Hariram Singh

Dr. A.P.J. Abdul Kalam Technical University

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Rajiv Roy

Calcutta National Medical College and Hospital

Rajeev Kumar

King George's Medical University

Tejendra Singh

Sarojini Naidu Medical College

Dheeraj Kumar

National Institute of Technology Warangal

Anurag Chaudhary

Zoological Survey of India

Amar Deep Singh

Dr. K.N.Modi University

Devender Pathak

Rajiv Gandhi University of Health Sciences

Vijay Kumar Sharma

Advanced Bioscience Laboratories (United States)

Rajarshi Roy

Jadavpur University

Sushil Kumar

IFTM University

Cooperative Institutions

Dr. K.N.Modi University

Jamia Hamdard

Central Drug Research Institute

Delhi Pharmaceutical Science and Research University

Indian Institute of Technology Delhi

Jadavpur University

Swami Vivekanand Subharti University

Shobhit University

Institute of Medical Sciences

Indian Institute of Technology Roorkee

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1,2,4-Triazine Analogs as Novel Class of Therapeutic Agents

Mini-Reviews in Medicinal Chemistry (2014)

Rajeev Kumar T.S. Sirohi Hariram Singh Ramji Lal Yadav Rajiv Roy

1,2,4-Triazine nucleus is a prominent structural core system present in numerous pharmacologically active compounds. Till date, various 1,2,4-triazine analogs, possesing a wide range of potent pharmacological activities, have been reported. This review is an attempt to compile the medicinal chemistry aspects of various synthesized 1,2,4-triazine analogs reported so far. Keywords: Anticancer activity, anticonvulsant activity, antimicrobial activity, 1, 2, 4-triazine.

Triazine

1,3,5-Triazine

10.2174/1389557514666140131111837

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Citations (106)

1,2,3-Triazine Scaffold as a Potent Biologically Active Moiety: A Mini Review

Mini-Reviews in Medicinal Chemistry (2014)

Rajeev Kumar Amar Singh Jitendra Singh Hariram Singh Rajarshi Roy

1,2,3-Triazine is an interesting class of heterocyclic compounds. Various synthetic analogs of 1,2,3-triazine have been prepared and evaluated for many pharmacological activities in different models with desired findings. Some analogs have shown potent pharmacological activity and may be considered as lead molecule for the development of future drugs. This review is an attempt to organize the chemical and pharmacological aspects of 1,2,3-triazine analogs reported till date systematically since 1970.

Moiety

Triazine

10.2174/1389557513666140103111017

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Citations (47)

Design, synthesis and anticonvulsant activity of some new 5,7-dibromoisatin semicarbazone derivatives.

PubMed (2013)

Dheeraj Kumar Vijay Kumar Sharma Rajeev Kumar Tejendra Singh Hariram Singh

A series of 5,7-dibromoisatin semicarbazones have been synthesized in good yield, involving aryl urea and aryl semicarbazide formation. The structures of the synthesized compounds were confirmed on the basis of their spectral data. All the compounds were evaluated for anticonvulsant and CNS depressant activities. Anticonvulsant activity was determined after intraperitoneal (i.p.) administration to mice by maximal electroshock (MES) induced seizure method and minimal motor impairment was determined by rotarod test. A computational study was carried out for prediction of pharmacokinetic properties and making them potentially promising agents for the treatment of epilepsy. Compounds (Z)-1-(5,7-dibromo-2-oxoindolin-3-ylidene)-4-(4-chlorophenyl)semicarbazide (DH-05), (Z)-1-(5,7-dibromo-2-oxoindolin-3-ylidene)-4-(3-chloro-4-fluorophenyl)semicarbazide (DH-11) and (Z)-1-(5,7-dibromo-1-methyl-2-oxoindolin-3-ylidene)-4-(3-chloro-4-fluorophenyl)semicarbazide (DH-12) exhibited prominent anticonvulsant effect in the series with little or no neurotoxicity and little CNS depressant effect as compared to standard drug.

