Osteoporosis is widely recognized as a major public health problem. It is a serious metabolic bone disorder that often results in hip fracture and is usually asymptomatic in its initial stages. It is mainly seen in elderly people as decreased quantities of sex hormones is one important factor causing bone loss. Most patients suffering from osteoporosis are post-menopausal women exhibiting loss of estrogen. Also, menopause is associated with a substantial decline in melatonin secretion which subsequently stimulates bone resorption. Numerous drugs are approved for both the prevention and treatment of osteoporosis but with multiple side effects. This book, therefore, provides new insights for developing novel melatonin analogues containing heterocyclic moieties that could be expected to be alternative modalities for prevention and intervention of osteoporosis in ovariectomized rats as an experimental model for postmenopausal osteoporotic women. Our finding could be useful for future strategies for osteoporosis management in postmenopausal women.