Pyridine- and Thiazole-Based Hydrazides with Promising Anti-inflammatory and Antimicrobial Activities along with Their In Silico Studies | Zendy

Vinuta Kamat | Zendy; Rangappa Santosh | Zendy; Boja Poojary | Zendy; Suresh P. Nayak | Zendy; Banoth Karan Kumar | Zendy; Sankaranarayanan Murugesan | Zendy; Faheem Faheem | Zendy; Sheela Khanapure | Zendy; Delicia A. Barretto | Zendy; Shyam Kumar Vootla | Zendy

Open Access

Pyridine- and Thiazole-Based Hydrazides with Promising Anti-inflammatory and Antimicrobial Activities along with Their In Silico Studies

Author(s) -

Vinuta Kamat,

Rangappa Santosh,

Boja Poojary,

Suresh P. Nayak,

Banoth Karan Kumar,

Sankaranarayanan Murugesan,

Faheem Faheem,

Sheela Khanapure,

Delicia A. Barretto,

Shyam Kumar Vootla

Publication year - 2020

Publication title -

acs omega

Language(s) - English

Resource type - Journals

ISSN - 2470-1343

DOI - 10.1021/acsomega.0c03386

Subject(s) - thiazole , antimicrobial , in silico , chemistry , pyridine , docking (animal) , stereochemistry , combinatorial chemistry , ic50 , in vitro , biochemistry , organic chemistry , medicine , nursing , gene

A new class of compounds formed by the linkage of -C(O)-NH- with pyridine and thiazole moieties was designed, synthesized, and characterized by various spectral approaches. The newly characterized compounds were evaluated for their antimicrobial as well as anti-inflammatory properties. The in vitro anti-inflammatory activity of these compounds was evaluated by denaturation of the bovine serum albumin method and showed inhibition in the range of IC 50 values-46.29-100.60 μg/mL. Among all the tested compounds, compound 5l has the highest IC 50 value and compound 5g has the least IC 50 value. On the other hand, antimicrobial results revealed that compound 5j showed the lowest MIC values and compound 5a has the highest MIC values. Furthermore, molecular docking of the active compounds demonstrated a better docking score and interacted well with the target protein. Physicochemical parameters of the titled compounds were found suitable in the reference range only. The in silico molecular docking study revealed their COX-inhibitory action. Compound 5j emerged as a significant bioactive molecule among the synthesized analogues.

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