Satish Shamrao Kola

EDUCATION

M.Sc, SET, GATE,Ph.D

RESEARCH, TEACHING, or OTHER INTERESTS

Chemistry

Scopus Publications

SYNTHESIS, ANTIMICROBIAL SCREENING AND MOLECULAR DOCKING STUDY OF SOME NEW PYRIMIDIN-2-AMINE DERIVATIVES AS POSSIBLE BIOACTIVE AGENTS
N. J. Siddiqui, S. D. Kawale, G. M. Phadnaik, H. M. Alone, S. S. Kola
Rasayan Journal of Chemistry, 2025
A novel series of 4, 6-disubstituted pyrimidin-2-amine derivatives (5a–f) was synthesized in good yields via a cyclocondensation reaction of chalcone-based intermediates (4a–f) with guanidine hydrochloride using sodium methoxide as the base. The key intermediates, N'-(5-(3-(2,4-disubstituted phenyl)-3-oxoprop-1-enyl)-4-(4- bromophenyl)-6-(3,4-disubstituted phenyl) pyrimidin-2-yl)-N, N-dimethylformamidine derivatives (4a–f), were prepared from aryl and heteroaryl acetophenones (3a–c) and 4,6-diaryl-substituted pyrimidine-5-carboxaldehydes (2a–b) via Claisen–Schmidt condensation. The structures of the synthesized compounds were confirmed through spectroscopic techniques, including IR, ¹HNMR, ¹³CNMR, mass spectrometry, and elemental analysis. The synthesized compounds were evaluated for their in vitro antibacterial activity against E. coli (Gram-negative) and S. aureus (Gram-positive). Notably, compounds exhibited significant inhibitory activity against E. coli, with compound 5a demonstrating superior performance, whereas moderate to poor activity was observed against S. aureus. Furthermore, molecular docking studies were conducted using the E. coli DNA gyrase B protein (PDB ID: 1KZN) to investigate the binding affinities of the ligands. Compounds 5a and 5b showed the highest docking scores and favourable binding interactions at the active site, correlating well with their biological activity. These results suggest that pyrimidin-2-amine derivatives, particularly 5a and 5b, represent promising candidates for the development of potent antibacterial agents targeting Gram-negative pathogens.
Microwave-assisted green synthesis and molecular docking study of some new 4-thiazolidinone derivatives as possible bioactive agents
Satish Shamrao Kola, Vishnu Nayak Badavath, Mohammad Idrees M. Siddique, Naqui Siddiqui, Chandrashekhar Devkate, Syed Abrar Ahmed
Indian Journal of Heterocyclic Chemistry, 2024
We have developed an economical and environmentally friendly microwave-assisted efficient method for the synthesis of a series of new 4-oxo-thiazolidine derivatives (4a-d). The method involves microwave irradiated cyclocondensation reaction of Schiff bases (3a-d) and thioglycolic acid in drug master file (DMF). 4-oxo-thiazolidine derivatives (4a-d) was also synthe 4-Oxo-Thiazolidine derivatives were also synthesized by conventional heating procedures and consequence were Compared with Microwave assisted green method. The results suggest that microwave-assisted syntheses lead to higher yields within very short reaction times. Antimicrobial screening of all the synthesized compounds was carried out using Gram-positive strains Staphylococcus aureus and Gram-negative strain encompassing Escherichia coli, Proteus vulgaris, and Salmonella typhi. The results were compared with the standard drug chloramphenicol. All the synthesized compounds were subsequently examined using molecular docking experiments against peptide deformylase (PDB ID: 1G2A), which evaluates the binding interaction of ligands with enzyme active sites.. KEYWORDS :Microwave irradiation, Thiazolidinone, Molecular docking, Peptide deformylase, Antimicrobial screening.
Synthesis of few 1,3,4-oxadiazole derivatives blended with different heterocycles and their in-vitro antibacterial activities
M. Idrees, Y.G. Bodkhe, N. J. Siddiqui, S. Kola
Rasayan Journal of Chemistry, 2020
Synthesis, characterization and in vitro antimicrobial screening of some novel series of 2-azetidinone derivatives integrated with quinoline, pyrazole and benzofuran moieties
M. Idrees, Y.G. Bodkhe, N.J. Siddiqui, S.S. Kola
Asian Journal of Chemistry, 2020
A series of 5-(benzofuran-2-yl)-N-(3-chloro-4-(2-(p-tolyloxy) substituted quinolin-3-yl)-2-oxoazetidin-1-yl)-1-phenyl-1H-pyrazole-3-carboxamide derivatives (4a-f) were synthesized with excellent yields by cyclocondensation reaction of 5-(benzofuran-2-yl)-N′-(2-(p-tolyloxy) substituted quinolin-3-yl)methylene)-1-phenyl-1H-pyrazole-3-carbohydrazide (3a-f) with chloroacetyl chloride in presence of triethylamine in DMF. One pot condensation of 5-(benzofuran-2-yl)-1-phenyl-1H-pyrazole-3-carbohydrazide (1) with 2-(p-tolyloxy) substituted quinoline-3-carbaldehyde (2a-f) in ethanol solvent in presence of catalytic amount of acetic acid gave intermediate compounds (3a-f). The structures of newly synthesized compounds have been substantiated through elemental analysis and spectral studies viz. 1H NMR, 13C NMR, IR and mass spectra. All the synthesized compounds were screened for their in vitro antibacterial activity against pathogenic bacteria such as S. aureus and E. coli at different concentrations.
Synthesis, characterization and antimicrobial screening of some novel 5-(benzofuran-2-yl)-N’-(2-substituted-4-oxothiazolidin-3-YL)-1-phenyl-1hpyrazole- 3-carboxamide derivatives
M. Idrees, S. Kola, N. J. Siddiqui
Rasayan Journal of Chemistry, 2019
A series of innovative 5-(benzofuran-2-yl)-N'-(2-substituted-4-oxothiazolidin-3-yl)-1-phenyl-1H-pyrazole-3carboxamide (4a-i) derivatives were synthesized by cyclocondensation reaction of various carbohydrazones (3a-i) with thioglycolic acid in DMF. The intermediate N'-(benzylidene)-5-(benzofuran-2-yl)-1phenyl-1H-pyrazole-3-carbohydrazides (3a-i) was obtained by condensation of 5-(benzofuran-2-yl)-1-phenyl-1Hpyrazole-3-carbohydrazide (1) with various substituted aromatic aldehydes (2a-i) in ethanol. The structures of newly synthesized compounds (4a-i) were corroborated through elemental analysis and spectral studies like IR, 1 H NMR, 13 C NMR and Mass spectra. The compounds were screened for their in-vitro antibacterial activity against a panel of pathogenic microorganism including gram-negative strains E. coli, P. vulgaris and S. typhi and grampositive bacterial strain, S. aureus at diverse concentrations and the result of bioassay was compared with Chloramphenicol.
Synthesis and antimicrobial screening of some new 5-oxo-imidazoline derivatives containing benzofuran, pyrazole and quinoline entities
Indian Journal of Heterocyclic Chemistry, 2019
Synthesis of novel series of quinolino[3,2-f][1,2,4]triazolo[3,4-b][1,3,4]-thiadiazepines derivatives incorporated with 3-[5-(benzofuran-2-yl)-1-phenyl-1H-pyrazol-3-yl] moiety as potent antimicrobial agent
M. Idrees, S. Kola, N.J. Siddiqui
Asian Journal of Chemistry, 2018