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A series of new (E)-1-[2-(2-ethylpyridin-4-yl)-4-methylthiazol-5-yl]-3-phenylprop-2-en-1-one derivatives have been synthesized starting from the antitubercular drug, ethionamide. The synthesized compounds have been tested for their in vitro antimicrobial activity, and five of those have demonstrated promising activity. According to molecular docking study the active compounds have display high binding affinity towards DNA Gyrase and Lumazine Synthase.

In the present study, two series of tetrazole containing maleamic (5a-h) and phthaleamic acid (5i-l) derivatives were synthesized and evaluated for their antimicrobial and β-lactamase enzyme inhibition activities. The synthesized compounds were characterized by IR, 1H NMR and 13C NMR spectral techniques. Among the screened compounds, the compound 5c, 5d, 5e, 5f, 5g and 5h have shown good antimicrobial activity. We further performed exploratory β-lactamase enzyme inhibitors studies on β-lactamase.

In the present study, a series of sixteen new isoniazid embedded triazole derivatives have been synthesized. These compounds were evaluated for their in vitro antitubercular and antimicrobial activities. Among the screened compounds, six have exhibited potent antitubercular activity against Mycobacterium tuberculosis H37Rv strain with MIC value 0.78 μg/mL, Whereas, three compounds have displayed activity with MIC value ranging from 1.56 to 3.125 μg/mL. The cytotoxicity of the active compounds was studied against RAW 264.7 cell line by MTT assay and no toxicity was observed even at 25 μg/mL concentration. The five compounds have displayed good antimicrobial activities. Molecular docking have been performed against mycobacterial InhA enzyme to gain an insight into the plausible mechanism of action which could pave the way for our endeavor to identify potent antitubercular candidates. We believe that further optimization of these molecules may lead to potent antitubercular agents.

In a search for safer and potent antitubercular agents, here a library of newly substituted dioxoisoindolinylmethyl-triazolyl-N-phenylacetamide derivatives (5a–l) has been synthesized via click chemistry approach. All synthesized compounds were evaluated for their antitubercular activity against Mycobacterium tuberculosis H37Rv (MTB). Among the screened compounds, 5d, 5e, 5h, and 5l showed good antitubercular activity. The compounds 5d and 5l have shown very effective antitubercular activity against Mycobacterium tuberculosis H37Rv (MTB) with MIC 12.5 μg/mL. All the newly synthesized compounds were thoroughly characterized by 1H NMR, 13C NMR, and HRMS spectral data. We further performed exploratory docking studies on the crystal structure of Mycobacterium tuberculosis enoyl reductase to demonstrate the mechanism of antitubercular activity.

The present study describes designing, synthesis and anticancer screening of a proline rich cyclic octapeptide polycarponin C, by solution phase synthesis. The synthesis was carried out by coupling a tetrapeptide Boc-Pro-Thr-Leu-Pro-OH with another tetrapeptide Boc-Pro-Val-Leu-PheOH, followed by cyclization of the linear octapeptide.The structure of the synthesized compound was then confirmed by spectral analysis. From the results of biological activity, it was concluded that the compound has shown moderate activity against SR human tumor cell lines of Leukemia when compared with Vincristine as a standard. key words:Cyclic Peptide, Solution phase synthesis, p-nitro phenyl ester Method, Coupling Agent, Anticancer.

Synthesis of new drug for anticancer activity has always been fascinating and interesting for researchers. Increase in the demand for new anticancer agents promotes the researchers for synthesizing new molecules with good activity on human cancer cell lines. Here design, synthesis and cytotoxic, antimicrobial activity of delavayin A is described. The structure of this synthesized compound was confirmed by (IR), 1H NMR, 13C NMR, Mass and elemental analysis. The synthesized compound was evaluated for in vitro cytotoxic activity by using Brine shrimp assay and on PC 3 and HL-60 cancer cell lines at Advanced Centre for Treatment Research and Education in Cancer (ACTREC), Mumbai. The compound was also evaluated for antimicrobial activity by using minimum inhibitory concentration (MIC) technique. The synthesized cyclopeptide possessed moderate cytotoxic activity against cell lines and found to show moderate activity against Gram positive bacteria. Key words: Cyclopeptide, cytotoxic, antimicrobial, p-nitro phenyl ester method.

In a search of new antitubercular agents, herein we have reported a series of new thirty-two indanol-1,2,3-triazole derivatives. The synthesized compounds were screened for their in vitro antitubercular and antimicrobial activities. Among the screened compounds, most of the compounds have displayed good antitubercular activity against Mycobacterium tuberculosis H37Rv. The compound 5g has been identified as potent antitubercular agent with MIC value 1.56 µM. The most active compounds of the series were further studied for their cytotoxicity against HEK 293 cells using MTT assay and found to be nontoxic. In addition, ten compounds were shown good antimicrobial activities against both antibacterial and antifungal pathogens. A molecular docking study against Mycobacterial enoyl-ACP-reductase (InhA) was performed to gain an insight into the molecular mechanism of antitubercular action. The pharmacokinetic parameters of these compounds were studied and displayed acceptable drug-likeness score.