Semicarbazide

Semicarbazone

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Citations (10)

Unveiling the Anti-convulsant Potential of Novel Series of 1,2,4-Triazine- 6H-Indolo[2,3-b]quinoline Derivatives: In Silico Molecular Docking, ADMET, DFT, and Molecular Dynamics Exploration

Current Computer - Aided Drug Design (2023)

Hariram Singh Devender Pathak

Epilepsy is a chronic neurological disorder caused by irregular electrical activity in the brain. To manage this disorder effectively, it is imperative to identify potential pharmacological targets and to understand the pathophysiology of epilepsy in depth.

Convulsants

Docking (animal)

Quinoline

Triazine

10.2174/1573409920666230817144710

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Citations (1)

Original article: DESIGN, SYNTHESIS AND ANTICONVULSANT ACTIVITY OF SOME NEW 5,7-DIBROMOISATIN SEMICARBAZONE DERIVATIVES

Dheeraj Kumar Vijay Kumar Sharma Rajeev Kumar Tejendra Singh Hariram Singh

A series of 5,7-dibromoisatin semicarbazones have been synthesized in good yield, involving aryl urea and aryl semicarbazide formation. The structures of the synthesized compounds were confirmed on the basis of their spectral data. All the compounds were evaluated for anticonvulsant and CNS depressant activities. Anticonvulsant activity was determined after intraperitoneal (i.p.) administration to mice by maximal electroshock (MES) induced seizure method and minimal motor impairment was determined by rotarod test. A computational study was carried out for prediction of pharmacokinetic properties and making them potentially promising agents for the treatment of epilepsy. Compounds (Z)-1-(5,7-dibromo-2-oxoindolin-3-ylidene)-4-(4-chlorophenyl)semicarbazide (DH-05), (Z)-1-(5,7-dibromo-2-oxoindolin-3-ylidene)-4-(3-chloro-4-fluorophenyl)semicarbazide (DH-11) and (Z)-1-(5,7-dibromo-1methyl-2-oxoindolin-3-ylidene)-4-(3-chloro-4-fluorophenyl)semicarbazide (DH-12) exhibited prominent anticonvulsant effect in the series with little or no neurotoxicity and little CNS depressant effect as compared to standard drug.

Semicarbazide

Semicarbazone

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GLP-1 Targeted Novel 3-phenyl-7-hydroxy Substituted Coumarins Mitigate STZ-induced Pancreatic Damage and Improve Glucose Homeostasis in OGTT Method

Protein and Peptide Letters (2022)

Mandeep Kumar Gupta Rajnish Srivastava Sushil Kumar Krishna Kumar Varshney Hariram Singh

Worldwide, type 2 diabetes mellitus accounts for a considerable burden of disease, with an estimated global cost of >800 billion USD annually. For this reason, the search for more effective and efficient therapeutic anti-diabetic agents is continuing. Recent studies support the search for coumarins or related compounds with potential blood glucose-lowering properties.The study aims to design, synthesize and evaluate the hypoglycemic activity of a new class of 7-hydroxy coumarin derivatives.To explore and establish the in-silico-driven pharmacological role of a new class of 7- hydroxy coumarin derivatives as the therapeutic strategies against type 2 diabetes mellitus.A new class of 7-hydroxy coumarin derivatives was designed by assessment of their physicochemical properties and molecular docking against the Glucagon-like peptide-1 (GLP-1) receptor. Two novel series of 30 compounds were synthesized. The chemical structures of all the synthesized analogues have been elucidated by spectral studies of IR, 1H-NMR, and mass spectroscopy. After considering the molecular docking score and their physicochemical properties, the compounds were screened out for the evaluation of their hypoglycemic potential. The compounds were investigated for their hypoglycemic activity using a streptozotocin (STZ) induced diabetic model and an oral glucose tolerance test (OGTT) method at different dose levels.The molecular docking studies of synthesized derivatives reveal significant molecular interaction with the various amino acid residues of the GLP-1 receptor. IR spectral analysis revealed a strong band of -NH stretching in the range of 3406.7-3201.61 cm-1 and one strong band for the lactone carbonyl group of the coumarin ring in the range of 1722.0-1703.5 cm-1, confirming the chemical structure of all produced compounds. The synthesized coumarin analogues with the best docking score exhibited remarkable hypoglycemic potential as assessed by the STZ model and the OGTT method.Coumarin derivatives explored a good structure-activity relationship (SAR) and produced significant hypoglycemic potential.

