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6 results on '"Jallapally A"'

1. Design, synthesis and evaluation of novel 2-butyl-4-chloroimidazole derived peptidomimetics as Angiotensin Converting Enzyme (ACE) inhibitors.

Author

Jallapally A, Addla D, Bagul P, Sridhar B, Banerjee SK, and Kantevari S

Subjects
Angiotensin-Converting Enzyme Inhibitors pharmacology, Antihypertensive Agents pharmacology, Benzazepines chemistry, Benzazepines pharmacology, Catalytic Domain, Cell Line, Tumor, Cell Survival drug effects, Drug Design, Enalapril chemistry, Enalapril pharmacology, Epithelial Cells, HEK293 Cells, Humans, Imidazoles pharmacology, Lisinopril chemistry, Lisinopril pharmacology, Molecular Docking Simulation, Peptidomimetics pharmacology, Protein Binding, Quinapril, Ramipril chemistry, Ramipril pharmacology, Structure-Activity Relationship, Tetrahydroisoquinolines chemistry, Tetrahydroisoquinolines pharmacology, Angiotensin-Converting Enzyme Inhibitors chemical synthesis, Antihypertensive Agents chemical synthesis, Imidazoles chemical synthesis, Peptidomimetics chemical synthesis, Peptidyl-Dipeptidase A chemistry
Abstract

A series of novel 2-butyl-4-chloro-1-methylimidazole derived peptidomimetics were designed, synthesized and evaluated for their Angiotensin Converting Enzyme (ACE) inhibitor activity. 2-Butyl-4-chloro-1-methylimidazole-5-carboxylic acid 2 obtained after oxidation of respective carboxaldehyde 1, was condensed with various amino acid methyl esters 3a-k to give imidazole-amino acid conjugates 4a-k in very good yields. Ester hydrolysis of 4a-k with aqueous LiOH gave the desired peptidomimetics 5a-k. Screening all the new compounds 4a-k and 5a-k using ACE inhibition assay, resulted five compounds 4i, 4k, 5e, 5h and 5i as potent ACE inhibitors with IC50 of 0.647, 0.531, 1.12, 0.657 and 0.100μM with minimal toxicity. Among them, 5i emerged as most active ACE inhibitor with greater potency than marketed drugs Lisinopril, Ramipril and relatively equipotent to Benazepril, Quinapril and Enalapril., (Copyright © 2015. Published by Elsevier Ltd.)

Published
2015
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2. Design and green synthesis of 2-(diarylalkyl)aminobenzothiazole derivatives and their dual activities as angiotensin converting enzyme inhibitors and calcium channel blockers.

Author

Kalavagunta PK, Bagul PK, Jallapally A, Kantevari S, Banerjee SK, and Ravirala N

Subjects
Angiotensin-Converting Enzyme Inhibitors chemistry, Animals, Benzothiazoles chemistry, Benzothiazoles metabolism, Calcium Channel Blockers chemistry, Calcium Channel Blockers metabolism, Chemistry Techniques, Synthetic, Dose-Response Relationship, Drug, Green Chemistry Technology, Male, Molecular Docking Simulation, Peptidyl-Dipeptidase A chemistry, Peptidyl-Dipeptidase A metabolism, Protein Conformation, Rats, Rats, Sprague-Dawley, Angiotensin-Converting Enzyme Inhibitors chemical synthesis, Angiotensin-Converting Enzyme Inhibitors pharmacology, Benzothiazoles chemical synthesis, Benzothiazoles pharmacology, Calcium Channel Blockers chemical synthesis, Calcium Channel Blockers pharmacology, Drug Design
Abstract

A series of novel 2-(diarylalkyl)aminobenzothiazoles were designed based on commercial synthetic calcium channel blockers (CCBs) and angiotensin converting enzyme (ACE) inhibitors. Which are further modified based on the natural products which are angiotensin converting enzyme (ACE) inhibitors. Completely green protocol was developed for their synthesis. As they are initially designed based on CCBs, they were screened for their ACE inhibition property believing that almost all the compounds will be CCBs. Out of 42 compounds two lead molecules were identified as ACE inhibitors, which were further screened for CCB. As expected both were identified as CCBs with different selectivity over ACE inhibition. Their selectivity over ACE and CCB can be used to treat resistant hypertension., (Copyright © 2014 Elsevier Masson SAS. All rights reserved.)

