized some substituted benzene sulphonyl glutamines and evaluated their inhibitory activities against Ehrlich Ascites Carcinoma (EAC) cell line in Swiss albino mice. Quantitative structure activity relationship (QSAR) studies of these inhibitory activities using Fujita-Ban model as well as Modified Hansch-Fujita model gave excellent correlations (correlation coefficient r = 0.89 and 0.82 respectively). These results could be useful in designing 'lead' compound with potent inhibitory activity on DNA and RNA synthesis and tumour development
An attempt was made to develop a two Dimensional Quantitative Structure-Activity Relationship (2D... more An attempt was made to develop a two Dimensional Quantitative Structure-Activity Relationship (2D-QSAR) and molecular docking studies on a series of quinazolinone derivatives acting as glutamate receptor inhibitors for correlating the chemical composition of quinazolinone analogs and estimation of their anticonvulsant activity using Multiple Linear Regression (MLR) Analysis. New Chemical Entities (NCEs) were designed using results of pharmacophore profiling from known anticonvulsants. Binding affinities of designed NCEs were studied on Glutamate receptor using docking studies and their ADMET properties were also predicted. Finally, most promising compounds were selected from molecular modeling studies. 12 compounds showed significant Glutamate receptor inhibiting activity compared to standard ligand bound with glutamate receptor (PDB: 1GR2). These four basic strategies (pharmacophore mapping, QSAR, docking & ADMET screening) were implemented to evaluate the performance of derivative...
Current Bioactive Compounds, 2019
Background: Epilepsy is one of the most prevalent noncommunicable neurological conditions. More t... more Background: Epilepsy is one of the most prevalent noncommunicable neurological conditions. More than 10 million people in India are afflicted with epilepsy. Treatment available has many detrimental side effects. Up to one-third of epilepsy patients remain resistance to optimum drug treatment. These facts triggered the further scope and search for newer more effective and less toxic anticonvulsants. Methods: Quinazolinone semicarbazone derivatives showing protection in chemoconvulsant induced seizure models (as reported in our previous study) were further screened in MES and scPTZ induced seizure models. Neurotoxicity was determined; quantification of anticonvulsant activity and toxicity was also done. Finally compounds were screened by liver functional test to ascertain the possible hepatotoxicity in the active compounds. Results: Compounds N-1- (menthone) -N- [3-(4-(substituted)-phenyl) -4-oxo- 3,4-dihydroquinazolin- 2-yl] methyl semicarbazone (3A-d-4, 3B-d-4 and 3C-d-4) showed sig...
ChemInform, 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.
Few series of glutamic acid analogs and its cyclised variants were designed, synthesized and char... more Few series of glutamic acid analogs and its cyclised variants were designed, synthesized and characterized by FT-IR, 1 H NMR, Protondecoupled 13 C NMR, MS and elemental analysis. Compounds were tested in vivo for antineoplastic activity in female Swiss albino mice against EAC (Ehrlich Ascites Carcinoma) strain. Cytotoxicity study was carried out on HUVEC and Vero cell lines by MTT assay method. Some promising results are noticed which show that few molecules are having selective inhibitory effect on EAC cell growth and probable antiangiogenic activity but there is no significant toxic effect on normal cell.
Crystal Research and Technology, 2002
The crystal structure and molecular conformation of solvated 1-(4-methoxybenzenesulfonyl)-5-oxopy... more The crystal structure and molecular conformation of solvated 1-(4-methoxybenzenesulfonyl)-5-oxopyrrolidine-2-carboxamide (C 12 H 14 O 5 N 2 S.H 2 O), synthesized and biologically evaluated as a possible antineoplastic agent, have been studied by X-ray analysis and AM1 molecular orbital methods. The compound crystallizes in the monoclinic space group P2 1 , with a = 9.661(4), b = 7.246(3), c = 11.378(5)Å, β = 113.42(2)°, Z= 2. The structure has been solved by direct methods and refined to R = 0.0438 for 1721 observed reflections. The crystal structure consists of an essentially planar methoxyphenyl ring linked to a 2-carboxamide substituted oxo-pyrrolidine moiety via sulfonyl group and a lattice water molecule. The conformational analysis of the title compound investigated by semiempirical quantum mechanical AM1 calculations shows a good agreement with the X-ray structure except a rotation of the carboxamide moiety about the C (oxo-pyrrolidine)-C (carboxamide) bond. In the solid state, the molecules translated in the b-direction are linked by intermolecular N-H⋅⋅⋅O hydrogen bonds to form infinite one-dimensional chain.