Version 1
: Received: 29 August 2024 / Approved: 30 August 2024 / Online: 30 August 2024 (09:38:35 CEST)
How to cite:
Alvarado Salazar, J. A.; Valdes, M.; Cruz, A.; Moreno De Jesús, B.; Patiño González, D.; Olivares-Corichi, I. M.; Tamay Cach, F.; Mendieta Wejebe, J. E. In Silico and In Vivo Evaluation of Novel 2-Aminobenzothiazole Derivative Compounds as Antidiabetic Agents. Preprints2024, 2024082205. https://doi.org/10.20944/preprints202408.2205.v1
Alvarado Salazar, J. A.; Valdes, M.; Cruz, A.; Moreno De Jesús, B.; Patiño González, D.; Olivares-Corichi, I. M.; Tamay Cach, F.; Mendieta Wejebe, J. E. In Silico and In Vivo Evaluation of Novel 2-Aminobenzothiazole Derivative Compounds as Antidiabetic Agents. Preprints 2024, 2024082205. https://doi.org/10.20944/preprints202408.2205.v1
Alvarado Salazar, J. A.; Valdes, M.; Cruz, A.; Moreno De Jesús, B.; Patiño González, D.; Olivares-Corichi, I. M.; Tamay Cach, F.; Mendieta Wejebe, J. E. In Silico and In Vivo Evaluation of Novel 2-Aminobenzothiazole Derivative Compounds as Antidiabetic Agents. Preprints2024, 2024082205. https://doi.org/10.20944/preprints202408.2205.v1
APA Style
Alvarado Salazar, J. A., Valdes, M., Cruz, A., Moreno De Jesús, B., Patiño González, D., Olivares-Corichi, I. M., Tamay Cach, F., & Mendieta Wejebe, J. E. (2024). In Silico and In Vivo Evaluation of Novel 2-Aminobenzothiazole Derivative Compounds as Antidiabetic Agents. Preprints. https://doi.org/10.20944/preprints202408.2205.v1
Chicago/Turabian Style
Alvarado Salazar, J. A., Feliciano Tamay Cach and Jessica Elena Mendieta Wejebe. 2024 "In Silico and In Vivo Evaluation of Novel 2-Aminobenzothiazole Derivative Compounds as Antidiabetic Agents" Preprints. https://doi.org/10.20944/preprints202408.2205.v1
Abstract
Currently, there are several drugs used for the treatment of type 2 diabetes (T2D), however, all of them have adverse effects. Benzothiazoles have a broad spectrum of biological activities such as antidiabetic. This study aimed to evaluate in silico and in vivo two series of 2-aminobenzothiazole derivatives linked to isothioureas (3a-w) or guanidines (4a-z) for the treatment of T2D. The ADMET properties were determined in silico from which it was possible to select compounds 3a, 3b, 4a, 4b, 4c, 4r, 4s, 4x, and 4y and, with molecular docking, it was shown that 3b and 4y showed high affinity for PPAR gamma (ΔG = -7.8 and -8.4 kcal/mol, respectively). In vivo, the LD50 value was estimated in rat based on OECD Guideline 425, being > 1750 mg/kg for both compounds. The pharmaco-logical effect of 3b and 4y was evaluated in the T2D rat model, showing that after oral admin-istration in equimolar ratio to pioglitazone (15 mg/kg) for 4 weeks, both compounds were able to reduce blood glucose levels (< 200 mg/dL) and improve the lipid profile. Therefore, 3b and 4y could be used in the future as antidiabetic agents.
Keywords
2-aminobenzotiazol; isotioureas; guanidinas; diabetes tipo 2; actividad antidiabética
Subject
Medicine and Pharmacology, Pharmacology and Toxicology
Copyright:
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
