Literature DB >> 17723306

Synthesis and antidiabetic activity of 2,5-disubstituted-3-imidazol-2-yl-pyrrolo[2,3-b]pyridines and thieno[2,3-b]pyridines.

Rajesh H Bahekar1, Mukul R Jain, Pradip A Jadav, Vijay M Prajapati, Dipam N Patel, Arun A Gupta, Ajay Sharma, Robby Tom, Debdutta Bandyopadhya, Honey Modi, Pankaj R Patel.   

Abstract

In the present investigation, two series of 2,5-disubstituted-3-imidazol-2-yl-pyrrolo[2,3-b]pyridines (2a-l) and thieno[2,3-b]pyridines (3a-l) were designed as analogs of BL 11282 (1). The in vitro glucose dependent insulinotropic activity of all the test compounds was evaluated using RIN5F cell based assay and all the test compounds showed glucose and concentration dependent insulin secretion. The in vivo antidiabetic activities of most potent compounds from each series (2c and 3c) were assessed in C57BL/6J mice. Compounds 2c and 3c showed dose dependent insulin secretion and significant glucose reduction in vivo. In general, compounds 2c and 3c were found to be equipotent at all the three different doses selected and with respect to BL 11282, both the test compounds were found to be more potent, at all the time points.

Entities:  

Mesh:

Substances:

Year:  2007        PMID: 17723306     DOI: 10.1016/j.bmc.2007.08.005

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  9 in total

1.  Synthesis and Structure-Activity Relationships of 3,5-Disubstituted-pyrrolo[2,3- b]pyridines as Inhibitors of Adaptor-Associated Kinase 1 with Antiviral Activity.

Authors:  Sven Verdonck; Szu-Yuan Pu; Fiona J Sorrell; Jon M Elkins; Mathy Froeyen; Ling-Jie Gao; Laura I Prugar; Danielle E Dorosky; Jennifer M Brannan; Rina Barouch-Bentov; Stefan Knapp; John M Dye; Piet Herdewijn; Shirit Einav; Steven De Jonghe
Journal:  J Med Chem       Date:  2019-06-12       Impact factor: 7.446

2.  Further modifications of 1H-pyrrolo[2,3-b]pyridine derivatives as inhibitors of human neutrophil elastase.

Authors:  Maria P Giovannoni; Niccolò Cantini; Letizia Crocetti; Gabriella Guerrini; Antonella Iacovone; Igor A Schepetkin; Claudia Vergelli; Andrei I Khlebnikov; Mark T Quinn
Journal:  Drug Dev Res       Date:  2019-04-19       Impact factor: 4.360

3.  Crystal structure and Hirshfeld surface analysis of 5-acetyl-3-amino-6-methyl-N-phenyl-4-[(E)-2-phenyl-ethen-yl]thieno[2,3-b]pyridine-2-carbox-amide.

Authors:  Shaaban K Mohamed; Etify A Bakhite; Sevim Türktekin Çelikesir; Hajjaj H M Abdu-Allah; Mehmet Akkurt; Omaima F Ibrahim; Joel T Mague; Safiyyah A H Al-Waleedy
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2022-01-28

4.  Design, synthesis and evaluation of amino-3,5-dicyanopyridines and thieno[2,3-b]pyridines as ligands of adenosine A1 receptors for the potential treatment of epilepsy.

Authors:  Gaofenngwe Nkomba; Gisella Terre'Blanche; Helena D Janse van Rensburg; Lesetja J Legoabe
Journal:  Med Chem Res       Date:  2022-05-24       Impact factor: 2.351

Review 5.  Pyridine: the scaffolds with significant clinical diversity.

Authors:  Sourav De; Ashok Kumar S K; Suraj Kumar Shah; Sabnaz Kazi; Nandan Sarkar; Subhasis Banerjee; Sanjay Dey
Journal:  RSC Adv       Date:  2022-05-20       Impact factor: 4.036

6.  Investigation of Antihyperglycaemic Activity of Banana (Musa sp. Var. Nanjangud rasa bale) Flower in Normal and Diabetic Rats.

Authors:  Ramith Ramu; Prithvi S Shirahatti; S P Dhanabal; Farhan Zameer; B L Dhananjaya; M N Nagendra Prasad
Journal:  Pharmacogn Mag       Date:  2017-10-11       Impact factor: 1.085

7.  Efficient Synthesis of Novel Pyridine-Based Derivatives via Suzuki Cross-Coupling Reaction of Commercially Available 5-Bromo-2-methylpyridin-3-amine: Quantum Mechanical Investigations and Biological Activities.

Authors:  Gulraiz Ahmad; Nasir Rasool; Hafiz Mansoor Ikram; Samreen Gul Khan; Tariq Mahmood; Khurshid Ayub; Muhammad Zubair; Eman Al-Zahrani; Usman Ali Rana; Muhammad Nadeem Akhtar; Noorjahan Banu Alitheen
Journal:  Molecules       Date:  2017-01-27       Impact factor: 4.411

8.  Sulfaguanidine Hybrid with Some New Pyridine-2-One Derivatives: Design, Synthesis, and Antimicrobial Activity against Multidrug-Resistant Bacteria as Dual DNA Gyrase and DHFR Inhibitors.

Authors:  Ahmed Ragab; Sawsan A Fouad; Ola A Abu Ali; Entsar M Ahmed; Abeer M Ali; Ahmed A Askar; Yousry A Ammar
Journal:  Antibiotics (Basel)       Date:  2021-02-05

Review 9.  Heterocyclic compounds as a magic bullet for diabetes mellitus: a review.

Authors:  Umme Farwa; Muhammad Asam Raza
Journal:  RSC Adv       Date:  2022-08-16       Impact factor: 4.036

  9 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.