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Antimycobacterial activity: synthesis of novel 3-(substituted phenyl)-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]isoxazole analogues

Ali MA, Ismail R, Choon TS, Pandian S, Hassan Ansari MZ

J Enzyme Inhib Med Chem, 2011 Aug;26(4):598-602.

PMID: 21714764 DOI: 10.3109/14756366.2010.529805

In this study, a series of novel 3-(substituted phenyl)-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]isoxazole analogues were synthesized and evaluated for antimycobacterial activity against Mycobacterium tuberculosis (MTB) H(37)Rv and isoniazid resistant M. tuberculosis (INHR-MTB). All the newly synthesized compounds were showing moderate to high inhibitory activities. The compound 6,7-dimethoxy-3-(4-chloro phenyl)-4H-indeno[1,2-c]isoxazole (4b) was found to be the most promising compound, active against MTB H(37)Rv and INHR-MTB with minimum inhibitory concentrations of 0.22 and 0.34 μM.

Proteomics and genomics insights on malignant osteosarcoma

Kathiresan N, Selvaraj C, Pandian S, Subbaraj GK, Alothaim AS, Safi SZ, et al.

Adv Protein Chem Struct Biol, 2024;138:275-300.

PMID: 38220428 DOI: 10.1016/bs.apcsb.2023.06.001

Osteosarcoma is a malignant osseous neoplasm. Osteosarcoma is a primary bone malignancy capable of producing osteoid tissue or immature bones. A subsequent malignant degeneration of the primary bone pathology occurs less frequently in adults. The over-expression of several proteins, including Heat shock proteins, Cofilin, Annexins, Insulin-like growth factor, transforming growth factor-β, Receptor tyrosine kinase, Ezrin, Runx2, SATB2, ATF4, Annexins, cofilin, EGFR, VEGF, retinoblastoma 1 (Rb1) and secreted protein, has been associated to the development and progression of osteosarcoma. These proteins are involved in cell adhesion, migration, invasion, and the control of cell cycle and apoptosis. In genomic studies, osteosarcoma has been associated with several genetic abnormalities, including chromosomal rearrangements, gene mutations, and gene amplifications. These differentially expressed proteins could be used as early identification biomarkers or treatment targets. Proteomics and genomics play significant parts in enhancing our molecular understanding of osteosarcoma, and their integration provides essential insights into this aggressive bone cancer. This review will discuss the tumour biology that has assisted in helping us better understand the causes of osteosarcoma and how they could potentially be used to find new treatment targets and enhance the survival rate for osteosarcoma patients.

Fulltext Synthesis and anti-HIV activity of novel 3-substituted phenyl-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]isoxazole analogues

Ali MA, Ismail R, Choon TS, Yoon YK, Wei AC, Pandian S, et al.

Acta Pol Pharm, 2011 May-Jun;68(3):343-8.

PMID: 21648188

A series of novel 3-(substituted phenyl)-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]isoxazole analogues were synthesized by the reaction of 5,6-dimethoxy-2-[(E)-1-phenylmethylidene]-1-indanone with hydroxylamine hydrochloride. The title compounds were tested for their in vitro anti-HIV activity. Among the compounds, (4g) showed a promising anti-HIV activity in the in vitro testing against IIIB and ROD strains. The IC50 of both IIIB and ROD were found to be 9.05 microM and > 125 microM, respectively.

Discovery of novel methanone derivatives acting as antimycobacterial agents

Ali MA, Bastian S, Ismail R, Choon TS, Ali S, Aubry A, et al.

J Enzyme Inhib Med Chem, 2011 Dec;26(6):890-4.

PMID: 21395486 DOI: 10.3109/14756366.2011.559945

A series of pyrazoline derivatives were synthesized and in vitro activity against Mycobacterium tuberculosis H37Rv was carried out. Among the synthesized compounds, compounds (4d) and (4f) 4-aminophenyl-3-(3,4-dimethoxyphenyl)-6,7-dimethoxy-2,3,3a,4-tetrahydroindeno[1,2-c]pyrazol-2-ylmethanone and 4-aminophenyl-6,7-dimethoxy-3-phenyl-2,3,3a,4-tetrahydroindeno[1,2-c]pyrazol-2-ylmethanone were found to be the most active agent against M. tuberculosis H37Rv with a minimum inhibitory concentration of 10 μg/mL.