Published
2014
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3. Design, synthesis and evaluation of novel 2-hydroxypyrrolobenzodiazepine-5,11-dione analogues as potent angiotensin converting enzyme (ACE) inhibitors.

Author

Addla D, Jallapally A, Kanwal A, Sridhar B, Banerjee SK, and Kantevari S

Subjects
Angiotensin-Converting Enzyme Inhibitors chemical synthesis, Animals, Crystallography, X-Ray, Dose-Response Relationship, Drug, Drug Design, HEK293 Cells, Humans, Models, Molecular, Pyrroles chemical synthesis, Pyrroles chemistry, Pyrroles pharmacology, Rabbits, Structure-Activity Relationship, Angiotensin-Converting Enzyme Inhibitors chemistry, Angiotensin-Converting Enzyme Inhibitors pharmacology, Benzodiazepines chemical synthesis, Benzodiazepines chemistry, Benzodiazepines pharmacology
Abstract

A series of novel 10-substituted 2-hydroxypyrrolobenzodiazepine-5,11-diones designed through structure based rational hybridization approach, synthesized by the cyclodehydration of isotonic anhydride with (2S,4R)-4-hydroxypyrrolidine-2-carboxylic acid followed by N-substitution, were evaluated as angiotensin converting enzyme (ACE) inhibitors. Among all the new compounds screened (2R,11aS)-10-((4-bromothiophen-2-yl)methyl)-2-hydroxy-2,3-dihydro-1H-benzo[e]pyrrolo[1,2-a][1,4]diazepine-5,11(10H,11aH)dione, 5v (IC₅₀: 0.272 μM) emerged as most active non-carboxylic acid ACE inhibitor with minimal toxicity comparable to clinical drugs Lisinopril, Benazepril and Ramipril. Favorable binding characteristics in docking studies also supported the experimental results., (Copyright © 2013 Elsevier Ltd. All rights reserved.)

Published
2013
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4. Design, synthesis and evaluation of novel 2-hydroxypyrrolobenzodiazepine-5,11-dione analogues as potent angiotensin converting enzyme (ACE) inhibitors

Author

Abhinav Kanwal, Anvesh Jallapally, Srinivas Kantevari, Dinesh Addla, Balasubramanian Sridhar, and Sanjay K. Banerjee

Subjects
Models, Molecular, Ramipril, Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Benazepril, Angiotensin-Converting Enzyme Inhibitors, Crystallography, X-Ray, Biochemistry, Benzodiazepines, Structure-Activity Relationship, Drug Discovery, medicine, Animals, Humans, Structure–activity relationship, Pyrroles, Proline, Molecular Biology, Dose-Response Relationship, Drug, biology, Chemistry, Organic Chemistry, Lisinopril, Angiotensin-converting enzyme, HEK293 Cells, Docking (molecular), Drug Design, ACE inhibitor, biology.protein, Molecular Medicine, Rabbits, medicine.drug
Abstract

A series of novel 10-substituted 2-hydroxypyrrolobenzodiazepine-5,11-diones designed through structure based rational hybridization approach, synthesized by the cyclodehydration of isotonic anhydride with (2S,4R)-4-hydroxypyrrolidine-2-carboxylic acid followed by N-substitution, were evaluated as angiotensin converting enzyme (ACE) inhibitors. Among all the new compounds screened (2R,11aS)-10-((4-bromothiophen-2-yl)methyl)-2-hydroxy-2,3-dihydro-1H-benzo[e]pyrrolo[1,2-a][1,4]diazepine-5,11(10H,11aH)dione, 5v (IC₅₀: 0.272 μM) emerged as most active non-carboxylic acid ACE inhibitor with minimal toxicity comparable to clinical drugs Lisinopril, Benazepril and Ramipril. Favorable binding characteristics in docking studies also supported the experimental results.

