shashi kala - Academia.edu (original) (raw)
Papers by shashi kala
Materials Today: Proceedings, 2022
BMC Chemistry, 2021
Background 1,2,4-oxadiazole derivatives exhibited significant anti-cancer activity when they were... more Background 1,2,4-oxadiazole derivatives exhibited significant anti-cancer activity when they were evaluated, against human cancer cell lines. They also showed anti-inflammatory, analgesic, diabetic, immunosuppressive, α,β3-receptor antagonist, antimicrobial, anti-helminthic, histamine-H3 and antiparasitic properties. A pyrimidine analog, 5 fluoro-uracil is a chemotherapeutic drug used for treating multiple solid malignant tumors. But its application is limited, as it has side effects like low bioavailability and high toxicity. Molecular docking is an exemplary tool, helps in identifying target and designing a drug containing high bio-availability and minimum toxicity. Results A set of 1,2,4-oxadiazole linked 5-fluoruracil derivatives (7a–j) were synthesized and their structures were confirmed by 1HNMR, 13CNMR and Mass spectral analysis. Further, these compounds were investigated for their anticancer activity towards a panel of four human cancer cell lines such as (MCF-7, MDA MB-231)...
European Journal of Chemistry, 2017
A new facile and efficient synthesis of 2-((5-aryl-1,3,4-oxadiazol-2-yl) methoxy)-3-methyl quinox... more A new facile and efficient synthesis of 2-((5-aryl-1,3,4-oxadiazol-2-yl) methoxy)-3-methyl quinoxaline and 3-methylquinoxalin-2-yl-2-(5-aryl-2Htetrazol-2-yl)acetate derivatives
Organic and Medicinal Chemistry Letters, 2014
Background 1,8-Naphthyridine derivatives have attracted considerable attention because the 1,8-na... more Background 1,8-Naphthyridine derivatives have attracted considerable attention because the 1,8-naphthyridine skeleton is present in many compounds that have been isolated from natural substances, with various biological activities. Findings N,N-dimethoxy-N-methyl-1,8-naphthyridine-3-carboxamide (1) on reaction with Grignard reagent forms 2-methoxy-1,8-naphthyridine-3-carbaldehyde (2). Compound 2 on reaction with different aromatic aldehydes provided 1-(2-cyclopropyl-1,8-naphthyridin-3-yl)-3-arylprop-2-en-1-ones (3a-e) and these compounds on cyclisation with hydrazine hydrate 99% yielded 2-cyclopropyl-3-(5-aryl-1H-pyrazol-3-yl)-1,8-naphthyridines (4-a-e). Synthesis of the target compounds involved the formation of 4a-e. It was accomplished using Grignard reaction, condensation reaction, and cyclisation reactions. All the synthesized compounds were readily soluble in DMSO. Spectral data of the synthesized compounds were in full agreement with the proposed structures. Conclusions In co...
Objective: The main objective of this study is to find out the benefits of physical exercise, imp... more Objective: The main objective of this study is to find out the benefits of physical exercise, impact of nutrition education and to study the existing dietary pattern and nutrient intake of selected NIDDM patients. Method: The survey on diabetic patients indicates that incidence of diabetes is predominant in male than females. 54% of the subjects had a positive family history with either a single parent (24%) both the parents (10%) or in sibling (22%). Results: The results of the present study indicated the 68% of the subjects were not pursuing any kind of physical activity, but due to nutrition education there was a significant improvement (P<0.01). Walking was done by 32% of the subjects before nutrition education for a period of 15-30 minutes but the percentage significantly increased to 72% after nutrition education and the time increased from 30 min to 1 hour. 28% started doing stretch exercises after nutrition education. 65% of the subjects were often mentally tense but coun...
