Center for Innovative Research

Hyderabad, India

Center for Innovative Research

Hyderabad, India
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Poudapally S.,GVK Biosciences Pvt. Ltd. | Poudapally S.,JNTUH College of Engineering | Gurram V.,GVK Biosciences Pvt. Ltd. | Garlapati R.,GVK Biosciences Pvt. Ltd. | And 6 more authors.
Journal of Heterocyclic Chemistry | Year: 2017

C(sp)–C(sp2) bond formation via Sonogashira cross-coupling reactions on 6-halo-2-cyclopropyl-3-(pyridyl-3-ylmethyl)quinazolin-4(3H)-ones with appropriate alkynes was explored. Optimization of reaction conditions with various catalysts, ligands, bases, and solvents was conducted. The combination of PdCl2(MeCN)2 with X-Phos proved to be the best metal–ligand system for this conversion in the presence of triethylamine (Et3N) in tetrahydrofuran at room temperature for iodosubstrates, at 80°C for the bromosubstrates in 8 h, and also for the chlorosubstrates in 16 h. We also demonstrated synthesis of a successful diversity-oriented synthesis library of highly functionalized quinazolinones via Cu-free Sonogashira coupling of diverse aryl halides and azido-alkyne (“click”) ligation reactions with substituted azides. The library exhibited significant antimicrobial activity when screened against several microorganisms. © 2017 Wiley Periodicals, Inc.


Gurram V.,GVK Biosciences Pvt. Ltd | Garlapati R.,GVK Biosciences Pvt. Ltd | Thulluri C.,Center for Innovative Research | Madala N.,GVK Biosciences Pvt. Ltd | And 7 more authors.
Medicinal Chemistry Research | Year: 2014

Abstract To develop a lead anti-diabetic compound, a series of 21 novel quinazoline derivatives have been synthesized and screened against a-glucosidase. The binding mode of the compounds at the active site of a-glucosidase was explored using Glide docking method. The binding model suggests one to four hydrogen bonding interactions between quinazoline derivatives and a-glucosidase. 6-Bromo-2-cyclopropyl quinazoline-4(3H)-one has been modified by C-C cross coupling to obtain nine different aryl scaffolds. These scaffolds further modified at C-4 position using amidation method to generate 21 compounds. Based on the interaction profile and docking score, all these compounds were selected for in vitro enzymatic screening. Seven of the thirty six compounds showed <20 μM activity against a-glucosidase and among these, compound 6f showed the highest inhibition, with an IC50 of 3.4 #x003BC;M. In silico analysis was utilized to evaluate the diversity of the set of compounds against shape space, and relevant drug-like properties. © Springer Science+Business Media New York 2014.

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