Amit M. Dodiya

Conventional and microwave techniques for synthesis and antimicrobial studies of novel 1-[2-(2-chloro(3-quinolyl))-5-(4-nitrophenyl)-(1,3,4-oxadiazolin-3-yl)]-3-(aryl)prop-2-en-1-ones

In this article, we have described the conventional and microwave method for the synthesis of 1-[2-(2-chloro(3-quinolyl))-5-(4-nitrophenyl)(1,3,4-oxadiazolin-3-yl)]-3-(aryl)prop-2-en-1-ones (4a–l). Through this method, we have achieved reduction in reaction time and better yield than the previously described conventional method. The application of microwave irradiation (MWI) is used for carrying out chemical transformations which are pollution-free and eco-friendly. The structure of the compounds was characterized by spectral data. These compounds (4a–l) were evaluated for their in vitro antimicrobial screening on different strains of bacteria and fungi.

Synthesis, characterization, anticancer activity, and QSAR-studies of some new tetrahydropyrimidines

Several new substituted 1,2,3,4 tetrahydropyrimidine derivatives have been synthesized and evaluated for their in vitro anticancer activity on various cell lines. Some of the molecules have exhibited significantly potent inhibition on several cell lines. To find out inter correlation between anticancer activity and molecular descriptors, QSAR study was carried out. Molecular descriptors used for the study were ClogP (lipophilic), CMR (steric), and polarity (electronic). Anticancer activity is expressed in the form of LogGI50+. Activity on different cell lines was independently correlated with molecular descriptors. On the basis of the results, significant correlation between anticancer activity on some of the cell lines and molecular descriptor was observed.

Synthesis, characterization, and antimicrobial evaluation of novel naphthalene-based 1,2,4-triazoles

In order to search for new bioactive molecules with significant antimicrobial action, a series of 1,2,4-triazole and naphthalene analogs bearing structurally diverse substituents, N-(3-mercapto-5-(naphthalen-1-yl)-4H-1,2,4-triazol-4-yl)(aryl)amides 3a–l were synthesized in good yield by a multi-step synthetic procedure. Their antimicrobial activity was screened against various Gram-positive and Gram-negative bacteria and fungi. Compounds 3a, 3f, 3g, 3j, and 3k exerted strong inhibition of the investigated bacterial and fungal strains compared to control antibiotic ampicillin and antifungal griseofulvin. On the basis of statistical analysis, it is observed that the compounds give significant co-relation. All the synthesized compounds have been characterized by IR, 1H NMR, 13C NMR, and mass spectral data.

Antimicrobial screening of novel synthesized benzimidazole nucleus containing 4-oxo-thiazolidine derivatives

As a part of systematic investigation of synthesis, characterization and antimicrobial screening of some novel 3-(2-(6-methyl-1H-benzo[d]imidazol-2-yl)phenyl)-2-(aryl)thiazolidin-4-ones (3a–l), have been synthesized from Schiff bases of N-arylidene-2-(6-methyl-1H-benzo[d]imidazol-2-yl)anilines, (2a–l). The Schiff bases (2a–l) were prepared by condensation of different aldehydes with 2-(6-methyl-1H-benzo[d]imidazol-2-yl)aniline (1). The compound (1) was obtained from 2-amino benzoic acid and 4-methylbenzene-1,2-diamine. All the synthesized compounds were screened for in vitro antibacterial and antifungal activities on Escherichiacoli, Staphylococcusaureus, Pseudomonasaeruginosa, Staphylococcuspyogenes, Candidaalbicans, Aspergillusniger, and Aspergillusclavatus. The structures of the compounds synthesized were elucidated by IR, 1H-NMR, 13C-NMR, and mass spectra.

A clubbed quinazolinone and 4-thiazolidinone as potential antimicrobial agents

A series of N-{5-[(2-chlorophenyl)methylene]-2-(4-hydroxyphenyl]-4-oxo(1,3-thiazolidin-3-yl)}{4-[2-(4-methylphenyl)-4-oxo(3-hydroquinazolin-3-yl)]phenyl}carboxamides (6a–n) have been synthesized. All the synthesized compounds were screened for in vitro antibacterial and antifungal activities on Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Staphylococcus pyogenes, Candida albicans, Aspergillus niger, and Aspergillus clavatus. The structures of the compounds were elucidated by IR, 1H NMR, 13C NMR, and Mass spectra.

