SYNTHESIS AND BIOLOGICAL EVALUATION OF 1H-(INDOLE-5-YL)-3-SUBSTITUTED-1,2,4-OXADIAZOLES AS NOVEL 5-LOX INHIBITORS

Berihu Tekluu; Siddaiah Vidavalur; Sunanda Kumari Kadiri

Makale detayları

SYNTHESIS AND BIOLOGICAL EVALUATION OF 1H-(INDOLE-5-YL)-3-SUBSTITUTED-1,2,4-OXADIAZOLES AS NOVEL 5-LOX INHIBITORS

Yazarlar:

Berihu Tekluu | Siddaiah Vidavalur | Sunanda Kumari Kadiri

Yayıncı:

Turkish Chemical Society

Ana Başlıklar:

Organic Chemical Synthesis

Dergi:

Journal of the Turkish Chemical Society Section A: Chemistry Vol.11 Issue 1, pp.11-18

Belge Tipi:

Makale

Yayın Tarihi:

4/2024

Belge Dili:

İngilizce

Document ID (Org No.):

2001303735

pISSN:

2149-0120

Anahtar kelimeler:

Özet:

 : A series of indolyloxadiazoles were synthesized from amidoxime and indole 3-carboxaldehyde using CAN as a catalyst and PEG as a solvent. In vitro, a 5-LOX inhibitory assay has been performed for all the synthesized compounds. Among the tested compounds, 4bf showed the highest potency IC50 18.78 µgml. The synthesized compound carried out docking on the 5-LOX enzyme protein crystal structure. Compound 4bf docked snugly into the receptor site with a score of -9.1 Kcalmol, and it showed strong hydrogen bond interactions with two key amino acids, His368 and Asn555.

 : A series of indolyloxadiazoles were synthesized from amidoxime and indole 3-carboxaldehyde using CAN as a catalyst and PEG as a solvent. In vitro, a 5-LOX inhibitory assay has been performed for all the synthesized compounds. Among the tested compounds, 4bf showed the highest potency IC50 18.78 µgml. The synthesized compound carried out docking on the 5-LOX enzyme protein crystal structure. Compound 4bf docked snugly into the receptor site with a score of -9.1 Kcalmol, and it showed strong hydrogen bond interactions with two key amino acids, His368 and Asn555.

 : A series of indolyloxadiazoles were synthesized from amidoxime and indole 3-carboxaldehyde using CAN as a catalyst and PEG as a solvent. In vitro, a 5-LOX inhibitory assay has been performed for all the synthesized compounds. Among the tested compounds, 4bf showed the highest potency IC50 18.78 µgml. The synthesized compound carried out docking on the 5-LOX enzyme protein crystal structure. Compound 4bf docked snugly into the receptor site with a score of -9.1 Kcalmol, and it showed strong hydrogen bond interactions with two key amino acids, His368 and Asn555.

 : A series of indolyloxadiazoles were synthesized from amidoxime and indole 3-carboxaldehyde using CAN as a catalyst and PEG as a solvent. In vitro, a 5-LOX inhibitory assay has been performed for all the synthesized compounds. Among the tested compounds, 4bf showed the highest potency IC50 18.78 µgml. The synthesized compound carried out docking on the 5-LOX enzyme protein crystal structure. Compound 4bf docked snugly into the receptor site with a score of -9.1 Kcalmol, and it showed strong hydrogen bond interactions with two key amino acids, His368 and Asn555.

Makale detayları

SYNTHESIS AND BIOLOGICAL EVALUATION OF 1H-(INDOLE-5-YL)-3-SUBSTITUTED-1,2,4-OXADIAZOLES AS NOVEL 5-LOX INHIBITORS

Yazarlar:

Berihu Tekluu | Siddaiah Vidavalur | Sunanda Kumari Kadiri

Yayıncı:

Turkish Chemical Society

Ana Başlıklar:

Organic Chemical Synthesis

Dergi:

Journal of the Turkish Chemical Society Section A: Chemistry Vol.11 Issue 1, pp.11-18

Belge Tipi:

Makale

Yayın Tarihi:

4/2024

Belge Dili:

İngilizce

Document ID (Org No.):

2001303735

pISSN:

2149-0120

1-2-4-oxadiazoles

Indolyloxadiazoles

5-LOX inhibitors

Sayı

Makale detayları

SYNTHESIS AND BIOLOGICAL EVALUATION OF 1H-(INDOLE-5-YL)-3-SUBSTITUTED-1,2,4-OXADIAZOLES AS NOVEL 5-LOX INHIBITORS

Yazarlar: Berihu Tekluu | Siddaiah Vidavalur | Sunanda Kumari Kadiri

Yayıncı: Turkish Chemical Society

Ana Başlıklar: Organic Chemical Synthesis

Dergi: Journal of the Turkish Chemical Society Section A: Chemistry Vol.11 Issue 1, pp.11-18

Belge Tipi: Makale

Yayın Tarihi: 4/2024

Belge Dili: İngilizce

Document ID (Org No.): 2001303735

pISSN: 2149-0120

1-2-4-oxadiazoles

Indolyloxadiazoles

5-LOX inhibitors

Sayı

Yazarlar:

Berihu Tekluu | Siddaiah Vidavalur | Sunanda Kumari Kadiri

Yayıncı:

Turkish Chemical Society

Ana Başlıklar:

Organic Chemical Synthesis

Dergi:

Journal of the Turkish Chemical Society Section A: Chemistry Vol.11 Issue 1, pp.11-18

Belge Tipi:

Makale

Yayın Tarihi:

4/2024

Belge Dili:

İngilizce

Document ID (Org No.):

2001303735

pISSN:

2149-0120