![Research paper thumbnail of Synthesis and antibacterial activity of novel 5,6,7,8-tetrahydroimidazo[1,2-a]pyrimidine-2-carbohydrazide derivatives](https://attachments.academia-assets.com/84112897/thumbnails/1.jpg)
](Chemistry Central Journal, 2015
Background: The intensely increasing multi-drug resistant microbial infections have encouraged th... more Background: The intensely increasing multi-drug resistant microbial infections have encouraged the search for new antimicrobial agents. Hydrazone derivatives are known to exhibit a wide variety of biological activities including antimicrobial. In heterocyclic moiety, imidazo[1,2-a]pyrimidines are the subject of immense interest for their antimicrobial activity and also for their analgesic, antipyretic and anti-inflammatory properties. Results: Condensation of 5,6,7,8-tetrahydroimidazo[1,2-a]pyrimidine-2-carbohydrazide 7 with aromatic aldehydes a-k in ethanol at reflux led to the generation of hydrazone derivatives 8a-k in 80-92% yield. The synthesis of carbohydrazide 7 was accomplished in six steps from commercially available 2-amino pyrimidine. The structures of the synthesized compounds were confirmed by 1 H, 13 C NMR, Mass and IR spectral data. All the synthesized hydrazone derivatives 8a-k were tested in vitro for their antibacterial activity. Compounds 8d, 8e and 8f exhibited excellent antibacterial activity with zone of inhibition 30-33 mm against E. coli (Gram negative bacteria) and S. aureus (Gram positive bacteria). These compounds also exhibited excellent antibacterial activity with zone of inhibition 22-25 mm against P. aeruginosa (Gram negative bacteria) and S. pyogenes (Gram positive bacteria). Conclusion: Synthesized and recorded antibacterial activity of some new 5,6,7,8-tetrahydro-imidazo[1,2-a]pyrimidine-hydrazone derivatives.
Background 1,2,4-oxadiazole derivatives exhibited significant anti-cancer activity when they were... more Background 1,2,4-oxadiazole derivatives exhibited significant anti-cancer activity when they were evaluated, against human cancer cell lines. They also showed anti-inflammatory, analgesic, diabetic, immunosuppressive, α,β3-receptor antagonist, antimicrobial, anti-helminthic, histamine-H3 and antiparasitic properties. A pyrimidine analog, 5 fluoro-uracil is a chemotherapeutic drug used for treating multiple solid malignant tumors. But its application is limited, as it has side effects like low bioavailability and high toxicity. Molecular docking is an exemplary tool, helps in identifying target and designing a drug containing high bio-availability and minimum toxicity. Results A set of 1,2,4-oxadiazole linked 5-fluoruracil derivatives (7a–j) were synthesized and their structures were confirmed by 1HNMR, 13CNMR and Mass spectral analysis. Further, these compounds were investigated for their anticancer activity towards a panel of four human cancer cell lines such as (MCF-7, MDA MB-231)...
Materials Today: Proceedings, 2021
Materials Today: Proceedings, 2022
BMC Chemistry, 2021
Background 1,2,4-oxadiazole derivatives exhibited significant anti-cancer activity when they were... more Background 1,2,4-oxadiazole derivatives exhibited significant anti-cancer activity when they were evaluated, against human cancer cell lines. They also showed anti-inflammatory, analgesic, diabetic, immunosuppressive, α,β3-receptor antagonist, antimicrobial, anti-helminthic, histamine-H3 and antiparasitic properties. A pyrimidine analog, 5 fluoro-uracil is a chemotherapeutic drug used for treating multiple solid malignant tumors. But its application is limited, as it has side effects like low bioavailability and high toxicity. Molecular docking is an exemplary tool, helps in identifying target and designing a drug containing high bio-availability and minimum toxicity. Results A set of 1,2,4-oxadiazole linked 5-fluoruracil derivatives (7a–j) were synthesized and their structures were confirmed by 1HNMR, 13CNMR and Mass spectral analysis. Further, these compounds were investigated for their anticancer activity towards a panel of four human cancer cell lines such as (MCF-7, MDA MB-231)...
European Journal of Chemistry, 2017
A new facile and efficient synthesis of 2-((5-aryl-1,3,4-oxadiazol-2-yl) methoxy)-3-methyl quinox... more A new facile and efficient synthesis of 2-((5-aryl-1,3,4-oxadiazol-2-yl) methoxy)-3-methyl quinoxaline and 3-methylquinoxalin-2-yl-2-(5-aryl-2Htetrazol-2-yl)acetate derivatives
Organic and Medicinal Chemistry Letters, 2014
Background 1,8-Naphthyridine derivatives have attracted considerable attention because the 1,8-na... more Background 1,8-Naphthyridine derivatives have attracted considerable attention because the 1,8-naphthyridine skeleton is present in many compounds that have been isolated from natural substances, with various biological activities. Findings N,N-dimethoxy-N-methyl-1,8-naphthyridine-3-carboxamide (1) on reaction with Grignard reagent forms 2-methoxy-1,8-naphthyridine-3-carbaldehyde (2). Compound 2 on reaction with different aromatic aldehydes provided 1-(2-cyclopropyl-1,8-naphthyridin-3-yl)-3-arylprop-2-en-1-ones (3a-e) and these compounds on cyclisation with hydrazine hydrate 99% yielded 2-cyclopropyl-3-(5-aryl-1H-pyrazol-3-yl)-1,8-naphthyridines (4-a-e). Synthesis of the target compounds involved the formation of 4a-e. It was accomplished using Grignard reaction, condensation reaction, and cyclisation reactions. All the synthesized compounds were readily soluble in DMSO. Spectral data of the synthesized compounds were in full agreement with the proposed structures. Conclusions In co...