Published
2013

5. Design, synthesis and evaluation of novel 2-butyl-4-chloroimidazole derived peptidomimetics as Angiotensin Converting Enzyme (ACE) inhibitors

Author

Balasubramanian Sridhar, Pankaj K. Bagul, Sanjay K. Banerjee, Srinivas Kantevari, Dinesh Addla, and Anvesh Jallapally

Subjects
Ramipril, Stereochemistry, Cell Survival, Clinical Biochemistry, Pharmaceutical Science, Benazepril, Angiotensin-Converting Enzyme Inhibitors, Peptidyl-Dipeptidase A, Biochemistry, Structure-Activity Relationship, Enalapril, Lisinopril, Catalytic Domain, Cell Line, Tumor, Tetrahydroisoquinolines, Drug Discovery, medicine, Humans, Molecular Biology, Antihypertensive Agents, chemistry.chemical_classification, biology, Chemistry, Organic Chemistry, Imidazoles, Quinapril, Angiotensin-converting enzyme, Epithelial Cells, Benzazepines, Amino acid, Molecular Docking Simulation, HEK293 Cells, Drug Design, ACE inhibitor, biology.protein, Molecular Medicine, Peptidomimetics, medicine.drug, Protein Binding
Abstract

A series of novel 2-butyl-4-chloro-1-methylimidazole derived peptidomimetics were designed, synthesized and evaluated for their Angiotensin Converting Enzyme (ACE) inhibitor activity. 2-Butyl-4-chloro-1-methylimidazole-5-carboxylic acid 2 obtained after oxidation of respective carboxaldehyde 1 , was condensed with various amino acid methyl esters 3a – k to give imidazole–amino acid conjugates 4a – k in very good yields. Ester hydrolysis of 4a – k with aqueous LiOH gave the desired peptidomimetics 5a – k . Screening all the new compounds 4a – k and 5a – k using ACE inhibition assay, resulted five compounds 4i , 4k , 5e , 5h and 5i as potent ACE inhibitors with IC 50 of 0.647, 0.531, 1.12, 0.657 and 0.100 μM with minimal toxicity. Among them, 5i emerged as most active ACE inhibitor with greater potency than marketed drugs Lisinopril, Ramipril and relatively equipotent to Benazepril, Quinapril and Enalapril.

Published
2015

6. Design and green synthesis of 2-(diarylalkyl)aminobenzothiazole derivatives and their dual activities as angiotensin converting enzyme inhibitors and calcium channel blockers

Author

Srinivas Kantevari, Praveen Kumar Kalavagunta, Pankaj K. Bagul, Narender Ravirala, Anvesh Jallapally, and Sanjay K. Banerjee

Subjects
Male, Protein Conformation, Resistant hypertension, Angiotensin-Converting Enzyme Inhibitors, Chemistry Techniques, Synthetic, Pharmacology, Peptidyl-Dipeptidase A, Rats, Sprague-Dawley, Drug Discovery, Animals, Benzothiazoles, Ace inhibition, biology, Dose-Response Relationship, Drug, Chemistry, Calcium channel, Organic Chemistry, Angiotensin-converting enzyme, Green Chemistry Technology, General Medicine, Calcium Channel Blockers, Combinatorial chemistry, Rats, Molecular Docking Simulation, Drug Design, biology.protein
Abstract

A series of novel 2-(diarylalkyl)aminobenzothiazoles were designed based on commercial synthetic calcium channel blockers (CCBs) and angiotensin converting enzyme (ACE) inhibitors. Which are further modified based on the natural products which are angiotensin converting enzyme (ACE) inhibitors. Completely green protocol was developed for their synthesis. As they are initially designed based on CCBs, they were screened for their ACE inhibition property believing that almost all the compounds will be CCBs. Out of 42 compounds two lead molecules were identified as ACE inhibitors, which were further screened for CCB. As expected both were identified as CCBs with different selectivity over ACE inhibition. Their selectivity over ACE and CCB can be used to treat resistant hypertension.

Published
2013

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