Polyhydroquinoline derivatives for diabetic management: synthesis, in vitro and in silico approaches

被引：15

作者：

Talab, Faiz ^{[1
]}

Zainab, Aftab ^{[2
]}

Alam, Aftab ^{[1
,2
]}

Ali, Mumtaz ^{[1
]}

Rehman, Najeeb Ur ^{[1
,3
]}

Ullah, Saeed ^{[3
]}

Halim, Sobia Ahsan ^{[3
]}

Islam, Mohammad Shahidul ^{[4
]}

Khan, Ajmal ^{[3
]}

Latif, Abdul ^{[1
]}

Ayaz, Muhammad ^{[1
]}

Al-Ghafri, Ahmed ^{[3
]}

Al-Harrasi, Ahmed ^{[3
]}

Ahmad, Manzoor ^{[1
]}

机构：

[1] Univ Malakand, Dept Chem, POB 18800, Totakan, Khyber Pakhtunk, Pakistan

[2] Hebei Normal Univ, Coll Chem & Mat Sci, Shijiazhuang 050024, Peoples R China

[3] Univ Nizwa, Nat & Med Sci Res Ctr, Nizwa 616, Oman

[4] King Saud Univ, Coll Sci, Dept Chem, POB 2455, Riyadh 11451, Saudi Arabia

来源：

FUTURE MEDICINAL CHEMISTRY | 2023年 / 15卷 / 23期

关键词：

molecular docking; NMR spectroscopy; polyhydroquinoline; structure-activity relationship; alpha-glucosidase; ALPHA-GLUCOSIDASE; MOLECULAR DOCKING; CATALYST; PATHWAY;

D O I：

10.4155/fmc-2023-0232

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Background: Medication used to treat Type 2 diabetes by decreasing the absorption of carbohydrates in the intestine consists of alpha-glucosidase inhibitors. Polyhydroquinoline derivatives have attracted interest as excellent antidiabetic agents. Methods: Polyhydroquinoline derivatives (1-17) were synthesized and tested for in vitro alpha-glucosidase inhibitory activity. Results: All the synthesized compounds exhibited excellent to good inhibitory activity, having IC50 values from 1.23 +/- 0.03 to 73.85 +/- 0.61 mu M, compared with the standard drug, acarbose. The binding mechanism of these derivatives with alpha-glucosidase was deduced by docking studies and indicated that a slight variation in the orientation of compounds, affects their binding capability. Conclusion: In order to find new antidiabetic drugs, this study has discovered prospective lead candidates.

引用

页码：2195 / 2208

页数：14

共 50 条

[1] Synthesis of 3-hydroxy-2-naphthohydrazide-based hydrazones and their implications in diabetic management via in vitro and in silico approaches
Tasleem, Mussarat
Ullah, Saeed
Halim, Sobia Ahsan
Urooj, Ifra
Ahmed, Nadeem
Munir, Rabia
Khan, Ajmal
El-kott, Attalla F.
Taslimi, Parham
Negm, Sally
Al-Harrasi, Ahmed
Shafiq, Zahid
ARCHIV DER PHARMAZIE, 2024, 357 (02)
[2] Exploration of Polyhydroquinoline (PHQ) derivatives for antibacterial effects: Synthesis, biological screening, and in-silico evaluation
Hussain, Sajid
Latif, Abdul
Ali, Mumtaz
Ammara
Ahmad, Manzoor
Khan, Ajmal
Al-Harrasi, Ahmed
Ozdemir, Fethi Ahmet
JOURNAL OF MOLECULAR STRUCTURE, 2025, 1334
[3] Synthesis of new bis(dimethylamino)benzophenone hydrazone for diabetic management: In-vitro and in-silico approach
Khan, Momin
Ahad, Ghulam
Alam, Aftab
Ullah, Saeed
Khan, Ajmal
Kanwal
Salar, Uzma
Wadood, Abdul
Ajmal, Amar
Khan, Khalid Mohammed
Perveen, Shahnaz
Uddin, Jalal
Al-Harrasi, Ahmed
HELIYON, 2024, 10 (01)
[4] Exploration of green catalytic Hantzsch process for synthesis of polyhydroquinoline derivatives and their in silico & in vitro evaluation as anti-tubercular agents
Savale, Tulshidas S.
Joshi, Nachiket
Rao, G. S. N. Koteswara
Mathure, Savita M.
Chobe, Santosh S.
More, Rahul A.
Budha, Roja Rani
Alavala, Rajasekhar Reddy
JOURNAL OF MOLECULAR STRUCTURE, 2025, 1320
[5] Investigating Novel Thiophene Carbaldehyde Based Thiazole Derivatives as Potential Hits for Diabetic Management: Synthesis, In Vitro and In Silico Approach
Ullah, Najeeb
Alam, Aftab
Zainab
Elhenawy, Ahmed A.
Naz, Saira
Islam, Mohammad Shahidul
Ahmad, Shujaat
Shah, Syed Adnan Ali
Ahmad, Manzoor
CHEMISTRYSELECT, 2024, 9 (08):
[6] Stereoselective Synthesis of Highly Functionalized Aminobenzothiazole-Fused Spirooxindole Derivatives: in silico and in vitro Anti-Diabetic Studies
Nivetha, Narayanasamy
Patil, Shashank M.
Ramu, Ramith
Sreenivasa, Swamy
Velmathi, Sivan
SYNTHESIS-STUTTGART, 2023, 55 (24): : 4145 - 4162
[7] Novel acyl hydrazide derivatives of polyhydroquinoline as potent anti-diabetic and anti-glycating agents: Synthesis, in vitro α-amylase, α-glucosidase inhibition and anti-glycating activity with molecular docking insights
Rahman, Sajjad Ur
Alam, Aftab
Parveen, Zahida
Zainab
Assad, Mohammad
Shah, Syed Adnan Ali
Rafiq, Huma
Ayaz, Muhammad
Latif, Abdul
Umar, Muhammad Naveed
Ali, Mumtaz
Ahmad, Manzoor
BIOORGANIC CHEMISTRY, 2024, 150
[8] Oxamide Derivatives as Potent α-Glucosidase Inhibitors: Design, Synthesis, In Vitro Inhibitory Screening and In Silico Docking Studies
Malik, Naseema Perveen
Naz, Maira
Ashiq, Uzma
Jamal, Rifat A.
Gul, Sana
Saleem, Faiza
Khan, Khalid M.
Yousuf, Sammer
CHEMISTRYSELECT, 2021, 6 (28): : 7188 - 7201
[9] Synthesis, in vitro α-glucosidase and α-amylase activities, and an in silico molecular docking study of triazinoindole-thiazolidinone hybrid derivatives
Khan, Aftab Ahmad
Ullah, Hayat
Rahim, Fazal
Taha, Muhammad
Khan, Fahad
Rehman, Wajid
Wadood, Abdul
Khan, Khalid Mohammed
CHEMICAL DATA COLLECTIONS, 2023, 45
[10] Design, synthesis, in vitro and in silico studies of naproxen derivatives as dual lipoxygenase and α-glucosidase inhibitors
Sardar, Asma
Abid, Obaid-ur-Rahman
Daud, Saima
Fakhar-E-Alam, M.
Siddique, Muhammad Hussnain
Ashraf, Muhammad
Shahid, Wardah
Ejaz, Syeda Abida
Atif, M.
Ahmad, Shafiq
Shafeeq, Sulman
Afzal, Muhammad
JOURNAL OF SAUDI CHEMICAL SOCIETY, 2022, 26 (03)

← 1 2 3 4 5 →