A large number of significant bioactive natural and synthetic alkyl(methyl)maleic anhydrides are known in the contemporary literature. A broad range of suitably functionalized substrates have been tailored to accomplish concise and efficient syntheses of an array of alkyl(methyl)maleic anhydrides employing a variety of elegant synthetic strategies. This review presents a brief literature account of the isolation and activity of these important target compounds with a special emphasis on their synthesis. 1 Introduction 2 Recent Synthetic Strategies towards the Natural and Unnatural Alkyl(methyl)maleic Anhydrides 2.1 Dimethylmaleic Anhydride 2.2 Ethyl/hexyl/octyl(methyl)maleic Anhydrides 2.3 Chaetomellic Anhydrides A–C 2.4 Tyromycin A 2.5 Aspergillus Acids A–D 2.6 Tautomycin and Tautomycetin 2.7 Lindenanolide E, Itaconitin, Graphenone and 2,3-Didehydrotelfairic Anhydride 2.8 Synthetic Analogues of Alkyl(methyl)maleic Anhydrides 3 Summary

Diabetes mellitus is a chronic endocrine disorder that affects the metabolism of carbohydrates, proteins, fat, electrolytes and water. α -Amylase and α -glucosidase are the important enzymes required for the digestion of the carbohydrate. These enzymes plays a vital role in the breakdown of starch in the diet and its activity has been correlated to postprandial blood glucose levels, the control of which is essential for maintaining quality of life for diabetic patients. We report the synthesis, characterization and biological evaluation of new substituted 2-phenoxynicotinaldehydes as α -amylase inhibitors. A new general method based on the aromatic nucleophilic substitution reactions of 2-chloronicotinaldehyde with different substituted phenols in presence of K 2 CO 3 in dry dioxane was developed to furnish the corresponding substituted 2-phenoxynicontinaldehydes with 70-80% yields.

Starting from citraconic anhydride, a three-step approach to fimbrolide congener is reported by taking the advantage of a regioselective Grignard reaction with an anhydride, followed by a dehydrative cyclization and double bromination-dehydrobromination sequence. Starting from N-(4-tolyl)maleimide, an eight-step synthesis of two natural fimbrolides is reported with good yields via the synthesis of requisite butylmaleic anhydride, its regioselective Grignard coupling reaction, and a bromination-dehydrobromination pathway.

A simple and efficient access to alkyl and dialkyl substituted maleimides has been demonstrated via the new contrathermodynamic rearrangement of ( E )-alkylidenesuccinimides to alkylmaleimides. The ( E )-alkylidenesuccinimides obtained from the Wittig-condensation of N -arylmaleimide with aliphatic aldehydes on regioselective hydrolysis furnished the corresponding ( E )-alkylidenesuccinanilic acids in 95–98% yields. The β-alkylidenesuccinanilic acids on treatment with cyanuric chloride in the presence of triethylamine gave the corresponding β-alkylisomaleimides in 78–80% yields via the β-alkylideneisosuccinimides with the exocyclic to endocyclic carbon–carbon double bond migration. The kinetically controlled products alkylisomaleimides in refluxing acetic acid furnished the thermodynamically controlled alkylmaleimides in 98% yield. The Wittig condensation of alkyl substituted isomaleimides/maleimides with aliphatic aldehydes gave the desired dialkyl substituted maleimides in high yields. A conversion of α-methylenesuccinanilic acids to α-methylisomaleimides has also been described, with 90% yield.

A large number of significant bioactive natural and synthetic alkyl(methyl)maleic anhydrides are known in the contemporary literature. A broad range of suitably functionalized substrates have been tailored to accomplish concise and efficient syntheses of an array of alkyl(methyl)maleic anhydrides employing a variety of elegant synthetic strategies. This review presents a brief literature account of the isolation and activity of these important target compounds with a special emphasis on their synthesis. 1 Introduction 2 Recent Synthetic Strategies towards the Natural and Unnatural Alkyl(methyl)maleic Anhydrides 2.1 Dimethylmaleic Anhydride 2.2 Ethyl/hexyl/octyl(methyl)maleic Anhydrides 2.3 Chaetomellic Anhydrides A–C 2.4 Tyromycin A 2.5 Aspergillus Acids A–D 2.6 Tautomycin and Tautomycetin 2.7 Lindenanolide E, Itaconitin, Graphenone and 2,3-Didehydrotelfairic Anhydride 2.8 Synthetic Analogues of Alkyl(methyl)maleic Anhydrides 3 Summary

Starting from alkylidenesuccinimides, a wide range of dialkylmaleic anhydrides have been synthesized via the generation of a carbanion on a succinimide unit and its condensation with various alkyl halides as the key reaction.

Starting from alkylidenesuccinimides, a wide range of dialkylmaleic anhydrides have been synthesized via the generation of a carbanion on a succinimide unit and its condensation with various alkyl halides as the key reaction.

Starting from maleanilic and maleamic acids, a facile general approach to kinetically controlled isomaleimides has been described for the first time using cyanuric chloride as a dehydrating agent with 85–98% yields. The effect of a variety of substituents present on the aromatic ring in amine and maleic anhydride moiety, on these kinetic/thermodynamic dehydration processes of anilic acids has been also described. Under the same set of reaction conditions the phthalanilic acid gave kinetically controlled product, isophtalimide in 91% yield, while the corresponding succinanilic acid furnished the thermodynamically more stable succinimide in high yield.