Synthesis and discovery of novel hexacyclic cage compounds as inhibitors of acetylcholinesterase

Suresh Kumar R, Ashraf Ali M, Osman H, Ismail R, Choon TS, Yoon YK, et al.

Bioorg Med Chem Lett, 2011 Jul 1;21(13):3997-4000.

PMID: 21621414 DOI: 10.1016/j.bmcl.2011.05.003

Hexacyclic derivatives share vital pharmacological properties, considered useful in Alzheimer's disease. The aim of this study was synthesis and its evaluation for acetyl cholinesterase inhibitory activity of novel hexacyclic analogues. Compound 4f, showed potent inhibitory activity against acetyl cholinesterase enzyme with IC(50) 0.72 μmol/L.

Substituted spiro [2.3'] oxindolespiro [3.2″]-5,6-dimethoxy-indane-1″-one-pyrrolidine analogue as inhibitors of acetylcholinesterase

Ali MA, Ismail R, Choon TS, Yoon YK, Wei AC, Pandian S, et al.

Bioorg Med Chem Lett, 2010 Dec 1;20(23):7064-6.

PMID: 20951037 DOI: 10.1016/j.bmcl.2010.09.108

Series of pyrolidine analogues were synthesized and examined as acetylcholinesterase (AChE) inhibitors. Among the compounds, compounds 4k and 6k were the most potent inhibitors of the series. Compound 4k, showed potent inhibitory activity against acetyl cholinesterase enzyme with IC(50) 0.10 μmol/L. Pyrolidine analogues might be potential acetyl cholinesterase agents for AD.

Systematic review of clinical practice guidelines for traumatic dental injuries

Saikia A, Patil SS, Ms M, Cv D, Sabarish R, Pandian S, et al.

Dent Traumatol, 2023 Aug;39(4):371-380.

PMID: 36920339 DOI: 10.1111/edt.12838

BACKGROUND/AIMS: Traumatic dental injuries (TDI) are considered a public health problem due to their high prevalence and associated physical, economic, psychological and social consequences. Hence, good Clinical Practice Guidelines are essential to achieving a favourable prognosis. The aim of this review was to appraise the existing Clinical Practice Guidelines (CPGs) on TDI using AGREE II and AGREE-REX.

MATERIALS AND METHODS: A systematic search for existing guidelines on TDI was performed on PubMed, EMBASE, CINAHL, Cochrane Library, ProQuest, National Institute for Health Care Excellence, BMJ Best Practice, Trip database, Guideline International Network, Scottish Intercollegiate Guidelines Network, World Health Organisation, Web of Science and 'Ministry of Health worldwide' databases. Four appraisers independently appraised the included CPGs. The AGREE II tool was applied to assess the methodological quality, while AGREE REX assessed the quality of recommendations of the included guidelines.

RESULTS: Of the 7736 titles screened, three guidelines, namely the International Association of Dental Traumatology Guidelines (IADT), and the Italian and Malaysian guidelines, were included for the final analysis. These guidelines were published between 2019 and 2020. The AGREE II analysis demonstrated scores above 80% for the IADT and Italian guidelines for the scope and purpose domain. Overall, the Malaysian guidelines achieved the highest score for all domains. The AGREE REX analysis indicated variability in implementation across the nine items, with five that scored above the midpoint of 4.0 on the response scale. Both the Italian and the IADT guidelines had a similar score for the values and preference domains (36.36%).

CONCLUSIONS: Several deficiencies exist in the methodological quality of existing CPGs on TDI. Future guidelines should consider improvements for domains such as 'rigour of development', 'stakeholder involvement' and 'applicability' to overcome the existing limitations.

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