A search of novel antimicrobial based on benzimidazole and 2-pyridone heterocycles

The increasing incidence of bacterial drug resistance imposes a new search on existing antimicrobial drugs leading to the development of new bioactive molecules. In continuation to this, the present article deals with the synthesis and antimicrobial activity of 1-(1-(1H-benzo[d]imidazol-2-yl)ethylideneamino)-6-(arylideneamino)-4-(2-hydroxyphenyl)-2-oxo-1,2-dihydropyridine-3,5-dicarbonitriles (4a–k). All newly synthesized compounds have been evaluated against two gram positive bacteria (Staphylococcus aureus, Streptococcus pyogenes), two gram negative bacteria (Escherichia coli, Pseudomonas aeruginosa), and three fungi (Candida albicans, Aspergillus niger, Aspergillus clavatus) using serial broth dilution method. Compounds reported in the present article bearing chloro and hydroxy groups exhibit very good to excellent antimicrobial activity. All the newly synthesized compounds have been characterized by IR, 1H NMR, 13C NMR, and mass spectra.

Dimeric 2-(2-chlorophenyl)-quinazolin-4-ones as potential antimicrobial agents

Abstract3-(Aryl)-2-(2-chlorophenyl)-6-{2-[2-(2-chlorophenyl)-4-oxo(3-hydroquinazolin-3yl)]ethyl}-3-hydroquinazolin-4-ones had been selected as target bio-active molecules. Several quinazoline derivatives were prepared by using anthranilic acid, acid chloride, 2-amino-ethanol, and different amines. Newly synthesized compounds were screened for their antibacterial and antifungal activities on Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Staphylococcus pyogenes, Candida albicans, Aspergillus niger, and Aspergillus clavatus. The compounds 5e, 5g, and 5h are shown to have excellent activity, while 5c, 5d, 5i, 5k, 5l are shown to have very good activity against several strains of bacteria. The structures of the synthesized compounds were firmly established by well-defined spectral analysis techniques like IR, 1H-NMR, 13C-NMR, and Mass spectra.

Synthesis and antimicrobial activity of novel quinazolinone–thiazolidine–quinoline compounds

Abstract A series of 2-(2-chloroquinolin-3-yl)-5-((aryl)benzylidene)-3-(4-oxo-2-phenylquinazolin-3(4H)-yl)thiazolidin-4-ones (V)1–12 have been synthesized. In order to establish optimization of different parameters of chemical transformation, that is the reaction pathway for each step and reaction conditions in the each step, in the present paper, different solvents and catalysts were used. The structures of the synthesized compounds were assigned on the basis of elemental analysis, IR, 1H NMR and 13C NMR spectral data. All the newly synthesized compounds were screened against various strains of bacteria and fungi.

Synthesis, characterization and antimicrobial screening of thiazole based 1,3,4-oxadiazoles heterocycles

Abstract In an effort to find a new pharmacologically dynamic molecule, we report here the synthesis and in vitro antimicrobial activity of various N-(4-methyl-5-(4-((substituted phenylamino) methyl)-5-thioxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)thiazol-2-yl) benzamides. The structures of newly synthesized compounds were assigned on the bases of IR, 1H NMR, 13C NMR, and mass spectral data. Synthesized compounds were screened for their antibacterial and antifungal activities on gram-positive bacteria (Staphylococcus aureus and Streptococcus pyogenes), gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa) and three fungi (Candida albicans, Aspergillus niger and Aspergillus clavatus) by serial broth dilution method. Compounds 5e and 5k were associated with considerable potential antibacterial and compounds 5a and 5b antifungal activities.

Hybrid Bioactive Heterocycles as Potential Antimicrobial Agents- A Review

The ever increasing cases of microbial resistance pose a major threat to the scientific community and therefore the need for discovery and development of newer antimicrobial agents with novel mode of action is becoming critical. One of the ways to tackle this herculean problem is to generate hybrid molecules by combining two or more bioactive heterocyclic moieties in a single molecular platform. The review here describes published results of our research groups endeavors towards development of potential new and safe antimicrobial agents with better effectiveness by using the hybrid approach. In the present review article the landscaping of heterocycles like 4-thiazolidinones, benzimidazole and quinoline are described. Compounds displaying two of more fold antimicrobial activity are included in the review.