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Pyridine sulfonamide as a small key organic molecule for the potential treatment of type-II diabetes mellitus and Alzheimer's disease: In vitro studies against yeast α-glucosidase, acetylcholinesterase and butyrylcholinesterase.
Bioorg Chem. 2015 Dec; 63:64-71.BC

Abstract

This paper presents the efficient high yield synthesis of novel pyridine 2,4,6-tricarbohydrazide derivatives (4a-4i) along with their α-glucosidase, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition activities. The enzymes inhibition results showed the potential of synthesized compounds in controlling both type-II diabetes mellitus and Alzheimer's disease. In vitro biological investigations revealed that most of compounds were more active against yeast α-glucosidase than the reference compound acarbose (IC50 38.25±0.12μM). Among the tested series the compound 4c bearing 4-flouro benzyl group was noted to be the most active (IC50 25.6±0.2μM) against α-glucosidase, and it displayed weak inhibition activities against AChE and BChE. Compound 4a exhibited the most desired results against all three enzymes, as it was significantly active against all the three enzymes; α-glucosidase (IC50 32.2±0.3μM), AChE (IC50 50.2±0.8μM) and BChE (IC50 43.8±0.8μM). Due to the most favorable activity of 4a against the tested enzymes, for molecular modeling studies this compound was selected to investigate its pattern of interaction with α-glucosidase and AChE targets.

Authors+Show Affiliations

Department of Chemistry, GC University, Lahore 54000, Pakistan.Department of Chemistry, GC University, Lahore 54000, Pakistan. Electronic address: iuklodhi@yahoo.com.Department of Physicochemical Drug Analysis, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Cracow, Poland.Department of Chemistry, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan.Department of Biochemistry and Biotechnology, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan.Department of Biochemistry and Biotechnology, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan.Department of Chemistry, GC University, Lahore 54000, Pakistan.Department of Chemistry, GC University, Lahore 54000, Pakistan.Department of Chemistry, GC University, Lahore 54000, Pakistan.Department of Chemistry, GC University, Lahore 54000, Pakistan.Interdisciplinary Research Center in Biomedical Materials, COMSATS Institute of Information Technology, Lahore 54000, Pakistan. Electronic address: drmyar@ciitlahore.edu.pk.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

26451651

Citation

Riaz, Sadaf, et al. "Pyridine Sulfonamide as a Small Key Organic Molecule for the Potential Treatment of type-II Diabetes Mellitus and Alzheimer's Disease: in Vitro Studies Against Yeast Α-glucosidase, Acetylcholinesterase and Butyrylcholinesterase." Bioorganic Chemistry, vol. 63, 2015, pp. 64-71.
Riaz S, Khan IU, Bajda M, et al. Pyridine sulfonamide as a small key organic molecule for the potential treatment of type-II diabetes mellitus and Alzheimer's disease: In vitro studies against yeast α-glucosidase, acetylcholinesterase and butyrylcholinesterase. Bioorg Chem. 2015;63:64-71.
Riaz, S., Khan, I. U., Bajda, M., Ashraf, M., Qurat-Ul-Ain, ., Shaukat, A., Rehman, T. U., Mutahir, S., Hussain, S., Mustafa, G., & Yar, M. (2015). Pyridine sulfonamide as a small key organic molecule for the potential treatment of type-II diabetes mellitus and Alzheimer's disease: In vitro studies against yeast α-glucosidase, acetylcholinesterase and butyrylcholinesterase. Bioorganic Chemistry, 63, 64-71. https://doi.org/10.1016/j.bioorg.2015.09.008
Riaz S, et al. Pyridine Sulfonamide as a Small Key Organic Molecule for the Potential Treatment of type-II Diabetes Mellitus and Alzheimer's Disease: in Vitro Studies Against Yeast Α-glucosidase, Acetylcholinesterase and Butyrylcholinesterase. Bioorg Chem. 2015;63:64-71. PubMed PMID: 26451651.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Pyridine sulfonamide as a small key organic molecule for the potential treatment of type-II diabetes mellitus and Alzheimer's disease: In vitro studies against yeast α-glucosidase, acetylcholinesterase and butyrylcholinesterase. AU - Riaz,Sadaf, AU - Khan,Islam Ullah, AU - Bajda,Marek, AU - Ashraf,Muhammad, AU - Qurat-Ul-Ain,, AU - Shaukat,Ayesha, AU - Rehman,Tanzeel Ur, AU - Mutahir,Sadaf, AU - Hussain,Sajjad, AU - Mustafa,Ghulam, AU - Yar,Muhammad, Y1 - 2015/09/30/ PY - 2015/06/28/received PY - 2015/09/14/revised PY - 2015/09/28/accepted PY - 2015/10/10/entrez PY - 2015/10/10/pubmed PY - 2016/9/9/medline KW - AChE KW - Alzheimer’s disease KW - BChE KW - Diabetes mellitus type-II KW - Pyridine derivatives KW - α-glucosidase SP - 64 EP - 71 JF - Bioorganic chemistry JO - Bioorg. Chem. VL - 63 N2 - This paper presents the efficient high yield synthesis of novel pyridine 2,4,6-tricarbohydrazide derivatives (4a-4i) along with their α-glucosidase, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition activities. The enzymes inhibition results showed the potential of synthesized compounds in controlling both type-II diabetes mellitus and Alzheimer's disease. In vitro biological investigations revealed that most of compounds were more active against yeast α-glucosidase than the reference compound acarbose (IC50 38.25±0.12μM). Among the tested series the compound 4c bearing 4-flouro benzyl group was noted to be the most active (IC50 25.6±0.2μM) against α-glucosidase, and it displayed weak inhibition activities against AChE and BChE. Compound 4a exhibited the most desired results against all three enzymes, as it was significantly active against all the three enzymes; α-glucosidase (IC50 32.2±0.3μM), AChE (IC50 50.2±0.8μM) and BChE (IC50 43.8±0.8μM). Due to the most favorable activity of 4a against the tested enzymes, for molecular modeling studies this compound was selected to investigate its pattern of interaction with α-glucosidase and AChE targets. SN - 1090-2120 UR - https://www.unboundmedicine.com/medline/citation/26451651/Pyridine_sulfonamide_as_a_small_key_organic_molecule_for_the_potential_treatment_of_type_II_diabetes_mellitus_and_Alzheimer's_disease:_In_vitro_studies_against_yeast_α_glucosidase_acetylcholinesterase_and_butyrylcholinesterase_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0045-2068(15)30023-7 DB - PRIME DP - Unbound Medicine ER -