Synthesis of A New Thiadiazole-Benzodioxole Derivative, Investigation of Acetylcholinesterase Inhibition with In Vitro and In Silico Studies

Sare Peçe Göktaş; Derya Osmaniye; Serkan Levent; Begüm Nurpelin Sağlık Özkan; Bünyamin Göktaş; Harun Uslu; Yusuf Özkay

Makale detayları

Synthesis of A New Thiadiazole-Benzodioxole Derivative, Investigation of Acetylcholinesterase Inhibition with In Vitro and In Silico Studies

Yazarlar:

Sare Peçe Göktaş | Derya Osmaniye | Serkan Levent | Begüm Nurpelin Sağlık Özkan | Bünyamin Göktaş | Harun Uslu | Yusuf Özkay

Yayıncı:

Anadolu University

Ana Başlıklar:

Pharmacology and Pharmaceutical Sciences (Other)

Dergi:

European Journal of Life Sciences Vol.3 Issue 2, pp.82-92

Belge Tipi:

Makale

Yayın Tarihi:

8/2024

Belge Dili:

İngilizce

Document ID (Org No.):

2001326022

pISSN:

2822-5333

Anahtar kelimeler:

Özet:

 Alzheimers disease is a progressive and degenerative brain disease that negatively affects peoples lives and reduces cognitive and sensory human functions. Today, there are active ingredients that work on Alzheimers disease, containing benzodioxole and thiadiazole rings. Acetylcholinesterase terminates neurotransmission in the nervous system and leads to the accumulation of acetylcholine, overstimulation of various receptors and consequent impairment of neurotransmission. Thiadiazole and benzodioxole rings are compounds that exhibit a wide range of biological activities, especially known to be effective on acetylcholinesterase. A new compound containing benzodioxole and thiadiazole rings was designed, synthesized and its chemical structure was revealed using spectroscopic methods such as HRMS, 13C-NMR and 1H-NMR. Acetylcholinesterase inhibition activities were investigated using in vitro methods. To elucidate the acetylcholinesterase inhibition of compound 4a, it was subjected to in silico insertion procedure with 4EY7. Compound 4a exhibited 0.1140.005 µM against AChE. The above data is compared with data for donepezil 0.02010.0014 µM, the reference compound in our study.

 Alzheimers disease is a progressive and degenerative brain disease that negatively affects peoples lives and reduces cognitive and sensory human functions. Today, there are active ingredients that work on Alzheimers disease, containing benzodioxole and thiadiazole rings. Acetylcholinesterase terminates neurotransmission in the nervous system and leads to the accumulation of acetylcholine, overstimulation of various receptors and consequent impairment of neurotransmission. Thiadiazole and benzodioxole rings are compounds that exhibit a wide range of biological activities, especially known to be effective on acetylcholinesterase. A new compound containing benzodioxole and thiadiazole rings was designed, synthesized and its chemical structure was revealed using spectroscopic methods such as HRMS, 13C-NMR and 1H-NMR. Acetylcholinesterase inhibition activities were investigated using in vitro methods. To elucidate the acetylcholinesterase inhibition of compound 4a, it was subjected to in silico insertion procedure with 4EY7. Compound 4a exhibited 0.1140.005 µM against AChE. The above data is compared with data for donepezil 0.02010.0014 µM, the reference compound in our study.

 Alzheimers disease is a progressive and degenerative brain disease that negatively affects peoples lives and reduces cognitive and sensory human functions. Today, there are active ingredients that work on Alzheimers disease, containing benzodioxole and thiadiazole rings. Acetylcholinesterase terminates neurotransmission in the nervous system and leads to the accumulation of acetylcholine, overstimulation of various receptors and consequent impairment of neurotransmission. Thiadiazole and benzodioxole rings are compounds that exhibit a wide range of biological activities, especially known to be effective on acetylcholinesterase. A new compound containing benzodioxole and thiadiazole rings was designed, synthesized and its chemical structure was revealed using spectroscopic methods such as HRMS, 13C-NMR and 1H-NMR. Acetylcholinesterase inhibition activities were investigated using in vitro methods. To elucidate the acetylcholinesterase inhibition of compound 4a, it was subjected to in silico insertion procedure with 4EY7. Compound 4a exhibited 0.1140.005 µM against AChE. The above data is compared with data for donepezil 0.02010.0014 µM, the reference compound in our study.