Objective: The main objective of this study is to find out the benefits of physical exercise, imp... more Objective: The main objective of this study is to find out the benefits of physical exercise, impact of nutrition education and to study the existing dietary pattern and nutrient intake of selected NIDDM patients. Method: The survey on diabetic patients indicates that incidence of diabetes is predominant in male than females. 54% of the subjects had a positive family history with either a single parent (24%) both the parents (10%) or in sibling (22%). Results: The results of the present study indicated the 68% of the subjects were not pursuing any kind of physical activity, but due to nutrition education there was a significant improvement (P<0.01). Walking was done by 32% of the subjects before nutrition education for a period of 15-30 minutes but the percentage significantly increased to 72% after nutrition education and the time increased from 30 min to 1 hour. 28% started doing stretch exercises after nutrition education. 65% of the subjects were often mentally tense but coun...
Chemistry Central Journal, 2015
Background: The intensely increasing multi-drug resistant microbial infections have encouraged th... more Background: The intensely increasing multi-drug resistant microbial infections have encouraged the search for new antimicrobial agents. Hydrazone derivatives are known to exhibit a wide variety of biological activities including antimicrobial. In heterocyclic moiety, imidazo[1,2-a]pyrimidines are the subject of immense interest for their antimicrobial activity and also for their analgesic, antipyretic and anti-inflammatory properties. Results: Condensation of 5,6,7,8-tetrahydroimidazo[1,2-a]pyrimidine-2-carbohydrazide 7 with aromatic aldehydes a-k in ethanol at reflux led to the generation of hydrazone derivatives 8a-k in 80-92% yield. The synthesis of carbohydrazide 7 was accomplished in six steps from commercially available 2-amino pyrimidine. The structures of the synthesized compounds were confirmed by 1 H, 13 C NMR, Mass and IR spectral data. All the synthesized hydrazone derivatives 8a-k were tested in vitro for their antibacterial activity. Compounds 8d, 8e and 8f exhibited excellent antibacterial activity with zone of inhibition 30-33 mm against E. coli (Gram negative bacteria) and S. aureus (Gram positive bacteria). These compounds also exhibited excellent antibacterial activity with zone of inhibition 22-25 mm against P. aeruginosa (Gram negative bacteria) and S. pyogenes (Gram positive bacteria). Conclusion: Synthesized and recorded antibacterial activity of some new 5,6,7,8-tetrahydro-imidazo[1,2-a]pyrimidine-hydrazone derivatives.
Background 1,2,4-oxadiazole derivatives exhibited significant anti-cancer activity when they were... more Background 1,2,4-oxadiazole derivatives exhibited significant anti-cancer activity when they were evaluated, against human cancer cell lines. They also showed anti-inflammatory, analgesic, diabetic, immunosuppressive, α,β3-receptor antagonist, antimicrobial, anti-helminthic, histamine-H3 and antiparasitic properties. A pyrimidine analog, 5 fluoro-uracil is a chemotherapeutic drug used for treating multiple solid malignant tumors. But its application is limited, as it has side effects like low bioavailability and high toxicity. Molecular docking is an exemplary tool, helps in identifying target and designing a drug containing high bio-availability and minimum toxicity. Results A set of 1,2,4-oxadiazole linked 5-fluoruracil derivatives (7a–j) were synthesized and their structures were confirmed by 1HNMR, 13CNMR and Mass spectral analysis. Further, these compounds were investigated for their anticancer activity towards a panel of four human cancer cell lines such as (MCF-7, MDA MB-231)...
Materials Today: Proceedings, 2021