Docking (animal)

10.2174/0929866529666220829090810

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Synthesis of substituted 1-hydroxy-2-naphthanilides as potential cestodicidal agents

Journal of Medicinal Chemistry (1978)

Shikha Dubey Ashok Kumar Singh Hariram Singh S. SHARMA R. N. IYER

A series of substituted 1-hydroxy-2-naphthanilides 4--14 has been synthesized by treating 1-hydroxy-2-naphthoic acids 2 with substituted anilines 3. The nitronaphthanilides, on reduction and subsequent treatment with thiophosgene, gave the corresponding substituted 2-naphthanilide isothiocyanates 30--33. Substitution of the chlorine of 8 by various cyclic amines gave 3'-nitro-4'-substituted 1-hydroxy-2-naphthanilides 15--21. Various 3-aryl-4-oxo-2,3-dihydro-1,3-naphthoxazine-2-thiones 34-43 and 3 aryl-2,4-dioxo-2,3-dihydro-1,3-naphthoxazines 44--51 have been prepared by reacting the corresonding naphthanilides with thiophosgene and ethyl chloroformate, respectively. All the compounds were tested for their cestodicidal activity against Hymenolepis nana infection in rats; 30 was found to be the most active compound of the series, showing 100% clearance of infection at a single oral dose of 7.5 mg/kg.

10.1021/jm00209a020

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Citations (28)

Design, synthesis and anticonvulsant activity of some new 6,8-halo-substituted-2h-[1,2,4]triazino[5,6-b]indole-3(5h)-one/-thione and 6,8-halo-substituted 5-methyl-2h-[1,2,4]triazino[5,6-b]indol-3(5h)-one/-thione.

PubMed (2014)

Rajeev Kumar Tejendra Singh Hariram Singh Sandeep Jain Rajiv Roy

A new series of 6,8-halo-substituted-2H-[1,2,4]triazino[5,6-b]indole-3(5H)-one/-thione and 6,8-halo-substituted 5-methyl-2H-[1,2,4]triazino[5,6-b]indol-3(5H)-one/-thione (5a-5l) were designed and synthesized keeping in view of the structural requirement of pharmacophore. The above compounds were characterized by thin layer chromatography and spectral analysis. Anticonvulsant activity of the synthesized compounds was evaluated by the maximal electroshock (MES) test. Neurotoxicity and CNS depressant effects were evaluated by the rotarod motor impairment and Porsolt's force swim tests, respectively. A computational study was carried out, for calculation of pharmacophore pattern, prediction of pharmacokinetic properties and toxicity properties. The above study revealed that the compounds 8-chloro-2H-[1,2,4]triazino[5,6-b]indol-3(5H)-one (5e), 6,8-dibromo-2H-[1,2,4]triazino[5,6-b]indol-3(5H)-one (5i) and 6,8-dibromo-5-methyl-2H-[1,2,4]triazino[5,6-b]indol-3(5H)-one (5k) possess excellent anticonvulsant activity in the series with little CNS depressant effect and no neurotoxicity as compared to standard drugs phenytoin and carbamazepine.

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Exploring GABAA receptor modulation through integrated synthesis, bioactivity, and computational approach of 1,2,4-triazine derivatives

Journal of Molecular Structure (2024)

Hariram Singh Ajay Manaithiya Devender Pathak Faiyaz Shakeel

Triazine

Modulation (music)

10.1016/j.molstruc.2024.140924

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Citations (0)