 Alzheimers disease is a progressive and degenerative brain disease that negatively affects peoples lives and reduces cognitive and sensory human functions. Today, there are active ingredients that work on Alzheimers disease, containing benzodioxole and thiadiazole rings. Acetylcholinesterase terminates neurotransmission in the nervous system and leads to the accumulation of acetylcholine, overstimulation of various receptors and consequent impairment of neurotransmission. Thiadiazole and benzodioxole rings are compounds that exhibit a wide range of biological activities, especially known to be effective on acetylcholinesterase. A new compound containing benzodioxole and thiadiazole rings was designed, synthesized and its chemical structure was revealed using spectroscopic methods such as HRMS, 13C-NMR and 1H-NMR. Acetylcholinesterase inhibition activities were investigated using in vitro methods. To elucidate the acetylcholinesterase inhibition of compound 4a, it was subjected to in silico insertion procedure with 4EY7. Compound 4a exhibited 0.1140.005 µM against AChE. The above data is compared with data for donepezil 0.02010.0014 µM, the reference compound in our study.

Makale detayları

Synthesis of A New Thiadiazole-Benzodioxole Derivative, Investigation of Acetylcholinesterase Inhibition with In Vitro and In Silico Studies

Yazarlar:

Sare Peçe Göktaş | Derya Osmaniye | Serkan Levent | Begüm Nurpelin Sağlık Özkan | Bünyamin Göktaş | Harun Uslu | Yusuf Özkay

Yayıncı:

Anadolu University

Ana Başlıklar:

Pharmacology and Pharmaceutical Sciences (Other)

Dergi:

European Journal of Life Sciences Vol.3 Issue 2, pp.82-92

Belge Tipi:

Makale

Yayın Tarihi:

8/2024

Belge Dili:

İngilizce

Document ID (Org No.):

2001326022

pISSN:

2822-5333

AChE

ADME

Benzodioxole

Molecular Docking

Thiadiazole

Sayı

Makale detayları

Synthesis of A New Thiadiazole-Benzodioxole Derivative, Investigation of Acetylcholinesterase Inhibition with In Vitro and In Silico Studies

Yazarlar: Sare Peçe Göktaş | Derya Osmaniye | Serkan Levent | Begüm Nurpelin Sağlık Özkan | Bünyamin Göktaş | Harun Uslu | Yusuf Özkay

Yayıncı: Anadolu University

Ana Başlıklar: Pharmacology and Pharmaceutical Sciences (Other)

Dergi: European Journal of Life Sciences Vol.3 Issue 2, pp.82-92

Belge Tipi: Makale

Yayın Tarihi: 8/2024

Belge Dili: İngilizce

Document ID (Org No.): 2001326022

pISSN: 2822-5333

AChE

ADME

Benzodioxole

Molecular Docking

Thiadiazole

Sayı

Yazarlar:

Sare Peçe Göktaş | Derya Osmaniye | Serkan Levent | Begüm Nurpelin Sağlık Özkan | Bünyamin Göktaş | Harun Uslu | Yusuf Özkay

Yayıncı:

Anadolu University

Ana Başlıklar:

Pharmacology and Pharmaceutical Sciences (Other)

Dergi:

European Journal of Life Sciences Vol.3 Issue 2, pp.82-92

Belge Tipi:

Makale

Yayın Tarihi:

8/2024

Belge Dili:

İngilizce

Document ID (Org No.):

2001326022

pISSN:

2822-5333