Background:
A series of new six thiazolyl-2-amine based Schiff base derivatives (4a-4f) were synthesized by a sequential multistep reactions starting with Salicylaldehyde.
Objective:
All the Schiff base derivatives were screened in-vitro for their antibacterial activity against Mycobacterium tuberculosis (H37RV strain) ATCC No-27294. The synthesized compounds were characterized by FTIR, 1H-NMR, 13C-NMR and Mass spectrometry.
Results:
Among the compounds tested, 4c and 4f exhibited potent antitubercular activity against M. Tuberculosis at MIC 6.25 µg/mL.
Conclusion:
We extended our study to explore the inhibition mechanism by conducting molecular docking analysis by using Schrodinger’s molecular modeling software. All the newly synthesized compounds were found to be in-silico AMES test non-toxic and non-carcinogens. The good Qikprop’s Absorption, Distribution, Metabolism and Excretion (ADMET) would definitely be help the researchers in order to make more potent Anti-TB agents.
Trichobezoars (hair ball) are usually located in the stomach, but may extend through the pylorus into the duodenum and small bowel (Rapunzel syndrome). Rapunzel syndrome remains uncommon; with fewer than 40 cases reported. To the best of our knowledge, this case may be the first well-documented case with a length of 75 cm. They are almost always associated with trichotillomania and trichophagia or other psychiatric disorders. In the literature several treatment options are proposed, including removal by conventional laparotomy, laparoscopy and endoscopy. Herein, we are reporting an interesting case of an 18-year mentally retarded girl with history of trichotillomania and trichophagia who presented to our emergency department with a history of central abdominal pain associated with vomiting and constipation for five days. An examination showed a trichobezoar requiring emergent surgical intervention, and indicating the need for psychiatric treatment. The trichobezoar was treated successfully by laparoscopy.
A series of substituted 2,7-dimethylimidazo[1,2-a]pyridine-3-carboxamides derivatives 5a-5m were synthesized through multi-step reactions. To achieve the synthesis of the desired compounds monobromo and dibromo substituted 2-amino-γ-picoline was reacted with ethyl 2-chloroacetoacetate. The crude ethyl ester subjected to hydrolysis in presence of lithium hydroxide to get 2a and 2b, with imidazo[1,2-a]pyridine-3-carboxylic acid to get 3a-3b, on treatment with substituted amines 4a-4g to get desired product 5a-5m in presence of EDCI and HOBt. The substituted imidazo[1,2-a]pyridine-3-carboxamides are characterized by FTIR, 1 H-NMR, 13 C-NMR and mass spectra. These newly synthesized compounds were tested in vitro for their antimycobacterial activity. The preliminary results of antituberculosis study showed that most of the synthesized compounds 5a-5m demonstrated moderate to good antituberculosis activity. Among the tested compounds 5b, 5d and 5e were found to be the most active with minimum inhibitory concentration (MIC) of 12.5 μg/mL against Mycobacterium tuberculosis (H37 RV strain) ATCC No-27294.
Malaria is a serious illness transmitted through the bite of an infected mosquito, which is caused by a type of parasite called plasmodium and can be fatal if left untreated. Thus, newer antimalarials with unique mode of actions are encouraged. Fused pyridines have been vastly reported for numerous pharmacological activities including but not limited to analgesics, antitubercular, antifungal, antibacterial and antiapoptotic agents. In a current study, a series of substituted Imidazo[1,2-a]pyridine-3-carboxamides (IMPCs) (SM-IMP-01-13) along with some hydrazides (DA-01-DA-02) were synthesized and characterized by Fourier-transform infrared spectroscopy (FTIR), 1H-/[Formula: see text]C-NMR (proton/carbon nuclear magnetic resonance), elemental analyses and mass spectra. These synthesized analogies were subjected for in vitro biological activities such as Brine Shrimp lethality (BSL), and assay of [Formula: see text]-hematin formation inhibitions. The BSL assay results suggested that compounds, SM-IMP-09, SM-IMP-05 were found to be less toxic and they also had comparable toxicity as of 5-Flurouracil (control) ((e.g., at 10 [Formula: see text]g/ml: 20% deaths of nauplii). Derivatives SM-IMP-02, and DA-05inhibited [Formula: see text]-hematin formation: IC[Formula: see text]: 1.849 and 0.042 [Formula: see text]M, respectively). Our molecular docking analysis on plasmodial cysteine protease falcipain-2 indicated that compound DA-05(–9.993 kcal/mol) had highest docking score and it was comparable to standard Chloroquine (–7.673 kcal/mol). The most active molecule, DA-05 was also retained with lower HOMO–LUMO energy gap as 3.36 eV. Further, we have also analyzed MEP, and other global reactivity indexes for all IMPCs using DFT. Finally, our in-silico pharmacokinetic analysis suggested that all compounds were having good% human oral absorption values ([Formula: see text]100%), good Caco-2 cell permeabilities ([Formula: see text]1600 nm/s), and non-carcinogenic profiles.
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